Genomes and Genes
Summary: Peptides composed of two amino acid units.
Publications322 found, 100 shown here
- Lactobacillus reuteri-produced cyclic dipeptides quench agr-mediated expression of toxic shock syndrome toxin-1 in staphylococciJingru Li
Department of Microbiology and Immunology, Schulich School of Medicine and Dentistry, University of Western Ontario, London, ON, Canada N6A 5C1
Proc Natl Acad Sci U S A 108:3360-5. 2011..reuteri RC-14 supernatant, and the cyclic dipeptides cyclo(L-Phe-L-Pro) and cyclo(L-Tyr-L-Pro) were identified as the signaling molecules...
- Efficacy and safety of saxagliptin in older patients with type 2 diabetes mellitusJean Doucet
Rouen University Hospital, Rouen, France
Curr Med Res Opin 27:863-9. 2011..To assess the safety and efficacy of saxagliptin (5 mg once-daily) in older patients (≥65 years of age) with inadequately controlled type 2 diabetes...
- Alanyl-glutamine hastens morphologic recovery from 5-fluorouracil-induced mucositis in miceBenedito A Carneiro-Filho
Department of Morphology, Institute of Biomedicine and Clinical Research Unit University Hospital, Federal University of Ceara, Brazil
Nutrition 20:934-41. 2004..In this study, we postulated the beneficial role of oral alanyl-glutamine, a more stable glutamine derivative to decrease 5-fluorouracil (5-FU)-induced mucositis in mice...
- Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brainH F Dovey
Elan Pharmaceuticals, Inc, South San Francisco, CA 94080, USA
J Neurochem 76:173-81. 2001..Development of such novel functional gamma-secretase inhibitors will enable a clinical examination of the A beta hypothesis that Ass peptide drives the neuropathology observed in Alzheimer's disease...
- Saxagliptin improves glycaemic control and is well tolerated in patients with type 2 diabetes mellitus and renal impairmentM Nowicki
Department of Nephrology, Hypertension and Kidney Transplantation, Medical University, Łódź, Poland
Diabetes Obes Metab 13:523-32. 2011..To evaluate the efficacy and safety of saxagliptin vs. placebo in patients with type 2 diabetes mellitus (T2DM) and renal impairment...
- Phase II trial of single agent Val-boroPro (Talabostat) inhibiting Fibroblast Activation Protein in patients with metastatic colorectal cancerKalyani Narra
Department of Medical Oncology, Fox Chase Cancer Center, Philadelphia, Pennsylvania 19111, USA
Cancer Biol Ther 6:1691-9. 2007..The clinical impact of FAP inhibition was tested using Val-boroPro (Talabostat), the first clinical inhibitor of FAP enzymatic activity, in a phase II study of patients with metastatic colorectal cancer...
- Serum metabolomics reveals γ-glutamyl dipeptides as biomarkers for discrimination among different forms of liver diseaseTomoyoshi Soga
Institute for Advanced Biosciences, Keio University, Tsuruoka 997 0052, Japan
J Hepatol 55:896-905. 2011..We applied a metabolome profiling approach to serum samples obtained from patients with different liver diseases, to discover noninvasive and reliable biomarkers for rapid-screening diagnosis of liver diseases...
- N-methyl-D-glucamine improves the laser-induced fluorescence capillary electrophoresis performance in the total plasma thiols measurementAngelo Zinellu
Chair of Clinical Biochemistry, University of Sassari, Viale San Pietro 43 B, I 07100 Sassari, Italy
Electrophoresis 24:2796-804. 2003....
- L-685,458, an aspartyl protease transition state mimic, is a potent inhibitor of amyloid beta-protein precursor gamma-secretase activityM S Shearman
Department of Molecular Biology, Merck Sharp and Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Harlow, Essex CM20 2QR, England
Biochemistry 39:8698-704. 2000..Specific and potent inhibitors of A beta PP gamma-secretase activity such as L-685,458 will enable important advances toward the identification and elucidation of the mechanism of action of this enigmatic protease...
- Plant growth-promoting Pseudomonas putida WCS358 produces and secretes four cyclic dipeptides: cross-talk with quorum sensing bacterial sensorsGiuliano Degrassi
Bacteriology Group, International Centre for Genetic Engineering and Biotechnology, Area Science Park, Padriciano 99, 34012 Trieste, Italy
Curr Microbiol 45:250-4. 2002..Surprisingly, it was observed that the most abundant compounds in these fractions were cyclic dipeptides (diketopiperazines, DKPs), a rather novel finding in Gram-negative bacteria...
- The renal type H+/peptide symporter PEPT2: structure-affinity relationshipsA Biegel
Institute of Biochemistry, Department of Biochemistry Biotechnology, Martin Luther University Halle Wittenberg, Halle, Germany
Amino Acids 31:137-56. 2006..In this review we compiled available affinity constants of 352 compounds, measured at different mammalian tissues and expression systems and compare the data whenever possible with those of PEPT1...
- Phase II assessment of talabostat and cisplatin in second-line stage IV melanomaRobert M Eager
Mary Crowley Cancer Research Centers, Dallas, TX, USA
BMC Cancer 9:263. 2009..Metastatic melanoma is an incurable disease with an average survival of less than one year. Talabostat is a novel dipeptidyl peptidase inhibitor with immunostimulatory properties...
