solubility

Summary

Top Publications

  1. ncbi Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
    C A Lipinski
    Central Research Division, Pfizer Inc, Groton, CT 06340, USA
    Adv Drug Deliv Rev 46:3-26. 2001
  2. ncbi A metalloproteinase disintegrin that releases tumour-necrosis factor-alpha from cells
    R A Black
    Immunex Corporation, Seattle, Washington 98101, USA
    Nature 385:729-33. 1997
  3. ncbi In vitro cytotoxicity of oxide nanoparticles: comparison to asbestos, silica, and the effect of particle solubility
    Tobias J Brunner
    Institute for Chemical and Bioengineering, Department of Chemistry and Applied Biosciences, ETH Zurich, CH 8093 Zurich, Switzerland
    Environ Sci Technol 40:4374-81. 2006
  4. ncbi Zeta potential and solubility to toxic ions as mechanisms of lung inflammation caused by metal/metal oxide nanoparticles
    Wan Seob Cho
    ELEGI Colt Laboratory, Centre for Inflammation Research, University of Edinburgh, Edinburgh EH16 4TJ, UK
    Toxicol Sci 126:469-77. 2012
  5. ncbi Enhancement of soluble protein expression through the use of fusion tags
    Dominic Esposito
    Protein Expression Laboratory, Research Technology Program, SAIC Frederick, Inc, NCI Frederick, Frederick, MD 21702, USA
    Curr Opin Biotechnol 17:353-8. 2006
  6. ncbi Pharmaceutical applications of cyclodextrins: basic science and product development
    Thorsteinn Loftsson
    Faculty of Pharmaceutical Sciences, University of Iceland, Reykjavik, Iceland
    J Pharm Pharmacol 62:1607-21. 2010
  7. ncbi Inhaled nanoparticles--a current review
    Wei Yang
    College of Pharmacy, University of Texas at Austin, TX 78712 1074, USA
    Int J Pharm 356:239-47. 2008
  8. ncbi Mechanisms of chaperone suppression of polyglutamine disease: selectivity, synergy and modulation of protein solubility in Drosophila
    H Y Chan
    Department of Biology, Howard Hughes Medical Institute, 415 South University Avenue, University of Pennsylvania, Philadelphia, PA 19104 6018, USA
    Hum Mol Genet 9:2811-20. 2000
  9. ncbi Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and 'self-microemulsifying' drug delivery systems
    C W Pouton
    Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, UK
    Eur J Pharm Sci 11:S93-8. 2000
  10. pmc Bimodal protein solubility distribution revealed by an aggregation analysis of the entire ensemble of Escherichia coli proteins
    Tatsuya Niwa
    Department of Medical Genome Sciences, Graduate School of Frontier Sciences, University of Tokyo, Kashiwa, Chiba 277 8562, Japan
    Proc Natl Acad Sci U S A 106:4201-6. 2009

Detail Information

Publications301 found, 100 shown here

  1. ncbi Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
    C A Lipinski
    Central Research Division, Pfizer Inc, Groton, CT 06340, USA
    Adv Drug Deliv Rev 46:3-26. 2001
    Experimental and computational approaches to estimate solubility and permeability in discovery and development settings are described...
  2. ncbi A metalloproteinase disintegrin that releases tumour-necrosis factor-alpha from cells
    R A Black
    Immunex Corporation, Seattle, Washington 98101, USA
    Nature 385:729-33. 1997
    ..Our results should facilitate the development of therapeutically useful inhibitors of TNF-alpha release, and they indicate that an important function of adamalysins may be to shed cell-surface proteins...
  3. ncbi In vitro cytotoxicity of oxide nanoparticles: comparison to asbestos, silica, and the effect of particle solubility
    Tobias J Brunner
    Institute for Chemical and Bioengineering, Department of Chemistry and Applied Biosciences, ETH Zurich, CH 8093 Zurich, Switzerland
    Environ Sci Technol 40:4374-81. 2006
    ..b>Solubility was found to strongly influence the cytotoxic response...
  4. ncbi Zeta potential and solubility to toxic ions as mechanisms of lung inflammation caused by metal/metal oxide nanoparticles
    Wan Seob Cho
    ELEGI Colt Laboratory, Centre for Inflammation Research, University of Edinburgh, Edinburgh EH16 4TJ, UK
    Toxicol Sci 126:469-77. 2012
    ..oxide NPs and attempted to relate various physicochemical parameters, including zeta potential (ζP) and solubility, to lung inflammogenicity...
  5. ncbi Enhancement of soluble protein expression through the use of fusion tags
    Dominic Esposito
    Protein Expression Laboratory, Research Technology Program, SAIC Frederick, Inc, NCI Frederick, Frederick, MD 21702, USA
    Curr Opin Biotechnol 17:353-8. 2006
    ..can sometimes solve the problem, the best available tools to date have been fusion tags that enhance the solubility of expressed proteins...
  6. ncbi Pharmaceutical applications of cyclodextrins: basic science and product development
    Thorsteinn Loftsson
    Faculty of Pharmaceutical Sciences, University of Iceland, Reykjavik, Iceland
    J Pharm Pharmacol 62:1607-21. 2010
    ..This short review is intended to provide both some basic science information as well as data on the ability to develop drugs in cyclodextrin-containing formulations...
  7. ncbi Inhaled nanoparticles--a current review
    Wei Yang
    College of Pharmacy, University of Texas at Austin, TX 78712 1074, USA
    Int J Pharm 356:239-47. 2008
    ..The potential application of pulmonary drug delivery of nanoparticles to the lungs, specifically in context of published results reported on nanomaterials in environmental epidemiology and toxicology is reviewed in this paper...
  8. ncbi Mechanisms of chaperone suppression of polyglutamine disease: selectivity, synergy and modulation of protein solubility in Drosophila
    H Y Chan
    Department of Biology, Howard Hughes Medical Institute, 415 South University Avenue, University of Pennsylvania, Philadelphia, PA 19104 6018, USA
    Hum Mol Genet 9:2811-20. 2000
    ..Our analysis also reveals that chaperones alter the solubility properties of the protein, indicating that chaperone modulation of neurodegeneration in vivo is associated with ..
  9. ncbi Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and 'self-microemulsifying' drug delivery systems
    C W Pouton
    Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath BA2 7AY, UK
    Eur J Pharm Sci 11:S93-8. 2000
    ..Priorities for future work are discussed. More data is needed on the solubility of drugs in various types of formulations, and in particular, on the relationship between the physical chemistry ..
  10. pmc Bimodal protein solubility distribution revealed by an aggregation analysis of the entire ensemble of Escherichia coli proteins
    Tatsuya Niwa
    Department of Medical Genome Sciences, Graduate School of Frontier Sciences, University of Tokyo, Kashiwa, Chiba 277 8562, Japan
    Proc Natl Acad Sci U S A 106:4201-6. 2009
    ..The aggregation propensity is most prominently correlated with the structural classification of proteins, implying that the prediction of aggregation propensity requires structural information about the protein...
  11. ncbi The solubility and stability of recombinant proteins are increased by their fusion to NusA
    Valeria De Marco
    EMBL Heidelberg, Meyerhofstrasse 1, D 69117 Heidelberg, Germany
    Biochem Biophys Res Commun 322:766-71. 2004
    ..Structural analysis indicated that the purified proteins were monodispersed and correctly folded. NusA has been used to raise antibodies that have been successfully used for Western blot and immunoprecipitation of NusA fusion proteins...
  12. ncbi Familial-associated mutations differentially disrupt the solubility, localization, binding and ubiquitination properties of parkin
    Sathya R Sriram
    Institute for Cell Engineering, Johns Hopkins University School of Medicine, Baltimore, MD 21205, USA
    Hum Mol Genet 14:2571-86. 2005
    ..mutations result in loss of parkin's E3 ligase activity, but they all appear to manifest as loss-of-function mutants due to defects in solubility, aggregation, enzymatic activity or targeting proteins to the proteasome for degradation.
  13. ncbi Curcumin-phospholipid complex: Preparation, therapeutic evaluation and pharmacokinetic study in rats
    Kuntal Maiti
    School of Natural Product Studies, Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700 032, India
    Int J Pharm 330:155-63. 2007
    ..The result proved that curcumin-phospholipid complex has better hepatoprotective activity, owe to its superior antioxidant property, than free curcumin at the same dose level...
  14. ncbi Soluble adenylyl cyclase as an evolutionarily conserved bicarbonate sensor
    Y Chen
    Department of Pharmacology, Joan and Sanford I Weill Medical College of Cornell University, 1300 York Avenue, New York, NY 10021, USA
    Science 289:625-8. 2000
    ..sAC is also expressed in other bicarbonate-responsive tissues, which suggests that bicarbonate regulation of cAMP signaling plays a fundamental role in many biological systems...
