- 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...
- 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...
- 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...
- 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...
- Enhancement of soluble protein expression through the use of fusion tags
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...
- Pharmaceutical applications of cyclodextrins: basic science and product development
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...
- Inhaled nanoparticles--a current review
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...
- 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 ..
- 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 ..
- Bimodal protein solubility distribution revealed by an aggregation analysis of the entire ensemble of Escherichia coli proteins
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...
- 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...
- 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.
- Curcumin-phospholipid complex: Preparation, therapeutic evaluation and pharmacokinetic study in rats
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...
- Soluble adenylyl cyclase as an evolutionarily conserved bicarbonate sensor
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...
- 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...
- 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...
- The in vitro stability and in vivo pharmacokinetics of curcumin prepared as an aqueous nanoparticulate formulation
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...
- A seeding reaction recapitulates intracellular formation of Sarkosyl-insoluble transactivation response element (TAR) DNA-binding protein-43 inclusions
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...
- Toward the structural genomics of complexes: crystal structure of a PE/PPE protein complex from Mycobacterium tuberculosis
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...
- Elevated placental soluble vascular endothelial growth factor receptor-1 inhibits angiogenesis in preeclampsia
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...
- 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.
- 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...
- Tagging recombinant proteins to enhance solubility and aid purification
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 ..
- 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 ..
- tRNA concentration fine tunes protein solubility
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...
- Sequence-based prediction of protein solubility
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...
- 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...
- Accounting for the solubility-permeability interplay in oral formulation development for poor water solubility drugs: the effect of PEG-400 on carbamazepine absorption
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...
- Amyloid-like properties of bacterial inclusion bodies
Institut de Biotecnologia i de Biomedicina, Universitat Autonoma de Barcelona, 08193 Bellaterra Barcelona, Spain
J Mol Biol 347:1025-37. 2005
- 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 ..
- Nanosizing: a formulation approach for poorly-water-soluble compounds
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...
- MTA solubility: a long term study
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 ..
- 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...
- 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...
- In vivo and in vitro protein solubility assays using split GFP
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...
- Solubility and stability of cytochrome c in hydrated ionic liquids: effect of oxo acid residues and kosmotropicity
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...
- Interleukin-6 triggers the association of its receptor with a possible signal transducer, gp130
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...
- 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...
- Bacterial inclusion bodies of Alzheimer's disease β-amyloid peptides can be employed to study native-like aggregation intermediate states
Leibniz Institut fur Molekulare Pharmakologie, Robert Rossle Strasse 10, 13125 BerlinBuch, Germany
Chembiochem 12:407-23. 2011
- Synthesis and characterization of conformationally preorganized, (R)-diethylene glycol-containing γ-peptide nucleic acids with superior hybridization properties and water solubility
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...
- Proteomic analysis of age-dependent changes in protein solubility identifies genes that modulate lifespan
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...
- Protection from Fas-mediated apoptosis by a soluble form of the Fas molecule
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...
- 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...
- 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
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...
- 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...
- Modeling and comparison of dissolution profiles
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
- 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.
- The impact of aqueous solubility and dose on the pharmacokinetic profiles of resveratrol
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.
- Development and bioavailability assessment of ramipril nanoemulsion formulation
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...
- 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 ..
- 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.
- 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.
- Prediction of solubility and permeability class membership: provisional BCS classification of the world's top oral drugs
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 ..
- Formulation design and photochemical studies on nanocrystal solid dispersion of curcumin with improved oral bioavailability
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...
- 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...
- 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...
- Oral bioavailability enhancement of acyclovir by self-microemulsifying drug delivery systems (SMEDDS)
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...
- Cyclodextrins in drug delivery
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...
- 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, ..
- Deep architectures and deep learning in chemoinformatics: the prediction of aqueous solubility for drug-like molecules
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...
- 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...
- 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 ..
- 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...
- Comprehensive profiling of cartilage extracellular matrix formation and maturation using sequential extraction and label-free quantitative proteomics
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...
- Nanocrystals: industrially feasible multifunctional formulation technology for poorly soluble actives
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...
- 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...
- Cytosolic adenylyl cyclase defines a unique signaling molecule in mammals
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...
- Chitosan modification and pharmaceutical/biomedical applications
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...
- 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...
- 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
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...
- PROSO II--a new method for protein solubility prediction
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...
- Diminished parkin solubility and co-localization with intraneuronal amyloid-β are associated with autophagic defects in Alzheimer's disease
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 ..
- 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...
- Polymeric nanoparticles for increased oral bioavailability and rapid absorption using celecoxib as a model of a low-solubility, high-permeability drug
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.
- Enhancing the solubility of recombinant proteins in Escherichia coli by using hexahistidine-tagged maltose-binding protein as a fusion partner
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...
- Formulation design for poorly water-soluble drugs based on biopharmaceutics classification system: basic approaches and practical applications
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...
- 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...
- 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...
- 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...
- 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...
- ESPRIT: an automated, library-based method for mapping and soluble expression of protein domains from challenging targets
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- ..
- 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
- Solubilization of poorly water-soluble drugs by mixed micelles based on hydrogenated phosphatidylcholine
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...
- 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, ..
- 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
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...
- 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...
- New method for delivering a hydrophobic drug for photodynamic therapy using pure nanocrystal form of the drug
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...
- Preparation and evaluation of lectin-conjugated PLGA nanoparticles for oral delivery of thymopentin
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...
- 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
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...
- 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 ..
- Deciphering the role of the thermodynamic and kinetic stabilities of SH3 domains on their aggregation inside bacteria
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...
- Enhanced oral bioavailability of a poorly water soluble drug PNU-91325 by supersaturatable formulations
Worldwide Pharmaceutical Sciences, Pfizer Inc, Kalamazoo, Michigan 49007, USA
Drug Dev Ind Pharm 30:221-9. 2004
- Oral formulation strategies to improve solubility of poorly water-soluble drugs
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...
- 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
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...
- 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
- Sterically stabilized phospholipid mixed micelles: in vitro evaluation as a novel carrier for water-insoluble drugs
Department of Biopharmaceutical Sciences, University of Illinois at Chicago, Chicago, Illinois 60612, USA
Pharm Res 20:297-302. 2003
- 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...
- 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...
- 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 ..
- Suppression of protein interactions by arginine: a proposed mechanism of the arginine effects
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...
- Protein solubility: sequence based prediction and experimental verification
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 ..