- 2-Oxoamide inhibitors of phospholipase A2 activity and cellular arachidonate release based on dipeptides and pseudodipeptidesEfrosini Barbayianni
Department of Chemistry, Laboratory of Organic Chemistry, University of Athens, Panepistimiopolis, Athens, Greece
Bioorg Med Chem 17:4833-43. 2009A series of 2-oxoamides based on dipeptides and pseudodipeptides were synthesized and their activities towards two human intracellular phospholipases A(2) (GIVA cPLA(2) and GVIA iPLA(2)) and one human secretory phospholipase A(2) (GV sPLA(..
- Phase II trial of talabostat and docetaxel in advanced non-small cell lung cancerR M Eager
Mary Crowley Cancer Research Centers, Dallas, Texas, USA
Clin Oncol (R Coll Radiol) 21:464-72. 2009..The aim of this study was to determine the efficacy and safety of talabostat in NSCLC patients...
- Insights into the generation of structural diversity in a tRNA-dependent pathway for highly modified bioactive cyclic dipeptidesTobias W Giessen
Department of Chemistry and LOEWE Center for Synthetic Microbiology, Philipps University, Hans Meerwein Strasse, D 35034 Marburg, Germany
Chem Biol 20:828-38. 2013The nocazines are a newly defined family of antibacterial and cytotoxic cyclic dipeptides produced by different actinobacterial species...
- The bioactive dipeptide anserine is transported by human proton-coupled peptide transportersStefanie Geissler
Membrane Transport Group, Biozentrum of Martin Luther University Halle Wittenberg, Halle, Germany
FEBS J 277:790-5. 2010..In addition, anserine might be useful for the design of new substrates of peptide transporters, such as prodrugs, that can be administered orally...
- Functional and biochemical analysis of the Chlamydia trachomatis ligase MurEDelphine Patin
Universite Paris Sud, Institut de Biochimie et Biophysique Moleculaire et Cellulaire, CNRS, Laboratoire des Enveloppes Bactériennes et Antibiotiques, UMR 8619, Orsay F 91405, France
J Bacteriol 191:7430-5. 2009..However, due to the lack of specificity of MurE(Ct) for nucleotide substrates in vitro, it is not obvious which amino acid is present at the first position of the pentapeptide...
- Inhibition of the Notch-Hey1 axis blocks embryonal rhabdomyosarcoma tumorigenesisBrian C Belyea
Department of Pediatrics, Duke University Medical Center, Durham, North Carolina 27710, USA
Clin Cancer Res 17:7324-36. 2011..Given its physiologic role in myogenesis and oncogenic role in other human cancers, we hypothesized that aberrant Notch signaling may contribute to RMS tumorigenesis and present novel therapeutic opportunities...
- γ-glutamylcysteine ethyl ester protects cerebral endothelial cells during injury and decreases blood-brain barrier permeability after experimental brain traumaJosephine Lok
Neuroprotection Research Laboratory, Massachusetts General Hospital, Boston, Massachusetts 02114, USA
J Neurochem 118:248-55. 2011..These data suggest that the beneficial effects of GCEE on brain endothelial cells and microvessels may contribute to its potential efficacy as a neuroprotective agent in traumatic brain injury...
- Alanyl-glutamine and glutamine supplementation improves 5-fluorouracil-induced intestinal epithelium damage in vitroManuel B Braga-Neto
Institute of Biomedicine and Clinical Research Unit University Hospital, Federal University of Ceara, Fortaleza, Brazil
Dig Dis Sci 53:2687-96. 2008..05). These new findings support our earlier study on the benefit of oral glutamine in enhancing epithelial recovery after 5-FU challenge...
- Antihypertensive effect of valyl-tyrosine, a short chain peptide derived from sardine muscle hydrolyzate, on mild hypertensive subjectsT Kawasaki
Institute of Health Science, Kyushu University, Kasuga, Japan
J Hum Hypertens 14:519-23. 2000..VY appeared to have a significant antihypertensive effect on mild hypertensive subjects via Ang I-converting enzyme inhibition, as well as SHR, but no adverse effects could be detected at all...
- Membrane type 1 matrix metalloproteinase is a crucial promoter of synovial invasion in human rheumatoid arthritisMary Clare Miller
Imperial College London, London, UK
Arthritis Rheum 60:686-97. 2009..The aim of this study was to explore the role of one of the collagen-degrading matrix metalloproteinases (MMPs), membrane type 1 MMP (MT1-MMP), in synovial pannus invasiveness...
- Pharmacological inhibition of Notch signaling in the mature guinea pig cochleaRyusuke Hori
Department of Otolaryngology, Head and Neck Surgery, Graduate School of Medicine, Kyoto University, Kyoto, Japan
Neuroreport 18:1911-4. 2007..These findings indicate that pharmacological inhibition of Notch signaling is a possible strategy for hair cell regeneration in adult auditory epithelia...
- The interplay of matrix metalloproteinases, morphogens and growth factors is necessary for branching of mammary epithelial cellsM Simian
Life Sciences Division, Lawrence Berkeley National Laboratory, University of California, Berkeley 94720, USA
Development 128:3117-31. 2001..These results provide direct evidence for a crucial role of MMPs in branching in mammary epithelium and suggest that, in addition to epimorphin, MMP activity is a minimum requirement for branching morphogenesis in the mammary gland...