  15. ncbi Studies of curcumin and curcuminoids. XXVII. Cyclodextrin complexation: solubility, chemical and photochemical stability
    Hanne Hjorth Tønnesen
    Institute of Pharmacy, University of Oslo, P O Box 1068 Blindern, 0316 Oslo, Norway
    Int J Pharm 244:127-35. 2002
    Cyclodextrin complexes of the natural compound curcumin were prepared in order to improve the water solubility and the hydrolytic and photochemical stability of the compound...
  16. ncbi Comparative toxicity of nanoparticulate ZnO, bulk ZnO, and ZnCl2 to a freshwater microalga (Pseudokirchneriella subcapitata): the importance of particle solubility
    Natasha M Franklin
    Centre for Environmental Contaminants Research, CSIRO Land and Water, Private Mail Bag 7, Bangor, NSW, Australia 2234
    Environ Sci Technol 41:8484-90. 2007
    ..6), with a saturation solubility in the milligram per liter range, similar to that of bulk ZnO...
  17. ncbi The in vitro stability and in vivo pharmacokinetics of curcumin prepared as an aqueous nanoparticulate formulation
    Chandana Mohanty
    Institute of Life Sciences, Nalco Square, Bhubaneswar, Orissa 751023, India
    Biomaterials 31:6597-611. 2010
    Curcumin, the natural anticancer drug and its optimum potential is limited due to lack of solubility in aqueous solvent, degradation at alkaline pH and poor tissue absorption...
  18. pmc A seeding reaction recapitulates intracellular formation of Sarkosyl-insoluble transactivation response element (TAR) DNA-binding protein-43 inclusions
    Yoshiaki Furukawa
    Laboratory for Structural Neuropathology, RIKEN Brain Science Institute, Wako, Saitama 351 0198, Japan
    J Biol Chem 286:18664-72. 2011
    ..Although it has been so far difficult to initiate disease-associated changes of TDP-43 using cultured cell models, we propose that a seeding reaction is a key to construct a model to monitor TDP-43 pathologies...
  19. pmc Toward the structural genomics of complexes: crystal structure of a PE/PPE protein complex from Mycobacterium tuberculosis
    Michael Strong
    Howard Hughes Medical Institute, UCLA Department of Energy Institute of Genomics and Proteomics, University of California, Los Angeles, CA 90095, USA
    Proc Natl Acad Sci U S A 103:8060-5. 2006
    ..Our entire procedure for the identification, characterization, and structural determination of protein complexes can be scaled to a genome-wide level...
  20. ncbi Elevated placental soluble vascular endothelial growth factor receptor-1 inhibits angiogenesis in preeclampsia
    Shakil Ahmad
    Department of Reproductive and Vascular Biology, The Medical School, University of Birmingham, Edgbaston, Birmingham, West Midlands B15 2TG, UK
    Circ Res 95:884-91. 2004
    ..Our finding demonstrates the dysregulation of the VEGF/PlGF axis in preeclampsia and offers an entirely new therapeutic approach to its treatment...
  21. ncbi SOLpro: accurate sequence-based prediction of protein solubility
    Christophe N Magnan
    Institute for Genomics and Bioinformatics, School of Information and Computer Sciences, University of California, Irvine, CA, USA
    Bioinformatics 25:2200-7. 2009
    ..predict the propensity of a protein to be soluble on overexpression could be used, for instance, to prioritize targets in large-scale proteomics projects and to identify mutations likely to increase the solubility of insoluble proteins.
  22. pmc Improving the solubility of anti-LINGO-1 monoclonal antibody Li33 by isotype switching and targeted mutagenesis
    R Blake Pepinsky
    Department of Drug Discovery, Biogen Idec, Inc, Cambridge, Massachusetts 02142, USA
    Protein Sci 19:954-66. 2010
    ..However, the Li33 Fab had poor solubility when converted into a full antibody in an immunoglobulin G1 framework...
  23. ncbi Tagging recombinant proteins to enhance solubility and aid purification
    Dermot Walls
    School of Biotechnology and National Centre for Sensor Research, Dublin City University, Dublin, Ireland
    Methods Mol Biol 681:151-75. 2011
    ..The use of genetically engineered affinity and solubility-enhancing polypeptide "tags" has increased greatly in recent years and there now exists a considerable ..
  24. pmc Solubility-based genetic screen identifies RING finger protein 126 as an E3 ligase for activation-induced cytidine deaminase
    Rebecca K Delker
    Laboratories of Lymphocyte Biology, The Rockefeller University, New York, NY 10065, USA
    Proc Natl Acad Sci U S A 110:1029-34. 2013
    ..b>Solubility of a poorly soluble protein is thought to increase upon cofactor binding, possibly by masking otherwise exposed ..
  25. ncbi tRNA concentration fine tunes protein solubility
    Ivan Fedyunin
    Institute of Biochemistry and Biology, University of Potsdam, Potsdam, Germany
    FEBS Lett 586:3336-40. 2012
    ..Although proven with some examples, the impact of the ribosomal speed on the folding and solubility on a global, cell-wide level remains elusive...
  26. ncbi Sequence-based prediction of protein solubility
    Federico Agostini
    Centre for Genomic Regulation CRG and Universitat Pompeu Fabra UPF, Dr Aiguader, 88, Barcelona 08003, Spain
    J Mol Biol 421:237-41. 2012
    ..to investigate the relationship between the thermodynamics and kinetics of protein aggregation, we compared the solubility of proteins with their aggregation rates...
  27. pmc Secreted Wingless-interacting molecule (Swim) promotes long-range signaling by maintaining Wingless solubility
    Kimberly A Mulligan
    The Howard Hughes Medical Institute, Stanford University School of Medicine, Stanford, CA 94305, USA
    Proc Natl Acad Sci U S A 109:370-7. 2012
    ..In quantitative signaling assays, Swim is sufficient to maintain the solubility and activity of purified Wg...
  28. ncbi Accounting for the solubility-permeability interplay in oral formulation development for poor water solubility drugs: the effect of PEG-400 on carbamazepine absorption
    Avital Beig
    Department of Clinical Pharmacology, School of Pharmacy, Faculty of Health Sciences, Ben Gurion University of the Negev, Beer Sheva, Israel
    Eur J Pharm Biopharm 81:386-91. 2012
    The purpose of this paper was to study the solubility-permeability interplay in formulation development for oral administration of poor aqueous solubility drugs...
  29. ncbi Amyloid-like properties of bacterial inclusion bodies
    Mar Carrió
    Institut de Biotecnologia i de Biomedicina, Universitat Autonoma de Barcelona, 08193 Bellaterra Barcelona, Spain
    J Mol Biol 347:1025-37. 2005
    ....
  30. ncbi His tag effect on solubility of human proteins produced in Escherichia coli: a comparison between four expression vectors
    Esmeralda A Woestenenk
    Department of Biotechnology, Royal Institute of Technology KTH, AlbaNova University Center, Stockholm, Sweden
    J Struct Funct Genomics 5:217-29. 2004
    ..We looked at a total recombinant protein production levels per gram dry cell weight, solubility of the target proteins, and yield of soluble and total protein when purified by immobilized metal ion affinity ..
  31. ncbi Nanosizing: a formulation approach for poorly-water-soluble compounds
    Elaine Merisko-Liversidge
    Elan Drug Delivery, 3500 Horizon Dr, King of Prussia, PA 19406, USA
    Eur J Pharm Sci 18:113-20. 2003
    ..The technology has been successfully incorporated into all phases of the drug development cycle from identification of new chemical entities to refurbishing marketed products for improving their performance and value...
  32. ncbi MTA solubility: a long term study
    Marcela Fridland
    J Endod 31:376-9. 2005
    ..the amount of soluble material released by Mineral Trioxide Aggregate to a water medium, to determine if the solubility differences between specimens of various water/powder ratio, as demonstrated in a previous study, would be ..
  33. pmc Enhanced bioavailability of sirolimus via preparation of solid dispersion nanoparticles using a supercritical antisolvent process
    Min Soo Kim
    College of Pharmacy, Chungnam National University, Daejeon, Republic of Korea
    Int J Nanomedicine 6:2997-3009. 2011
    ..The aim of this study was to improve the physicochemical properties and bioavailability of poorly water-soluble sirolimus via preparation of a solid dispersion of nanoparticles using a supercritical antisolvent (SAS) process...
  34. pmc A high-throughput method for membrane protein solubility screening: the ultracentrifugation dispersity sedimentation assay
    Daniel A P Gutmann
    Membrane Protein Crystallography Group, Division of Molecular Biosciences, Imperial College London, UK
    Protein Sci 16:1422-8. 2007
    ..The implications of our results for membrane protein crystallization prescreening are discussed...
  35. ncbi In vivo and in vitro protein solubility assays using split GFP
    Stephanie Cabantous
    Bioscience Division, MS M888, Los Alamos National Laboratory, P O Box 1663, Los Alamos, New Mexico 87545, USA
    Nat Methods 3:845-54. 2006
    The rapid assessment of protein solubility is essential for evaluating expressed proteins and protein variants for use as reagents for downstream studies...
  36. ncbi Solubility and stability of cytochrome c in hydrated ionic liquids: effect of oxo acid residues and kosmotropicity
    Kyoko Fujita
    Department of Biotechnology, Tokyo University of Agriculture and Technology, Koganei, Tokyo, Japan
    Biomacromolecules 8:2080-6. 2007
    ..Some hydrated ILs show excellent solubilizing ability for proteins, keeping the basic properties of ILs. The solubility of cytochrome c (cyt c) depended on the structure of the component ions...
  37. ncbi Interleukin-6 triggers the association of its receptor with a possible signal transducer, gp130
    T Taga
    Division of Immunology, Osaka University, Japan
    Cell 58:573-81. 1989
    ..These findings indicate that the complex of IL-6 and IL-6-R can interact with a non-ligand-binding membrane glycoprotein, gp130, extracellularly and can provide the IL-6 signal...
  38. ncbi Improved solubility of TEV protease by directed evolution
    Susanne van den Berg
    Department of Medical Biochemistry and Biophysics, Karolinska Institute, SE 171 77 Stockholm, Sweden
    J Biotechnol 121:291-8. 2006
    ..However, the production of TEV protease in E. coli is hampered by low solubility. We have subjected the gene encoding TEV protease to directed evolution to improve the yield of soluble protein...
  39. ncbi Bacterial inclusion bodies of Alzheimer's disease β-amyloid peptides can be employed to study native-like aggregation intermediate states
    Muralidhar Dasari
    Leibniz Institut fur Molekulare Pharmakologie, Robert Rossle Strasse 10, 13125 BerlinBuch, Germany
    Chembiochem 12:407-23. 2011
    ....
  40. pmc Synthesis and characterization of conformationally preorganized, (R)-diethylene glycol-containing γ-peptide nucleic acids with superior hybridization properties and water solubility
    Bichismita Sahu
    Department of Chemistry and Center for Nucleic Acids Science and Technology CNAST, Carnegie Mellon University, Pittsburgh, Pennsylvania 15213, United States
    J Org Chem 76:5614-27. 2011
    ..and nucleases; however, the main drawbacks, as compared to other classes of oligonucleotides, are water solubility and biocompatibility...
  41. pmc Proteomic analysis of age-dependent changes in protein solubility identifies genes that modulate lifespan
    Pedro Reis-Rodrigues
    The Interdisciplinary Research Consortium on Geroscience, The Buck Institute for Research on Aging, Novato, CA 94949, USA
    Aging Cell 11:120-7. 2012
    ..This demonstrates that proteomic approaches can be used to identify genes that modify lifespan. Finally, these observations indicate that the accumulation of insoluble proteins with diverse functions may be a general feature of aging...
  42. ncbi Protection from Fas-mediated apoptosis by a soluble form of the Fas molecule
    J Cheng
    University of Alabama at Birmingham
    Science 263:1759-62. 1994
    ..Levels of soluble Fas were elevated in patients with systemic lupus erythematosus, and mice injected with soluble Fas displayed autoimmune features...
  43. pmc Role of mutant SOD1 disulfide oxidation and aggregation in the pathogenesis of familial ALS
    Celeste M Karch
    Department of Neuroscience, McKnight Brain Institute, University of Florida, Gainesville, FL 32610 0235, USA
    Proc Natl Acad Sci U S A 106:7774-9. 2009
    ..Within the final stages of disease, abnormalities in the oxidation of a normal intramolecular disulfide bond in mutant SOD1 facilitate the aggregation of mutant protein...
  44. ncbi Cytotrophoblasts up-regulate soluble fms-like tyrosine kinase-1 expression under reduced oxygen: an implication for the placental vascular development and the pathophysiology of preeclampsia
    Takeshi Nagamatsu
    Department of Obstetrics and Gynecology, Faculty of Medicine, University of Tokyo, 7 3 1 Hongo, Bunkyo ku, Tokyo 113 8655, Japan
    Endocrinology 145:4838-45. 2004
    ..The presented findings might provide a framework with which to understand the mechanism of uterine vascular remodeling and its perturbations as exemplified in preeclampsia...
  45. ncbi Structure and design of polymeric surfactant-based drug delivery systems
    V P Torchilin
    Department of Pharmaceutical Sciences, Bouve College of Health Sciences, Northeastern University, 360 Huntington Avenue, Boston, MA 02129, USA
    J Control Release 73:137-72. 2001
    ..Their in vitro and in vivo properties are discussed and the results of the initial animal experiments are presented...
  46. ncbi Modeling and comparison of dissolution profiles
    P Costa
    Serviço de Tecnologia Farmacêutica, Faculdade de Farmácia da Universidade do Porto Rua Aníbal Cunha, 164, 4050 047, Porto, Portugal
    Eur J Pharm Sci 13:123-33. 2001
    ....
  47. ncbi Changes in the surface of four calcium silicate-containing endodontic materials and an epoxy resin-based sealer after a solubility test
    R P Borges
    Department of Endodontics, University of Ribeirao Preto, Ribeirao Preto, Sao Paulo, Brazil
    Int Endod J 45:419-28. 2012
    ..in the surface structure and elemental distribution, as well as the percentage of ion release, of four calcium silicate-containing endodontic materials with a well-established epoxy resin-based sealer, submitted to a solubility test.
  48. ncbi The impact of aqueous solubility and dose on the pharmacokinetic profiles of resveratrol
    Surajit Das
    Department of Pharmacy, Faculty of Science, National University of Singapore, Building S4, Rm 05 02, 18 Science Drive 4, Singapore 117543, Singapore
    Pharm Res 25:2593-600. 2008
    This study aimed at the investigation of the impact of aqueous solubility and dose manipulation on the pharmacokinetics of resveratrol.
  49. ncbi Development and bioavailability assessment of ramipril nanoemulsion formulation
    Sheikh Shafiq
    Department of Pharmaceutics, Jamia Hamdard, Hamdard Nagar, India
    Eur J Pharm Biopharm 66:227-43. 2007
    ..and dilutable nanoemulsion formulation of Ramipril, with minimum surfactant concentration that could improve its solubility, stability and oral bioavailability...
  50. ncbi Predicting protein solubility by the general form of Chou's pseudo amino acid composition: approached from chaos game representation and fractal dimension
    Xiao hui Niu
    College of Science, Huazhong, Agricultural University, Wuhan, P R of China
    Protein Pept Lett 19:940-8. 2012
    ..protein sequence into a high-dimensional vector by CGR algorithm and fractal dimension, and then predict protein solubility by these fractal features together with Chou's pseudo amino acid composition features and support vector machine ..
  51. ncbi Process optimization, characterization and evaluation in vivo of oxymatrine-phospholipid complex
    Peng Fei Yue
    Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China
    Int J Pharm 387:139-46. 2010
    ..05), compared with those of oxymatrine or the physical mixture. This was mainly due to an improvement of the solubility of OMT-PLC.
  52. ncbi Matched molecular pairs as a guide in the optimization of pharmaceutical properties; a study of aqueous solubility, plasma protein binding and oral exposure
    Andrew G Leach
    AstraZeneca Pharmaceuticals, Mereside, Alderley Park, Macclesfield SK10 4TG, UK
    J Med Chem 49:6672-82. 2006
    ..In this paper, we focus upon the effects on aqueous solubility, plasma protein binding and oral exposure of adding substituents to aromatic rings and methylating heteroatoms.
  53. pmc Prediction of solubility and permeability class membership: provisional BCS classification of the world's top oral drugs
    Arik Dahan
    University of Michigan College of Pharmacy, 428 Church Street, Ann Arbor, MI 48109 1065, USA
    AAPS J 11:740-6. 2009
    ..System (BCS) categorizes drugs into one of four biopharmaceutical classes according to their water solubility and membrane permeability characteristics and broadly allows the prediction of the rate-limiting step in the ..
  54. ncbi Formulation design and photochemical studies on nanocrystal solid dispersion of curcumin with improved oral bioavailability
    Satomi Onoue
    Department of Pharmacokinetics and Pharmacodynamics, Global Center of Excellence Program, School of Pharmaceutical Sciences, University of Shizuoka, 52 1 Yada, Suruga ku, Shizuoka 422 8526, Japan
    J Pharm Sci 99:1871-81. 2010
    ..a wide variety of disorders, however, the therapeutic potential of curcumin could often be limited by its poor solubility, bioavailability, and photostability...