- Prediction of GTP interacting residues, dipeptides and tripeptides in a protein from its evolutionary informationJagat S Chauhan
Bioinformatics Centre, Institute of Microbial Technology IMTECH, Chandigarh, India
BMC Bioinformatics 11:301. 2010..In this study, an attempt has been made to develop a computational method for predicting GTP interacting residues in a protein with high accuracy (Acc), precision (Prec) and recall (Rc)...
- Caspase and bid involvement in Clostridium difficile toxin A-induced apoptosis and modulation of toxin A effects by glutamine and alanyl-glutamine in vivo and in vitroBenedito A Carneiro
Center for Global Health, Division of Infectious Diseases and International Health, University of Virginia, MR4, Lane Road, Room 3148, Charlottesville, VA 22908, USA
Infect Immun 74:81-7. 2006..Glutamine and alanyl-glutamine inhibited the apoptosis of T84 cells by preventing caspase 8 activation and reduced TxA-induced intestinal secretion and disruption...
- Voltage-gated Sodium Channel Activity Promotes Cysteine Cathepsin-dependent Invasiveness and Colony Growth of Human Cancer CellsLudovic Gillet
INSERM U921, Nutrition, Croissance et Cancer, and INSERM U618, Protéases et Vectorisation Pulmonaires, Universite Francois Rabelais, FacultédeMédecine, 37032 Tours, France
J Biol Chem 284:8680-91. 2009..This general mechanism could lead to the identification of new targets allowing the therapeutic prevention of metastases...
- CA-074Me protection against anthrax lethal toxinZachary L Newman
Bacterial Toxins and Therapeutics Section, Laboratory of Bacterial Diseases, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Bethesda, Maryland 20892, USA
Infect Immun 77:4327-36. 2009..We present results suggesting that LMP may be involved in the activation of the NLRP1b inflammasome...
- Novel variants of muscle calpain 3 identified in human melanoma cells: cisplatin-induced changes in vitro and differential expression in melanocytic lesionsD Moretti
Department of Physiopathology, Experimental Medicine and Public Health, University of Siena, Italy
Carcinogenesis 30:960-7. 2009..On the whole, our observations suggest that calpain 3 variants can play a proapoptotic role in melanoma cells and its downregulation, as observed in highly aggressive lesions, could contribute to melanoma progression...
- Two approaches to discovering and developing new drugs for Chagas diseaseJ H McKerrow
Sandler Center at Mission Bay, University of California, San Francisco, CA 94158 2330, USA
Mem Inst Oswaldo Cruz 104:263-9. 2009..It is optimized for robotic liquid handling and has been validated through a screen of a library of FDA-approved drugs identifying 65 hits...
- Casting metal nanowires within discrete self-assembled peptide nanotubesMeital Reches
Department of Molecular Microbiology and Biotechnology, George S Wise Faculty of Life Sciences, Tel Aviv University, Tel Aviv 69978, Israel
Science 300:625-7. 2003..The same dipeptide building block, made of D-phenylalanine, resulted in the production of enzymatically stable nanotubes...
- Linear non-competitive inhibition of solubilized human gamma-secretase by pepstatin A methylester, L685458, sulfonamides, and benzodiazepinesGaochao Tian
Department of Lead Discovery, AstraZeneca Pharmaceuticals, Wilmington, Delaware 19850, USA
J Biol Chem 277:31499-505. 2002..Models to rationalize how transition state analogs inhibit their targets by non-competitive inhibition are discussed...
- Use of a specific MMP-inhibitor (galardin) for preservation of hybrid layerLorenzo Breschi
Department of Biomedicine, Unit of Dental Sciences and Biomaterials, University of Trieste, Trieste, Italy
Dent Mater 26:571-8. 2010..This study aimed to determine the contribution of a synthetic MMPs inhibitor (galardin) to the proteolytic activity of dentinal MMPs and to the morphological and mechanical features of hybrid layers after aging...
- Stochastic-based descriptors studying peptides biological properties: modeling the bitter tasting threshold of dipeptidesRonal Ramos de Armas
Chemical Bioactives Center, Central University of Las Villas, 54830, Cuba
Bioorg Med Chem 12:4815-22. 2004MARCH-INSIDE methodology was applied to the prediction of the bitter tasting threshold of 48 dipeptides by means of pattern recognition techniques, in this case linear discriminant analysis (LDA), and regression methods...
- Classification of nuclear receptors based on amino acid composition and dipeptide compositionManoj Bhasin
Institute of Microbial Technology, Chandigarh 160036, India
J Biol Chem 279:23262-6. 2004..Furthermore, based on above approach, an online web service, NRpred, was developed, which is available at www.imtech.res.in/raghava/nrpred...
- Cyclo(Phe-Pro) modulates the expression of ompU in Vibrio sppDae Kyun Park
Department of Life Science, Sogang University, Sinsoo Dong 1, Mapo gu, Seoul 121 742, South Korea
J Bacteriol 188:2214-21. 2006..cholerae of the ctx genes, which are known to be regulated by ToxR. Our results suggest that cFP is a signal molecule controlling the expression of genes important for the pathogenicity of Vibrio spp...
- Microporous organic materials from hydrophobic dipeptidesCarl Henrik Görbitz
University of Oslo, Department of Chemistry, P O Box 1033 Blindern, 0315 Oslo, Norway
Chemistry 13:1022-31. 2007In the last few years dipeptides with two hydrophobic residues (hydrophobic dipeptides) have emerged as an unexpected source of stable microporous organic materials...
- ESLpred: SVM-based method for subcellular localization of eukaryotic proteins using dipeptide composition and PSI-BLASTManoj Bhasin
Bioinformatics Centre, Institute of Microbial Technology, Sector 39A, Chandigarh, India
Nucleic Acids Res 32:W414-9. 2004..5% of prediction can be made with an accuracy of 96.4%. Based on the above approach, an online web server ESLpred was developed, which is available at http://www.imtech.res.in/raghava/eslpred/...
- Differential regulation and substrate preferences in two peptide transporters of Saccharomyces cerevisiaeHoujian Cai
Department of Microbiology, University of Tennessee, Knoxville, TN 37996 0845, USA
Eukaryot Cell 6:1805-13. 2007..previously to act as an allantoate/ureidosuccinate permease and to play a role in the utilization of certain dipeptides as a nitrogen source in Saccharomyces cerevisiae...
- Controlled shedding of platelet glycoprotein (GP)VI and GPIb-IX-V by ADAM family metalloproteinasesE E Gardiner
Department of Immunology, Monash University, Alfred Medical Research and Education Precinct, Melbourne, VIC Australia
J Thromb Haemost 5:1530-7. 2007..Platelet glycoprotein (GP)VI that binds collagen, and GPIb-IX-V that binds von Willebrand factor, initiate thrombus formation...
- Incretin-based therapies in the management of type 2 diabetes: rationale and reality in a managed care settingAlan J Garber
Division of Diabetes, Endocrinology, and Metabolism, Baylor College of Medicine, Ste 1000, Houston, TX 77030, USA
Am J Manag Care 16:S187-94. 2010..The AACE/ACE guidelines clearly state that these agents should not be limited to third- or fourth-line therapy...
- The proteasome inhibitor PS-341 in cancer therapyB A Teicher
Dana Farber Cancer Institute and Joint Center for Radiation Therapy, Boston, Massachusetts 02115, USA
Clin Cancer Res 5:2638-45. 1999..c. tumor and was highly effective against disease metastatic to the lungs. The proteasome is an interesting new target for cancer therapy, and the proteasome inhibitor PS-341 warrants continued investigation in cancer therapy...
- Water-mediated conformations of the alanine dipeptide as revealed by distributed umbrella sampling simulations, quantum mechanics based calculations, and experimental dataVictor Cruz
BIOPHYM, Instituto de Estructura de la Materia, CSIC, Madrid, Spain
J Phys Chem B 115:4880-6. 2011..A suitable explanation of the stabilization of the Y conformation mediated by water for the alanine dipeptide is discussed on the basis of Car-Parrinello MD calculations of the dipeptide in water...
- Spinal cathepsin S and fractalkine contribute to chronic pain in the collagen-induced arthritis modelAnna K Clark
King s College London, London, UK
Arthritis Rheum 64:2038-47. 2012..The purpose of this study was to examine the development of pain in the rat model of collagen-induced arthritis (CIA) and to evaluate the contribution of neuroimmune interactions to established arthritis pain...
- A comprehensive library of blocked dipeptides reveals intrinsic backbone conformational propensities of unfolded proteinsKwang Im Oh
Department of Chemistry, Korea University, Seoul 136 701, Korea
Proteins 80:977-90. 2012..Here, we show that spectroscopic studies of a complete library of 400 dipeptides reveal that, irrespective of side-chain properties, the backbone conformation distribution is narrow and they ..
- Synthesis and evaluation of a dipeptide-drug conjugate library as substrates for PEPT1Lihui Zhang
School of Pharmacy, Shanghai Jiaotong University, PR China
ACS Comb Sci 14:108-14. 2012..Results showed that the designed library contained some new structure features that have high affinities toward PEPT1 and could be further explored for their application in prodrug design and development...
- Dipeptidyl peptidase IV inhibitory and antioxidative properties of milk protein-derived dipeptides and hydrolysatesAlice B Nongonierma
Department of Life Sciences and Food for Health Ireland FHI, University of Limerick, Limerick, Ireland
Peptides 39:157-63. 2013Selected synthetic dipeptides and milk protein hydrolysates were evaluated for their dipeptidyl peptidase IV (DPP-IV) inhibitory properties, and their superoxide (SO) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activities...
- Bitter taste receptor T2R1 is activated by dipeptides and tripeptidesJasbir Upadhyaya
Department of Oral Biology, University of Manitoba, Winnipeg, Canada MB R3E 0W4
Biochem Biophys Res Commun 398:331-5. 2010..The ligand binding pocket in T2R1 is present on the extracellular surface of the receptor, and is formed by the transmembrane helices 1, 2, 3 and 7 and with extracellular loops 1 and 2 forming a cap like structure on the binding pocket...