  55. ncbi Salt formation to improve drug solubility
    Abu T M Serajuddin
    Science, Technology and Outsourcing Section, Novartis Pharmaceuticals Corporation, One Health Plaza, East Hanover, NJ 07936, USA
    Adv Drug Deliv Rev 59:603-16. 2007
    Salt formation is the most common and effective method of increasing solubility and dissolution rates of acidic and basic drugs...
  56. ncbi Prediction of protein solubility in Escherichia coli using logistic regression
    Armando A Diaz
    University of Oklahoma, Norman, 73019, USA
    Biotechnol Bioeng 105:374-83. 2010
    In this article we present a new and more accurate model for the prediction of the solubility of proteins overexpressed in the bacterium Escherichia coli. The model uses the statistical technique of logistic regression...
  57. ncbi Oral bioavailability enhancement of acyclovir by self-microemulsifying drug delivery systems (SMEDDS)
    Deepa Patel
    TIFAC CORE IN NDDS, Pharmacy Department, Faculty of Technology and Engineering, The Maharaja Sayajirao University of Baroda, Vadodara, India
    Drug Dev Ind Pharm 33:1318-26. 2007
    ..b>Solubility of acyclovir was determined in various vehicles...
  58. ncbi Cyclodextrins in drug delivery
    Thorsteinn Loftsson
    University of Iceland, Faculty of Pharmacy, Hagi, Reykjavik
    Expert Opin Drug Deliv 2:335-51. 2005
    ..In the pharmaceutical industry cyclodextrins have mainly been used as complexing agents to increase aqueous solubility of poorly soluble drugs, and to increase their bioavailability and stability...
  59. pmc Comparison of SUMO fusion technology with traditional gene fusion systems: enhanced expression and solubility with SUMO
    Jeffrey G Marblestone
    LifeSensors Inc, 271 Great Valley Parkway, Malvern, PA 19355, USA
    Protein Sci 15:182-9. 2006
    ..These constructs were expressed in E. coli and evaluated for expression and solubility. As expected, the fusion tags varied in their ability to produce tractable quantities of soluble eGFP, MMP13, ..
  60. pmc Deep architectures and deep learning in chemoinformatics: the prediction of aqueous solubility for drug-like molecules
    Alessandro Lusci
    School of Computer Science and Informatics, University College Dublin, Belfield, Dublin 4, Ireland
    J Chem Inf Model 53:1563-75. 2013
    ..Several variants of this approach are applied to the problem of predicting aqueous solubility and tested on four benchmark data sets...
  61. ncbi Physicochemical properties and oral bioavailability of amorphous atorvastatin hemi-calcium using spray-drying and SAS process
    Jeong Soo Kim
    National Research Laboratory of Pharmaceutical Technology, College of Pharmacy, Chungnam National University, 220 Gung Dong, Yuseong Gu, Daejeon 305 764, Republic of Korea
    Int J Pharm 359:211-9. 2008
    ..and a tetrahydrofuran solution, respectively and appeared to be associated with better performance in apparent solubility, dissolution and pharmacokinetic studies, compared with unprocessed crystalline atorvastatin...
  62. ncbi Trimethyl chitosan and its applications in drug delivery
    V K Mourya
    Government College of Pharmacy, Vedant Hotel Road, Usmanpura, Aurangabad, India
    J Mater Sci Mater Med 20:1057-79. 2009
    ..Recommendations about uses of this polymer although could not be always realized due to limited solubility. Chitosan, for example, has been extensively evaluated for its mucoadhesive and absorption enhancement ..
  63. ncbi Role of a novel pyridostigmine bromide-phospholipid nanocomplex in improving oral bioavailability
    Qun You Tan
    Department of Thoracic Surgery, Institute of Surgery Research, Daping Hospital, Third Military Medical University, Chongqing 400042, China
    Arch Pharm Res 35:499-508. 2012
    ..21 μg·min/mL vs 1772.36 μg·min/mL, respectively. In conclusion, compared with free PB, PBPLC remarkably improves the oral bioavailability of PB, which is likely due to its higher lipophilicity and permeability...
  64. pmc Comprehensive profiling of cartilage extracellular matrix formation and maturation using sequential extraction and label-free quantitative proteomics
    Richard Wilson
    Murdoch Childrens Research Institute, Royal Children s Hospital, Parkville, Melbourne, Victoria 3052, Australia
    Mol Cell Proteomics 9:1296-313. 2010
    ..Differential analysis of the tissue proteome of 3-week neocartilage and 3-day postnatal mouse cartilage using solubility-based protein fractionation targeted components involved in neocartilage development, including ECM maturation...
  65. ncbi Nanocrystals: industrially feasible multifunctional formulation technology for poorly soluble actives
    Ranjita Shegokar
    Freie Universitat Berlin, Institute of Pharmacy, Pharmaceutical Technology, Department of Pharmaceutics, Biopharmaceutics and NutriCosmetics, Berlin, Germany
    Int J Pharm 399:129-39. 2010
    Poor solubility of new drugs and their related low oral bioavailability and general delivery problems are becoming a major challenge...
  66. pmc Disordered IL-33/ST2 activation in decidualizing stromal cells prolongs uterine receptivity in women with recurrent pregnancy loss
    Madhuri S Salker
    Division of Reproductive Health, Warwick Medical School, Clinical Sciences Research Laboratories, University Hospital, Coventry, United Kingdom
    PLoS ONE 7:e52252. 2012
    ..Failure to constrain this response predisposes to miscarriage by allowing out-of-phase implantation in an unsupportive uterine environment...
  67. pmc Cytosolic adenylyl cyclase defines a unique signaling molecule in mammals
    J Buck
    Department of Pharmacology, Joan and Sanford I Weill Medical College of Cornell University, 1300 York Avenue, New York, NY 10021, USA
    Proc Natl Acad Sci U S A 96:79-84. 1999
    ..The two presumptive catalytic domains of sAC are closely related to cyanobacterial adenylyl cyclases, providing an evolutionary link between bacterial and mammalian signaling molecules...
  68. pmc Chitosan modification and pharmaceutical/biomedical applications
    Jiali Zhang
    State Key Laboratory of Food Science and Technology, Jiangnan University, Wuxi, 214122, Jiangsu, China
    Mar Drugs 8:1962-87. 2010
    ..Our recent efforts focused on the chemical and biological modification of chitosan in order to increase its solubility in aqueous solutions and absorbability in the in vivo system, thus for a better use of chitosan...
  69. ncbi Strategies to address low drug solubility in discovery and development
    Hywel D Williams
    Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia
    Pharmacol Rev 65:315-499. 2013
    Drugs with low water solubility are predisposed to low and variable oral bioavailability and, therefore, to variability in clinical response...
  70. pmc The ability to enhance the solubility of its fusion partners is an intrinsic property of maltose-binding protein but their folding is either spontaneous or chaperone-mediated
    Sreejith Raran-Kurussi
    Protein Engineering Section, Macromolecular Crystallography Laboratory, Center for Cancer Research, Frederick National Laboratory for Cancer Research, Frederick, Maryland, United States of America
    PLoS ONE 7:e49589. 2012
    Escherichia coli maltose binding protein (MBP) is commonly used to promote the solubility of its fusion partners...
  71. ncbi PROSO II--a new method for protein solubility prediction
    Pawel Smialowski
    Department of Genome Oriented Bioinformatics, Technische Universitat Muenchen, Freising, Germany
    FEBS J 279:2192-200. 2012
    ..The solubility of proteins upon expression is dependent on their amino acid sequence...
  72. ncbi Diminished parkin solubility and co-localization with intraneuronal amyloid-β are associated with autophagic defects in Alzheimer's disease
    Irina Lonskaya
    Department of Neuroscience, Laboratory for Dementia and Parkinsonism, Georgetown University Medical Center, Washington, DC 20057, USA
    J Alzheimers Dis 33:231-47. 2013
    ..We detected decreased parkin solubility in AD cortex and parkin co-localization with intraneuronal Aβ(1-42) in the hippocampus and cortex of AD ..
  73. ncbi The solubility-permeability interplay: mechanistic modeling and predictive application of the impact of micellar solubilization on intestinal permeation
    Jonathan M Miller
    Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064, United States
    Mol Pharm 8:1848-56. 2011
    Surfactants are routinely employed to increase the apparent aqueous solubility of poorly soluble drugs...
  74. pmc Polymeric nanoparticles for increased oral bioavailability and rapid absorption using celecoxib as a model of a low-solubility, high-permeability drug
    Michael Morgen
    Bend Research Inc, 64550 Research Road, Bend, Oregon 97701, USA
    Pharm Res 29:427-40. 2012
    To demonstrate drug/polymer nanoparticles can increase the rate and extent of oral absorption of a low-solubility, high-permeability drug.
  75. ncbi Enhancing the solubility of recombinant proteins in Escherichia coli by using hexahistidine-tagged maltose-binding protein as a fusion partner
    Ping Sun
    Macromolecular Crystallography Laboratory, Center for Cancer Research, National Cancer Institute at Frederick, Frederick, MD, USA
    Methods Mol Biol 705:259-74. 2011
    ..one of the most effective solubilizing agents, having frequently been observed to improve the yield, enhance the solubility, and promote the proper folding of its fusion partners...
  76. ncbi Formulation design for poorly water-soluble drugs based on biopharmaceutics classification system: basic approaches and practical applications
    Yohei Kawabata
    Department of Pharmacokinetics and Pharmacodynamics and Global Center of Excellence COE Program, School of Pharmaceutical Sciences, University of Shizuoka, 52 1 Yada, Suruga ku, Shizuoka 422 8526, Japan
    Int J Pharm 420:1-10. 2011
    The poor oral bioavailability arising from poor aqueous solubility should make drug research and development more difficult...
  77. pmc A single immunization with soluble recombinant trimeric hemagglutinin protects chickens against highly pathogenic avian influenza virus H5N1
    Lisette A H M Cornelissen
    Central Veterinary Institute of Wageningen University, Lelystad, The Netherlands
    PLoS ONE 5:e10645. 2010
    ..Effective vaccination against HPAI H5N1 would protect commercial poultry and would thus provide an important control measure by reducing the likelihood of bird-to-bird and bird-to-human transmission...
  78. pmc Sweeping away protein aggregation with entropic bristles: intrinsically disordered protein fusions enhance soluble expression
    Aaron A Santner
    Molecular Kinetics Inc, Indianapolis, Indiana 46268, United States
    Biochemistry 51:7250-62. 2012
    ..This work thus illustrates the successful de novo design of intrinsically disordered fusions and presents a promising technology and complementary resource for researchers attempting to solubilize recalcitrant proteins...
  79. ncbi Drug nanocrystals of poorly soluble drugs produced by high pressure homogenisation
    Cornelia M Keck
    PharmaSol GmbH, Berlin, Germany
    Eur J Pharm Biopharm 62:3-16. 2006
    For many new chemical entities (NCE) of very low solubility oral bioavailability enhancement by micronisation is not sufficient, the next step taken was nanonisation...
  80. ncbi Refolding solubilized inclusion body proteins
    Richard R Burgess
    McArdle Laboratory for Cancer Research, University of Wisconsin Madison, Madison, Wisconsin, USA
    Methods Enzymol 463:259-82. 2009
    ..This chapter describes the main techniques and strategies for achieving successful refolding...
  81. ncbi ESPRIT: an automated, library-based method for mapping and soluble expression of protein domains from challenging targets
    Hayretin Yumerefendi
    Unit of Virus Host Cell Interactions, UJF EMBL CNRS, UMI 3265, 6 rue Jules Horowitz, Grenoble Cedex 9, France
    J Struct Biol 172:66-74. 2010
    ..In order to improve yield, solubility or crystallisability of a protein, it is common to subclone shorter genetic constructs corresponding to single- ..
  82. pmc Inhibition of vascular endothelial cell growth factor activity by an endogenously encoded soluble receptor
    R L Kendall
    Department of Biochemistry, Merck Research Laboratories, Rahway, NJ 07065
    Proc Natl Acad Sci U S A 90:10705-9. 1993
    ....
  83. ncbi Solubilization of poorly water-soluble drugs by mixed micelles based on hydrogenated phosphatidylcholine
    Christopher Rupp
    Department of Pharmaceutics and Biopharmaceutics, Christian Albrecht University Kiel, Gutenbergstrasse 76, 24118 Kiel, Germany
    Int J Pharm 395:272-80. 2010
    ..ingredients is rejected in early phase development and will never find a way to a patient because of poor water solubility which is often paired with poor bioavailability...
  84. ncbi Enhancement of oral bioavailability of atorvastatin calcium by self-emulsifying drug delivery systems (SEDDS)
    Pawan J Kadu
    R C Patel Institute of Pharmaceutical Education and Research, Shirpur, Dhule, Maharashtra, India
    Pharm Dev Technol 16:65-74. 2011
    ..The solubility of atorvastatin calcium was determined in various vehicles such as Captex 355, Captex 355 EP/NF, Ethyl oleate, ..
  85. pmc Immunostimulatory cellular responses of cured Leishmania-infected patients and hamsters against the integral membrane proteins and non-membranous soluble proteins of a recent clinical isolate of Leishmania donovani
    R Garg
    Division of Parasitology, Central Drug Research Institute, Lucknow, India
    Clin Exp Immunol 140:149-56. 2005
    ..These results suggest that protective, immunostimulatory molecules are present in the IMP and NSP fractions, which may be exploited for development of a subunit vaccine for VL...
  86. pmc Chaperone-fusion expression plasmid vectors for improved solubility of recombinant proteins in Escherichia coli
    Christos A Kyratsous
    Department of Pharmaceutical Sciences, Aristotle University of Thessaloniki, Thessaloniki, 54124, Greece
    Gene 440:9-15. 2009
    ..have been developed that employ simultaneous over-expression of chaperone proteins to aid proper folding and solubility during bacterial expression...
  87. pmc New method for delivering a hydrophobic drug for photodynamic therapy using pure nanocrystal form of the drug
    Koichi Baba
    Institute for Lasers, Photonics and Biophotonics, SUNY at Buffalo, Buffalo, NY 14260, USA
    Mol Pharm 4:289-97. 2007
    ..Under similar treatment conditions, the HPPH in nanocrystal form or in 1% Tween-80/water formulation showed comparable in vitro and in vivo efficacy...
  88. ncbi Preparation and evaluation of lectin-conjugated PLGA nanoparticles for oral delivery of thymopentin
    Yashu Yin
    Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, Liaoning, 110016, China
    J Control Release 116:337-45. 2006
    ..These results confirmed that the conjugation of WGA onto PLGA nanoparticles effectively improved the intestinal absorption of TP5 due to specific bioadhesion on GI cell membrane...
  89. pmc A cluster of ring stage-specific genes linked to a locus implicated in cytoadherence in Plasmodium falciparum codes for PEXEL-negative and PEXEL-positive proteins exported into the host cell
    Tobias Spielmann
    Infectious Diseases and Immunology Division, Queensland Institute of Medical Research, PO Royal Brisbane Hospital, Herston QLD 4029, Australia
    Mol Biol Cell 17:3613-24. 2006
    ..Biochemical and photobleaching studies using these proteins reveal new properties of the parasite-induced membrane compartments in the host cell. This has important implications for the biogenesis and connectivity of these structures...
  90. ncbi Lipid-based delivery systems for improving the bioavailability and lymphatic transport of a poorly water-soluble LTB4 inhibitor
    D J Hauss
    Department of Drug Metabolism and Pharmacokinetics, Boehringer Ingelheim Pharmaceuticals, Inc, Ridgefield, Connecticut 06877 0368, USA
    J Pharm Sci 87:164-9. 1998
    ..improvement in bioavailability, which may be due to the elimination or reduction of the barriers of poor aqueous solubility and slow dissolution to absorption of ontazolast from the gastrointestinal tract, or the effects of lipid on the ..
  91. ncbi Deciphering the role of the thermodynamic and kinetic stabilities of SH3 domains on their aggregation inside bacteria
    Virginia Castillo
    Institut de Biotecnologia i de Biomedicina and Departament de Bioquimica i Biologia Molecular, Universitat Autonoma de Barcelona, Bellaterra Barcelona, Spain
    Proteomics 10:4172-85. 2010
    ..These results have implications regarding the evolution of proteins...
  92. ncbi Enhanced oral bioavailability of a poorly water soluble drug PNU-91325 by supersaturatable formulations
    Ping Gao
    Worldwide Pharmaceutical Sciences, Pfizer Inc, Kalamazoo, Michigan 49007, USA
    Drug Dev Ind Pharm 30:221-9. 2004
    ....
  93. ncbi Oral formulation strategies to improve solubility of poorly water-soluble drugs
    Abhishek Singh
    Laboratory of Pharmacotechnology and Biopharmacy, Katholieke Universiteit Leuven, B 3000 Leuven, Belgium
    Expert Opin Drug Deliv 8:1361-78. 2011
    ..these advances have been accompanied by an increase in the structural complexity and a decrease in the solubility of the active pharmaceutical ingredient...
  94. ncbi The Sushi domain of soluble IL-15 receptor alpha is essential for binding IL-15 and inhibiting inflammatory and allogenic responses in vitro and in vivo
    M Orchardson
    Department of Immunology and Bacteriology and Center of Rheumatic Disease, University of Glasgow, Glasgow, United Kingdom
    J Immunol 167:277-82. 2001
    ..Thus, the Sushi domain is critical for the functional activity of sIL-15Ralpha...