- Predicting the physicochemical profile of diastereoisomeric histidine-containing dipeptides by property space analysisGiulio Vistoli
Dipartimento di Scienze Farmaceutiche Pietro Pratesi, Facolta di Farmacia, Universita degli Studi di Milano, Milano, Italy
Chirality 24:566-76. 2012This study aimed at measuring the lipophilicity and ionization constants of diastereoisomeric dipeptides, interpreting them in terms of conformational behavior, and developing statistical models to predict them.
- Toward the selective delivery of chemotherapeutics into tumor cells by targeting peptide transporters: tailored gold-based anticancer peptidomimeticsMorelle Negom Kouodom
Department of Chemical Sciences, University of Padova, via F Marzolo 1, Padova 35131, Italy
J Med Chem 55:2212-26. 2012..Biological results are here reported and discussed in terms of the structure-activity relationship...
- The transmembrane tyrosines Y56, Y91 and Y167 play important roles in determining the affinity and transport rate of the rabbit proton-coupled peptide transporter PepT1Myrtani Pieri
School of Life Sciences, Oxford Brookes University, Headington, Oxford OX3 OBP, UK
Int J Biochem Cell Biol 41:2204-13. 2009..Y167 was demonstrated to play a pivotal role in rabbit PepT1 function since Y167F, Y167R and Y167Q demonstrated very little transport function. These results are discussed with regard to a proposed mechanism for PepT1 substrate binding...
- Designed aromatic homo-dipeptides: formation of ordered nanostructures and potential nanotechnological applicationsMeital Reches
Department of Molecular Microbiology and Biotechnology, George S Wise Faculty of Life Sciences, Tel Aviv University, Tel Aviv 69978, Israel
Phys Biol 3:S10-9. 2006..We later explored other amine and carboxyl modified diphenylalanine peptide analogues and revealed that these dipeptides can form ordered tubular structures at the nanometric scale...
- Nanovesicles based on self-assembly of conformationally constrained aromatic residue containing amphiphilic dipeptidesAseem Mishra
International Centre for Genetic Engineering and Biotechnology, New Delhi, and National Institute of Virology, Pune, India
Langmuir 24:4571-6. 2008..We here report the self-assembly of amphiphilic dipeptides containing conformation-constraining alpha,beta-dehydrophenylalanine into nanovesicles...
- Mutagenesis and cysteine scanning of transmembrane domain 10 of the human dipeptide transporterLiya Xu
Alcohol and Brain Research Laboratory, Titus Family Department of Clinical Pharmacy and Pharmaceutical Economics and Policy, School of Pharmacy, University of Southern California, Los Angeles, California 90033, USA
Pharm Res 26:2358-66. 2009The human dipeptide transporter (hPEPT1) facilitates transport of dipeptides and drugs from the intestine into the circulation...
- γ-Glutamylcysteine inhibits oxidative stress in human endothelial cellsYukiko K Nakamura
Department of Nutrition, University of Nevada, Reno 89557, USA
Life Sci 90:116-21. 2012..The objective of this study was to investigate the efficacy of GGC on GSH synthesis and oxidative stress in human endothelial cells...
- Ligand binding analyses of the putative peptide transporter YjdL from E. coli display a significant selectivity towards dipeptidesHeidi A Ernst
Biostructural Research, Department of Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark
Biochem Biophys Res Commun 389:112-6. 2009..These results clearly indicate that unlike most POT members characterized to date, including YdgR and YhiP, YjdL shows significantly higher specificity towards dipeptides.
- Cruzain : the path from target validation to the clinicMohammed Sajid
Afd Parasitologie, Leiden University Medical Center, Leiden, The Netherlands
Adv Exp Med Biol 712:100-15. 2011....
- Effect of sequences of the active-site dipeptides of DsbA and DsbC on in vivo folding of multidisulfide proteins in Escherichia coliP H Bessette
Department of Chemical Engineering, University of Texas, Austin, Texas 78712, USA
J Bacteriol 183:980-8. 2001We have examined the role of the active-site CXXC central dipeptides of DsbA and DsbC in disulfide bond formation and isomerization in the Escherichia coli periplasm...
- Cathepsins B, L and D in inflammatory bowel disease macrophages and potential therapeutic effects of cathepsin inhibition in vivoK Menzel
Department of Internal Medicine I, University of Regensburg, Regensburg, Germany
Clin Exp Immunol 146:169-80. 2006..Inhibition of CTSD as well as CTSB/CTSL is followed by an amelioration of experimental colitis. The prevention of mucosal damage by cathepsin inhibition could represent a new approach for the therapy of IBD...
- The structure and mechanism of the Mycobacterium tuberculosis cyclodityrosine synthetaseMatthew W Vetting
Department of Biochemistry, Albert Einstein College of Medicine, Bronx, New York, USA
Nat Chem Biol 6:797-9. 2010....
- Switch of CD4+ T cell differentiation from Th2 to Th1 by treatment with cathepsin B inhibitor in experimental leishmaniasisY Maekawa
Department of Parasitology and Immunology, University of Tokushima School of Medicine, Japan
J Immunol 161:2120-7. 1998..These findings indicate that cathepsin B inhibitor could switch CD4+ T cell differentiation from Th2 to Th1, suggesting that the alteration in Ag processing modulates the polarity of Th differentiation...