  95. ncbi Modulatory effects of sCD14 and LBP on LPS-host cell interactions
    Richard L Kitchens
    Division of Infectious Diseases, Department of Internal Medicine, University of Texas Southwestern Medical Center, Dallas, Texas 75390 9113, USA
    J Endotoxin Res 11:225-9. 2005
    ....
  96. ncbi Sterically stabilized phospholipid mixed micelles: in vitro evaluation as a novel carrier for water-insoluble drugs
    Aparna Krishnadas
    Department of Biopharmaceutical Sciences, University of Illinois at Chicago, Chicago, Illinois 60612, USA
    Pharm Res 20:297-302. 2003
    ....
  97. pmc Colloid formation by drugs in simulated intestinal fluid
    Allison K Doak
    Department of Pharmaceutical Chemistry, University of California San Francisco, San Francisco, California 94158 2550, USA
    J Med Chem 53:4259-65. 2010
    ..Six formed colloids at concentrations equal to or lower than the concentrations reached in the gut, suggesting that aggregation may have an effect on the absorption and distribution of these drugs, and potentially others, in vivo...
  98. ncbi alpha2-Macroglobulin and haptoglobin suppress amyloid formation by interacting with prefibrillar protein species
    Justin J Yerbury
    School of Biological Sciences, University of Wollongong, Northfields Avenue, Wollongong, New South Wales 2522, Australia
    J Biol Chem 284:4246-54. 2009
    ..We also provide evidence that both alpha(2)M and Hp interact with prefibrillar species to maintain the solubility of amyloidogenic proteins...
  99. ncbi Thioredoxin reduction alters the solubility of proteins of wheat starchy endosperm: an early event in cereal germination
    Joshua H Wong
    Department of Plant and Microbial Biology, 111 Koshland Hall, University of California, Berkeley, CA 94720, USA
    Plant Cell Physiol 45:407-15. 2004
    ..in addition to modifying activity and increasing protease sensitivity, reduction by thioredoxin alters protein solubility, thereby promoting processes of the grain starchy endosperm, notably the mobilization of reserves during ..
  100. ncbi Suppression of protein interactions by arginine: a proposed mechanism of the arginine effects
    Tsutomu Arakawa
    Alliance Protein Laboratories, Thousand Oaks, CA 91360, United States
    Biophys Chem 127:1-8. 2007
    ..The effects of weakly interacting additives, such as arginine, on protein solubility, stability and aggregation have been explained from three different approaches: i.e...
  101. ncbi Protein solubility: sequence based prediction and experimental verification
    Pawel Smialowski
    Department of Genome Oriented Bioinformatics, Technische Universitat Munchen, Wissenschaftszentrum Weihenstephan, 85350 Freising, Germany
    Bioinformatics 23:2536-42. 2007
    ..b>Solubility is an individual trait of proteins which, under a given set of experimental conditions, is determined by their ..

Research Grants80

  1. Therapeutic Effect of a Novel Antioxidant on Degenerative Eye Disorders
    Nuran Ercal; Fiscal Year: 2012
    ..In the lens, the result is a progressive reduction in solubility of crystalline proteins that manifests in an opacification of te lens...
  2. Detection of engineered nanomaterials in drinking water, food, commercial product
    Paul K Westerhoff; Fiscal Year: 2010
    ..will be handled in a similar fashion as organic chemicals, by pre-treating and analyzing (LC/MS) them based upon solubility and hydrophobicity characteristics...
  3. Novel Therapeutics for Neurotropic Alphaviruses
    David J Miller; Fiscal Year: 2013
    ..based on the initial structure-activity relationship analysis, to enhance potency, reduce toxicity, improve solubility and metabolic stability, and optimize membrane permeability;(2) identify molecular target(s) responsible for ..
  4. Evaluation of a new class of antimicrobial agents against Clostridium difficile
    SAUL R contact TZIPORI; Fiscal Year: 2011
    ..difficile, with a view to, a) increase solubility and MIC in vitro potency (≤0...
  5. CHEMISTRY SUPPORT SERVICES TO THE ENVIRONMENTAL TOXICOLOGY PROGRAM
    CLARK ALGAIER; Fiscal Year: 2009
    ..During the Fiscal Year hundreds of chemicals were tested for solubility, prepared 10/20mM solutions and shipped to different labs for high through-put screening experiments...
  6. Transscleral Transport & Polymeric Delivery of Antibody & Steroids for Macular Ed
    Ashim K Mitra; Fiscal Year: 2010
    ..Risk of drug precipitation due to poor solubility;and short vitreal half life upon intravitreal injection are the key deterrents in their delivery...
  7. Ionic Liquid Gas Sensors for Detection of Flammable Gases In Workplace
    Xiangqun Zeng; Fiscal Year: 2010
    ..Literature study shows that gases (i.e.CH4, C2H4, C2H6, CO2, O2) have widely varying gas solubility in ILs...
  8. Development of Transdermal Films for the the Delivery of HIV Therapeutics
    Anthony Sang Won Ham; Fiscal Year: 2010
    ..Due to low solubility and poor penetration through the mucosa to the target site of action, pyrimidinediones face significant ..
  9. Rigid-rod Peptides as Nanocarriers for Delivery of Cancer Drugs
    Katarzyna Slowinska; Fiscal Year: 2013
    ..Unfortunately, the currently used formulations which are intended to increase the solubility and thus bioavailability of PTX, are linked to adverse allergic reactions...
  10. Rational Development of Anti-Trypanosoma Cruzi Drugs
    Michael H Gelb; Fiscal Year: 2013
    ..cruzi amastigotes, and for cytotoxicity against mammalian cells. Follow up studies will test aqueous solubility, stability in liver microsomes, and inhibition of human CYP450 enzymes...
  11. Development and testing of polyvalent anthrax toxin inhibitors
    JEREMY S MOGRIDGE; Fiscal Year: 2012
    ..The second aim of this proposal is to perform preformulation studies to optimize inhibitor solubility and stability...
  12. Anti-Fibrotic Therapy for Scleroderma/SSc
    Latha Paka; Fiscal Year: 2013
    ..a small molecule receptor tyrosine kinase inhibitor/s with activity against both PDGFR and KDR and optimized for solubility in Phase I program...
  13. Adiponetin and AMPK Biosensor
    John Y J Shyy; Fiscal Year: 2010
    ..of 2 amino acids resulted in high expression by both bacterial- and mammalian cell-based systems and high solubility in saline...
  14. Pre-clinical testing of necrostatin as a potential small molecule for the treatme
    SERGE E PRZEDBORSKI; Fiscal Year: 2012
    ..steps toward testing this possibility, SA-2 will assess Nec-1 and its inactive structural analogue Nec-1ia solubility and stability in suitable vehicles for chronic in vivo use, and their central nervous system penetration, ..
  15. Surrogate endpoints for correlating protective immunity in response to influenza
    Gary Fujii; Fiscal Year: 2010
    ..The water solubility properties of the hydrophobic fusion protein allows for its isolation and purification using commercially viable ..
  16. A Diarylheptanoid Scaffold to Treat Taopathies
    Chad A Dickey; Fiscal Year: 2013
    ..eADME studies will include metabolism in mouse and human liver microsomes, human plasma protein binding, water solubility testing, broad receptor and ion channel profiling including hERG, and initial pharmacokinetic testing in rats...
  17. Phospholipid Nanocarriers Improve Chemotherapy by Targeted Drug Delivery
    Hayat Onyuksel; Fiscal Year: 2010
    ..To this end, the focus of this research project is to develop an innovative targeted nanocarrier so that drug solubility, efficacy and safety profile are significantly improved...
  18. Optimization of novel pyranopyridine efflux pump inhibitors
    Son Truong Nguyen; Fiscal Year: 2013
    ..for the key properties required for a lead compound: potency, cytotoxicity, metabolic stability, and solubility Compounds that meet the rigorous criteria specified in the milestones will be designated as lead compounds...
  19. Foundations of Pretargeted Radioimmunotherapy
    KARL D WITTRUP; Fiscal Year: 2013
    ..New data is presented that demonstrates the robust expression and solubility characteristics of the bsAbs...
  20. Novel mycobacterial translocase I inhibitors - a new class of anti-TB drugs
    Venkata M Reddy; Fiscal Year: 2010
    ..and insolubility problems by combining SQ641 with TPGS, a vitamin E analogue routinely used to improve drug solubility and hence bioavailability (EASTMAN and Company 2005)...
  21. Novel Inhibitors of Viral Replication
    Michael G Roth; Fiscal Year: 2013
    ..Aim 2. To address issues of ADME of antiviral compounds. We will test our best compound series for, solubility, cellular absorption, metabolism and cellular toxicity...
  22. Xenon MRI assessment of response to cystic fibrosis therapies
    IULIAN CONSTANTIN RUSET; Fiscal Year: 2012
    ..Hyperpolarized xenon-129 (HXe) has been perceived as less appropriate for children due to its solubility in blood and tissues, and concomitant side effects including brief euphoria, dysphoria, and/or numbness...
  23. Optimization of Protein Therapeutics Formulations
    Lawrence J Delucas; Fiscal Year: 2012
    ..The HSC technology provides a new paradigm for rapidly improving the solubility and physical stability of biopharmaceuticals...
  24. Identification of altered lipids predictive of anesthetic-induced brain injury
    Xianlin Han; Fiscal Year: 2013
    ..General anesthetics, due to their lipid solubility, readily enter the brain, dissolve into cellular membranes, penetrate organelle, disturb dynamics of neuronal ..
  25. DEVELOPING SOLUTES AS STRUCTURAL/MECHANISTIC PROBES OF PROTEIN-DNA INTERACTIONS
    M Thomas Record; Fiscal Year: 2013
    ..To interpret these data, osmometric or solubility studies of interactions of these solutes with appropriately chosen model compounds will be performed...
  26. Green Tea Nanocarriers: A Promising Approach for the Prevention and Treatment of
    Shu Wang; Fiscal Year: 2011
    ..of this line of research is to use biodegradable and biocompatible nanoparticles to increase bioavailability, solubility, stability and payload of therapeutic nutrients and natural compounds, lower their toxicity, prolong their ..
  27. Selective MRTF/SRF-Transcription Inhibitors: Novel Anti-fibrotics for IPF
    Vijaykumar M Baragi; Fiscal Year: 2013
    ..I, we will evaluate a set of 10 chemically diverse, selective and potent MRTF/SRF transcription inhibitors for solubility, metabolic stability and in vivo systemic exposure and bioavailability...
  28. Ceramic scaffolds with engineered topography and chemistry
    ISABELLE L DENRY; Fiscal Year: 2013
    ..The effect of ion-exchange on surface chemistry, solubility and bioactivity of the scaffolds will be tested in Aim 3...
  29. Preserving beta-lactam utility against pathogens producing all classes of beta-la
    LUIGI XERRI; Fiscal Year: 2012
    ..They will have high aqueous solubility (for formulating with water-soluble b-lactam antibiotics) and will rescue Azt in lethal mouse models of multi-..
  30. Optimizing selective in vivo inhibition of pancreatic tumor JAK2/STAT3 signaling
    Mitch A Phelps; Fiscal Year: 2013
    ..Pharmacokinetic (PK) studies revealed FLLL100P has superior solubility, rapid de-phosphorylation to active FLLL100, and 10-fold higher systemic exposure compared to FLLL32...
  31. Improvement of Liver Transplantation by a Sphingosine Kinase Inhibitor
    Zhi Zhong; Fiscal Year: 2010
    ..To synthesize sufficient amounts of SK inhibitor ABC294640 for in vivo studies, characterize its solubility and stability in cold storage solution and determine its penetration into liver in vivo and explants during cold ..
  32. Oral prodrug of a novel antiviral that blocks neuronal reactivation of HSV
    George E Wright; Fiscal Year: 2012
    ..to enhance its intestinal absorption;strategies include emulsions, small molecule adjuvants, and solubility enhancers;2...
  33. Therapeutic correction of deltaF508-CFTR cystic fibrosis by a novel PDZ12 drug.
    Alvin Bach; Fiscal Year: 2013
    ..Peptides wil be eliminated from further development only if they show low solubility or a half-life <30 minutes because this will lead to unacceptable bioavailability. Aim 2...
  34. Quick-Set Endodontic Material
    CAROLYN MARGARET PRIMUS; Fiscal Year: 2010
    ..and ISO 9917 standards for root canal sealers and dental cements for radiopacity, setting &working times, solubility, dimensional stability, and strength. Washout testing should determine the stability for clinical use...
  35. Catalytic Approach to Treatment of Cyanide Poisoning
    SIGRIDUR G SUMAN; Fiscal Year: 2010
    ..Thiosulfate's limited solubility in the liver leads to a slow reaction while facilitating sulfane sulfur transfer to rhodanese...
  36. Treatment of glucocorticoid-induced osteonecrosis with nano-fullerenes
    Quanjun Cui; Fiscal Year: 2013
    ..might be very effective in treatment of ONFH, and a polyhydroxylated fullerene fullerol with better solubility might elicit a greater activity than the pristine C60. The following specific aims are included: 1...
  37. Development of a Novel TGF-beta Antagonist for Treating Hepatic Fibrosis
    Jung S Huang; Fiscal Year: 2010
    ..The use of TGF-[unreadable] peptantagonist for treating HF is limited by its poor solubility in aqueous solution at neutral pH...
  38. RECEPTOR TARGETED MOLECULAR IMAGING OF MULTIPLE MYELOMA
    Monica Shokeen; Fiscal Year: 2013
    ..The goal of aim 1 is twofold: a) to optimize the first-generation agent to enhance solubility and improve pharmacokinetics;and b) to synthesize optical and scrambled analogs for in vitro and in vivo binding ..
  39. Oral paclitaxel solubilized and bioenhanced by food compound for cancer therapy
    Zhijun Liu; Fiscal Year: 2013
    ..Our recent experiments demonstrate some promise for enhancing the solubility and permeability using rubusoside (RUB), a food ingredient isolated from the Rubus plant...
  40. Chlorite dismutase: a novel heme enzyme and its implications for human health
    Jennifer L Dubois; Fiscal Year: 2013
    ..The oxochlorates are man-made biocides, bleaches, and oxidizers that, because of their extensive use, high solubility, and toxicity, are now serious contaminants of fresh water...
  41. Efficacy and Mechanisms of GLN Dipeptide in the SICU
    Thomas R Ziegler; Fiscal Year: 2012
    ..Properties of L-GLN limit provision in solution, but the GLN dipeptide alanyl-GLN (AG) confers stability and solubility in PN (AG-PN)...
  42. The Role of TDP-43 Phosphorylation in Protein Function and Neurodegeneration
    YOUHNA AYALA; Fiscal Year: 2013
    ..the novel phosphosites identified through our proposed analyses;(aim 2) determine if protein activity and solubility are affected by the patient-linked mutations that change the phosphorylation profile;and (aim 3) characterize ..
  43. Novel Thioderivatives as Neuroprotective Anticonvulsants
    DOUGLAS ERIC BRENNEMAN; Fiscal Year: 2010
    ..of promising neuroprotective, anti- seizure compounds, a limited number of tests will be conducted to assess solubility, drug permeability and potential cardiovascular liabilities (hERG channel interactions)...
  44. Targeted Polymer Micelles for Treatment of Metastatic Melanoma
    Kevin N Sill; Fiscal Year: 2013
    ..block copolymers are a particular type of nanocarrier that are attractive due to their ability to confer water solubility to hydrophobic drug by encapsulating them within the core of the micelle...
  45. MODEL SYNTHETIC CHANNEL ASSEMBLIES
    John M Tomich; Fiscal Year: 2013
    ..We hypothesized that the ideal channel-forming sequence should:1) have high aqueous solubility as a monomer;2)have no detectable antigenicity;3) bind to and then partition rapidly into biological membranes ..
  46. Production &Crystallization of Membrane Protein for 3D Structure
    Lawrence J Delucas; Fiscal Year: 2013
    ..virial coefficient data and performs in silico predictions of novel solution conditions that improve protein solubility and homogeneity...
  47. Designed Antimalarial Agents Overcoming Chloroquine-Resistance
    David H Peyton; Fiscal Year: 2010
    ..and chloroquine-resistant malaria in human red blood cells in vitro, as well as for other in vitro tests for solubility, central nervous system receptor activity, mutagenic activity, and cytotoxicity...
  48. New type of androgen receptor inhibitors for prostate cancer treatment
    Olga B Chernova; Fiscal Year: 2010
    ..properties were never optimized and are far from optimal, which includes low metabolic stability, low solubility etc. In this specific aim we will sensitize focus libraries around each of DARNAs...
  49. Co-Delivery of Antifungal Agents: Toxicity and Efficacy in Invasive Candidiasis
    Glen S Kwon; Fiscal Year: 2013
    ..of amphotericin B (AmB) with other antifungal agents via self-assembled polymers, fulfilling requirements in solubility, safety, stability, and synergy, which ca now be achieved by the coincident action of combination antifungal ..
  50. Celecoxib Derivative: Host Cell-Directed Inhibitors of Intracellular Pathogens
    Kristy M Ainslie; Fiscal Year: 2013
    ..To overcome solubility issues, we propose encapsulating AR-12 in acetalated dextran (Ac-DEX) particles that passively target the host ..