- Tissue distribution of antihypertensive dipeptide, Val-Tyr, after its single oral administration to spontaneously hypertensive ratsToshiro Matsui
Faculty of Agriculture, Graduate School of Kyushu University, Fukuoka, Japan
J Pept Sci 10:535-45. 2004....
- Pharmacokinetics and tissue distribution of PGG-paclitaxel, a novel macromolecular formulation of paclitaxel, in nu/nu mice bearing NCI-460 lung cancer xenograftsXinghe Wang
Biogroup, Nitto Denko Technical Corporation, 501 Via Del Monte, Oceanside, CA 92058, USA
Cancer Chemother Pharmacol 65:515-26. 2010..The purpose of this study was to compare the pharmacokinetics and tissue distribution of PTX following injection of either free PTX or PGG-PTX in mice...
- Calpain-dependent cleavage of SHP-1 and SHP-2 is involved in the dephosphorylation of Jurkat T cells induced by Entamoeba histolyticaK A Kim
Department of Environmental Medical Biology, Institute of Tropical Medicine, and Brain Korea 21 Project for Medical Science, Yonsei University College of Medicine, Seoul, Korea
Parasite Immunol 32:176-83. 2010..These results suggest that calpain-dependent cleavage of SHP-1 and SHP-2 may contribute to protein tyrosine dephosphorylation in Jurkat T cell death induced by E. histolytica...
- Calpain-dependent calpastatin cleavage regulates caspase-3 activation during apoptosis of Jurkat T cells induced by Entamoeba histolyticaKyeong Ah Kim
Department of Parasitology, Institute of Tropical Medicine, and Brain Korea 21 for Medical Science, Yonsei University College of Medicine, 134 Sinchon dong, Seodaemun gu, Seoul 120 752, Republic of Korea
Int J Parasitol 37:1209-19. 2007..Our results suggest that calpain-mediated calpastatin degradation plays a crucial role in regulation of caspase-3 activation during apoptosis of Jurkat T cells by E. histolytica...
- Entamoeba histolytica-induced dephosphorylation in host cellsJose E Teixeira
Department of Internal Medicine, University of Virginia, School of Medicine, Charlottesville, Virginia 22908, USA
Infect Immun 70:1816-23. 2002..histolytica. These results suggest that E. histolytica-mediated host cell death occurs by a mechanism that involves PTPase activation...
- AtPTR1 and AtPTR5 transport dipeptides in plantaNataliya Y Komarova
Molecular Plant Physiology, Institute of Plant Sciences, University of Bern, Bern, Switzerland
Plant Physiol 148:856-69. 2008..Both transporters facilitate transport of dipeptides with high affinity and are localized at the plasma membrane...
- Trichodermamide A and aspergillazine A, two cytotoxic modified dipeptides from a marine-derived fungus Spicaria elegansRui Liu
Key Laboratory of Marine Drugs, Chinese Ministry of Education, Institute of Marine Drugs and Food, Ocean University of China, Qingdao 266003, PR China
Arch Pharm Res 28:1042-6. 2005Two known modified dipeptides, trichodermamide A (1) and aspergillazine A (2), were isolated from an ethyl acetate extract of the metabolite of a marine-derived fungus Spicaria elegans, and were found to have a weak cytotoxic effect on ..
- Identification of gamma-secretase inhibitor potency determinants on presenilinByron Zhao
Elan Pharmaceuticals Inc, 700 Gateway Boulevard, South San Francisco, CA 94080, USA
J Biol Chem 283:2927-38. 2008..Our observations demonstrate that PS-selective inhibitors of gamma-secretase are feasible, and such inhibitors may allow differential inhibition of Abeta peptide production and Notch signaling...
- Effects of the calpain inhibitor MDL28170 on the clinically relevant forms of Trypanosoma cruzi in vitroVítor Ennes-Vidal
Laboratório de Biologia Molecular e Doenças Endêmicas, Instituto Oswaldo Cruz IOC, Fundação Oswaldo Cruz FIOCRUZ, Rio de Janeiro, Brazil
J Antimicrob Chemother 65:1395-8. 2010..In the present work, we evaluated the in vitro activity of the calpain inhibitor MDL28170 against Trypanosoma cruzi relevant clinical forms...
- Electric fields due to synaptic currents sharpen excitatory transmissionSergiy Sylantyev
Institute of Neurology, University College London, Queen Square, London, WC1N 3BG, UK
Science 319:1845-9. 2008..Voltage-dependent temporal tuning of excitatory synaptic responses may thus contribute to signal integration in neural circuits...
- The cytotoxicity of gamma-secretase inhibitor I to breast cancer cells is mediated by proteasome inhibition, not by gamma-secretase inhibitionJianxun Han
Department of Oncology, University of Alberta, Cross Cancer Institute, 11560 University Avenue, Edmonton, Alberta, Canada T6G 1Z2
Breast Cancer Res 11:R57. 2009....
- Determination of the MurD mechanism through crystallographic analysis of enzyme complexesJ A Bertrand
Laboratoire de Cristallographie Macromoléculaire, Institut de Biologie Structurale Jean Pierre Ebel CEA CNRS, 41 rue Jules Horowitz, Grenoble Cedex 1, F 38027, France
J Mol Biol 289:579-90. 1999..A key feature in the reaction intermediate is the presence of two magnesium ions bridging negatively charged groups...