  51. NextGen Lab-on-Bead: Harnessing Ion Torrent Sequencing for Cancer Drug Discovery
    Jed C Macosko; Fiscal Year: 2013
    ..represent an attractive class of drug candidates compared to their linear counterparts in terms of potency, solubility, lipophilicity, specificity, multivalent binding, metabolic stability, bioavailability and membrane permeability...
  52. Countermeasure for Chlorine Inhalation
    SIGRIDUR G SUMAN; Fiscal Year: 2011
    ..A small dose and solubility are key to the success of an IM development effort, since a paramedic responding to an incident can rapidly ..
  53. Development of Age-Appropriate Fast Disintegrating Pediatric Granules and Tablets
    MOJI ADEYEYE; Fiscal Year: 2009
    ..These properties could affect the solubility, disintegration and dissolution of the final product...
  54. Multifunctional PEG Hydrogel Nano/Microparticles for Targeted Treatment of NSCLC
    Patrick J Sinko; Fiscal Year: 2013
    ..Using a novel fabrication process, high drug loading into NPs is achieved that overcomes the solubility limitations of hydrophobic cancer drugs...
  55. Beta Amyloid and Oxidative Stress in Alzheimer's Disease
    Linda J Van Eldik; Fiscal Year: 2012
    ..the UK AD Center, 2) a unique Beta-Amyloid Core that will provide the AB index (total AB{1-40} and AB{1-42}, AB solubility, oligomeric and fibrillar AB quantitation and plaque quantitation) from human subjects and transgenic mice and ..
  56. Crystallization of outer membrane proteins for export of polysaccharide capsule
    Mark A Saper; Fiscal Year: 2012
    ..Proteins will be screened with a variety of detergents for optimal solubility and monodispersity. Pure protein will be used to screen for crystallization conditions...
  57. Blocking a novel cytokine signaling pathway for the treatment of rheumatoid arthr
    Kirill Ostanin; Fiscal Year: 2013
    ..In Phase II our efforts will focus on optimizing hit compounds for solubility, permeability, metabolic stability, and specificity, while minimizing potential safety concerns...
  58. THE ROLE OF AQUAPORIN-0 IN LENS DEVELOPMENT AND AGING
    Kevin L Schey; Fiscal Year: 2013
    ..over many decades and, to do so, lens fiber cells must minimize extracellular space and preserve protein solubility. Lens membrane proteins, such as channels and adhesion molecules, play essential roles in lens development and ..
  59. Development of novel targeted agents in lung cancer
    Alexander B Sigalov; Fiscal Year: 2012
    ..In order to increase peptide solubility, bioavailability and targeting to TAMs, we will utilize SignaBlok's proprietary nanosystem for macrophage-..
  60. Synthesis and Characterization of Polymeric Antioxidant microparticles for the pr
    NIHAR MANILAL SHAH; Fiscal Year: 2013
    ..physiologically represents a challenge due to its short half-life in physiological environments and poor aqueous solubility. The central hypothesis of this project is that curcumin-based polymers composed of natural antioxidants (C-PoNA)..
  61. Silk Fibroin Small-Molecule Drug Carriers for the Treatment of Osteoarthritis
    TIMOTHY KARIITHI MWANGI; Fiscal Year: 2013
    ..A very low solubility and oral bioavailability for curcumin is very limiting, however, as it is difficult to achieve nanomolar ..
  62. Novel Compounds Targeting Bacterial PBPs
    LUIGI XERRI; Fiscal Year: 2013
    ..coli and K. pneumoniae). In addition, the early leads have good aqueous solubility (>1 mg/mL), low protein binding (<50% in mouse, dog, and human serum), high selectivity vs...
  63. AGE-RELATED GASTRIC CHANGES AND DRUG ABSORPTION
    Aryeh Hurwitz; Fiscal Year: 1993
    ..The solubility of both drugs is markedly reduced at pH above 5 and their absorption is depressed by achlorhydria induced by ..
  64. ORAL DRUG DELIVERY AND BIOAVAILABILITY--AIDS
    Gordon Amidon; Fiscal Year: 1993
    ..of drug absorption from the gastrointestinal tract that includes permeability, stability, enzymatic activity, solubility and dissolution rate, measure the required parameters in animal models and/or humans and compare the estimated ..
  65. Novel Use of Confocal Microscopy on Cultured Porcine Corneas for Pre-Clinical Tes
    Michelle Piehl; Fiscal Year: 2011
    ..In PorFocal, test substances are placed directly onto living corneal tissue in culture;therefore solubility of the test substance is irrelevant...
  66. Amphotericin B Analogs
    Charles Hutchinson; Fiscal Year: 2009
    ..the potency and activity spectrum of the parent drug while minimizing its nephrotoxicity and improving its water solubility for ease of formulation...
  67. ORAL CONTROLLED-RELEASE DELIVERY SYSTEMS
    H Rawls; Fiscal Year: 1991
    ..The rate of biodegradation, the diffusivity through the matrix polymer, the solubility of the agent and the loading in the reservoir determine the rate and duration of release...
  68. Novel Organophosphorous Hydrolases for Decontamination
    Andrew Mesecar; Fiscal Year: 2007
    ..Unfortunately, the enzymes currently in development lack many of the desired properties such as solution solubility, thermal and pH stability, and substrate specificity for all of the potential applications of these enzymes...
  69. AZIDE TECHNOLOGY FOR DRUG DEVELOPMENT
    Kyoichi Watanabe; Fiscal Year: 2001
    ..have shown excellent biological activity, but could not be used in clinic due to their metabolic instability or solubility problems, clinically usable agents...
  70. Utilizing Ethyl Nitrate Gas in Laparoscopic Surgery
    James Reynolds; Fiscal Year: 2006
    ..In addition, due to its plasma solubility, insufflation with CO2 will increase pCOz and decrease blood pH, actions that can produce respiratory acidosis, ..
  71. CARBONATOAPATITE FORMATION IN ENAMEL MINERALIZATION
    Takaaki Aoba; Fiscal Year: 1993
    ..The present proposal aims at: a) determining the stoichiometry and solubility product constants of the carbonatoapatite in the enamel tissue at various developmental stages; b) assessing the ..
  72. EFFECTS OF BILE ACIDS ON CALCIUM AND IRON ABSORPTION
    Edward Moore; Fiscal Year: 1990
    ..Thus, upon entry of acid gastric contents into the alkaline duodenum, the solubility of each ion is governed by the least soluble species present...
  73. PHARMACOLOGY AND EFFICACY OF NOVEL TAXOL FORMULATIONS
    ROBERT STRAUBINGER; Fiscal Year: 1999
    ..Acute toxicity arises from the low solubility of taxol in water, which necessitates administration in Cremophor EL (polyethoxylated castor oil), an excipient ..
  74. A Therapeutic Agent for Radiation-induced Lung Fibrosis
    SHUAN HUANG; Fiscal Year: 2009
    ..However, the use of TGF-( peptantagonists to treat lung fibrosis is limited by its poor solubility in aqueous solution at neutral pH...
  75. Superior Near-IR Dyes for Bioimaging
    ARUNKUMAR EASWARAN; Fiscal Year: 2009
    ..However due to their poor solubility under aqueous conditions, their usefulness in biological applications remains a challenge thus limiting their ..
  76. Inhibition of Endocannabinoid Biosynthesis via Diacylglycerol Lipase
    RICHARD DUCLOS; Fiscal Year: 2009
    ..DAGL substrate (1,2-diacyl-sn-glycerol) and the selective inhibitor tetrahydrolipstatin (THL), which has poor solubility and absorption characteristics...
  77. Retrievable Blood Oxygen Carrier System
    Agnes E Ostafin; Fiscal Year: 2012
    ..They seem to have high oxygen and carbon dioxide solubility, quickly exchange them at the tissue and lungs, and may be further coated with short chain polyethylene oxide to ..
  78. AGING AND ALZHEIMER DEMENTIA--ROLE OF FIBROUS PROTEINS
    Shu Hui Yen; Fiscal Year: 2000
    ..from normal tau in phosphate content, isoelectric charge, number of and molecular weights of isoforms and solubility. Moreover, a pool of abnormal tau protein that is not associated with PHF, but has properties similar to PHF-tau,..
  79. EFFECTS OF GENERAL ANESTHETICS ON NICOTINIC MEMBRANES
    Leonard Firestone; Fiscal Year: 1991
    The potency of most general anesthetics can be predicted by a shared physical feature, lipid solubility. This originally led to the hypothesis that anesthetics worked on the lipid membrane, and more recently has motivated investigations ..
  80. Development of Novel Therapies or Methamphetamine Abuse
    Linda Dwoskin; Fiscal Year: 2009
    ..e., it specifically decreases methamphetamine SA. The physicochemical properties of GZ-793A provides enhanced solubility and drugability relative to the majority of compounds initially proposed in the funded project...