- N-Acetylaspartylglutamate: the most abundant peptide neurotransmitter in the mammalian central nervous systemJ H Neale
Department of Biology, Georgetown University, Washington, D C, USA
J Neurochem 75:443-52. 2000..A second role is the production of extracellular glutamate following NAAG hydrolysis...
- Combinatorial chemistry identifies high-affinity peptidomimetics against alpha4beta1 integrin for in vivo tumor imagingLi Peng
Division of Hematology and Oncology, Department of Internal Medicine, UC Davis Cancer Center, University of California, Davis, 4501 X Street, Sacramento, California 95817, USA
Nat Chem Biol 2:381-9. 2006..Thus, LLP2A provides an important tool for noninvasive monitoring of alpha4beta1 expression and activity during tumor progression, and it shows great potential as an imaging and therapeutic agent for alpha4beta1-positive tumors...
- Establishment of a novel B-cell lymphoma cell line with suppressed growth by gamma-secretase inhibitorsShuji Tohda
Department of Laboratory Medicine, Tokyo Medical and Dental University, Yushima 1 5 45, Bunkyo ku, Tokyo 113 8519, Japan
Leuk Res 30:1385-90. 2006..In addition to T-ALL, TMD8 is another unique cell line sensitive to GSI, and is useful to study effects of GSI in molecular targeting therapy...
- Clostridium difficile toxin A induces intestinal epithelial cell apoptosis and damage: role of Gln and Ala-Gln in toxin A effectsGerly A C Brito
Center for Global Health, Department of Intemal Medicine, School of Medicine, University of Virginia, Charlottesville, Virginia, USA
Dig Dis Sci 50:1271-8. 2005..In conclusion, both peptides reduced toxin-induced epithelial damage and thus might play an adjunctive role in C. difficile-induced colitis therapy...
- Arrested growth of Trypanosoma cruzi by the calpain inhibitor MDL28170 and detection of calpain homologues in epimastigote formsL S Sangenito
Departamento de Microbiologia Geral, Instituto de Microbiologia Prof Paulo de Goes, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Brazil
Parasitology 136:433-41. 2009..These results may contribute for the investigation of the functions of CALPs in trypanosomatids...
- Prediction and classification of aminoacyl tRNA synthetases using PROSITE domainsBharat Panwar
Bioinformatics Centre, Institute of Microbial Technology, Chandigarh, India
BMC Genomics 11:507. 2010..There are twenty different types of aaRSs, unique for each amino acid. These aaRSs have been divided into two classes, each comprising ten enzymes. It is important to predict and classify aaRSs in order to understand protein synthesis...
- A systematic assessment of cardiovascular outcomes in the saxagliptin drug development program for type 2 diabetesRobert Frederich
Bristol Myers Squibb, Princeton, NJ 08543, USA
Postgrad Med 122:16-27. 2010..The objective was to assess the relative risk (RR) for cardiovascular (CV) events across all 8 randomized phase 2/3 trials evaluating saxagliptin in patients with type 2 diabetes mellitus...
- Notch3 signaling promotes the development of pulmonary arterial hypertensionXiaodong Li
University of California San Diego, La Jolla, CA, USA
Nat Med 15:1289-97. 2009..These results suggest that the NOTCH3-HES-5 signaling pathway is crucial for the development of pulmonary arterial hypertension and provide a target pathway for therapeutic intervention...
- Deletion of the glutamate carboxypeptidase II gene in mice reveals a second enzyme activity that hydrolyzes N-acetylaspartylglutamateDean J Bacich
Department of Cancer Biology, The Cleveland Clinic, Cleveland, Ohio, USA
J Neurochem 83:20-9. 2002..The IC50 value for 2-PMPA was about 1 nm for wild-type brain membrane NAAG peptidase activity consistent with its activity against cloned ratand human GCPII, and 88 nm for the activity in brain membranes of the null mutants...
- Over-expression of calpastatin inhibits calpain activation and attenuates myocardial dysfunction during endotoxaemiaXiaoping Li
Shanghai Institute of Cardiovascular Diseases, Zhongshan Hospital, Fudan University, Shanghai, China
Cardiovasc Res 83:72-9. 2009..The present study was to investigate the roles of calpain/calpastatin system in cardiomyocyte caspase-3 activation, TNF-alpha expression, and myocardial dysfunction during LPS stimulation...
- NAAG peptidase inhibitor increases dialysate NAAG and reduces glutamate, aspartate and GABA levels in the dorsal hippocampus following fluid percussion injury in the ratChunlong Zhong
Department of Neurological Surgery, University of California at Davis, Davis, California 95616 8797, USA
J Neurochem 97:1015-25. 2006..The results are consistent with the hypothesis that inhibition of NAAG peptidase may reduce excitotoxic events associated with TBI...
- The disintegrin-like metalloproteinase ADAM10 is involved in constitutive cleavage of CX3CL1 (fractalkine) and regulates CX3CL1-mediated cell-cell adhesionChristian Hundhausen
Institute for Biochemistry, Christian Albrechts University, Kiel, Germany
Blood 102:1186-95. 2003..Our data demonstrate that ADAM10 is involved in the constitutive cleavage of CX3CL1 and thereby may regulate the recruitment of monocytic cells to CX3CL1-expressing cell layers...
- Peptides accelerate their uptake by activating a ubiquitin-dependent proteolytic pathwayG C Turner
Division of Biology, California Institute of Technology, Pasadena 91125, USA
Nature 405:579-83. 2000..We show that the degradation of Cup9 is allosterically activated by dipeptides with destabilizing N-terminal residues...
- Mechanism of Gly-Pro-pNA cleavage catalyzed by dipeptidyl peptidase-IV and its inhibition by saxagliptin (BMS-477118)Young B Kim
Department of Chemical Enzymology, Bristol Myers Squibb Pharmaceutical Company, Pharmaceutical Research Institute, P O Box 5400, Princeton, NJ 08543 5400, USA
Arch Biochem Biophys 445:9-18. 2006..4 and 14.1 ppm were observed upon mixing the enzyme with saxagliptin. Fractionation factors (phi) of 0.6 and 0.5 for the 17.4 and 14.1 ppm peaks, respectively, are suggestive of short strong hydrogen bonds in the enzyme-inhibitor complex...
- The design and rationale of the saxagliptin assessment of vascular outcomes recorded in patients with diabetes mellitus-thrombolysis in myocardial infarction (SAVOR-TIMI) 53 studyBenjamin M Scirica
TIMI Study Group, Cardiovascular Division, Brigham and Women s Hospital and Harvard Medical School, Boston, MA, USA
Am Heart J 162:818-825.e6. 2011....
- The cyclic dipeptide cyclo(Phe-Pro) inhibits cholera toxin and toxin-coregulated pilus production in O1 El Tor Vibrio choleraeXiaowen R Bina
The University of Tennessee Health Sciences Center, Department of Molecular Sciences, 858 Madison Avenue, Memphis, TN 38163, USA
J Bacteriol 192:3829-32. 2010..The cyclo(Phe-Pro) inhibition of CT and TCP production correlated with reduced transcription of the virulence regulator tcpPH and was alleviated by overexpression of tcpPH...
- Populations of the three major backbone conformations in 19 amino acid dipeptidesJoze Grdadolnik
National Institute of Chemistry, Hajdrihova 19, SI 1000 Ljubljana, Slovenia
Proc Natl Acad Sci U S A 108:1794-8. 2011..the relative populations of the three major backbone conformations (P(II), β, and α(R)) in 19 amino acid dipeptides. The results provide a benchmark for force field or other methods of predicting backbone conformations in ..
- Selective inhibition of human inducible nitric oxide synthase by S-alkyl-L-isothiocitrulline-containing dipeptidesJ M Park
Graduate School of Pharmaceutical Sciences, The University of Tokyo, Hongo, Bunkyo-ku, Tokyo 113-0033, Japan
Br J Pharmacol 132:1876-82. 2001..of this study was to investigate the structure-activity relationship of S-alkyl-L-isothiocitrulline-containing dipeptides towards three partially purified recombinant human nitric oxide synthase (NOS) isozymes, as well as the effects ..
- The protonation equilibria of selected glycine dipeptides in ethanol-water mixture: solvent composition effectAlev Dogan
Department of Science, Faculty of Gazi Education, University of Gazi, Ankara, Turkey
Amino Acids 36:373-9. 2009..In this study, the protonation constants of some aliphatic dipeptides (Gly-Gly, Gly-Val, Gly-Leu, Gly-Thr, Gly-Phe and Gly-Met) were studied in water and ethanol-water mixtures [20% ..
- Papain-specific activating esters in aqueous dipeptide synthesisRoseri J A C de Beer
Institute for Molecules and Materials, Radboud University Nijmegen, Heyendaalseweg 135, 6525 AJ Nijmegen, The Netherlands
Chembiochem 13:1319-26. 2012..Finally, selected ODmap- and OBn-activated amino acids were applied in the synthesis of two biologically active dipeptides on preparative scales.
- Structural basis for recognition of dipeptides by peptide transportersJ W Payne
School of Biological Sciences, University of Wales Bangor, Gwynedd, United Kingdom
Arch Biochem Biophys 384:9-23. 2000..Computer-based conformational analysis of the test dipeptides was performed to define the repertoire of conformers that each dipeptide adopts in solution...
- Self-assembly of amphiphilic dendritic dipeptides into helical poresVirgil Percec
Roy and Diana Vagelos Laboratories, Department of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104 6323, USA
Nature 430:764-8. 2004..Here we describe a library of amphiphilic dendritic dipeptides that self-assemble in solution and in bulk through a complex recognition process into helical pores...
- Comparison of quantitative conformer analyses by nuclear magnetic resonance and Raman optical activity spectra for model dipeptidesMilos Budesinsky
Institute of Organic Chemistry and Biochemistry, Academy of Sciences, Flemingovo nam 2, 16610, Prague 6, Czech Republic
J Phys Chem A 112:8633-40. 2008..However, on a series of the Pro-Gly, Gly-Pro, Pro-Ala, and Ala-Pro dipeptides more precise conformer ratios could be obtained with the aid of the density functional computations and ..
- Carnosine and related dipeptides protect human ceruloplasmin against peroxyl radical-mediated modificationJung Hoon Kang
Department of Genetic Engineering, Chongju University, Korea
Mol Cells 13:498-502. 2002..We investigated the effects of antioxidant dipeptides carnosine, homocarnosine and anserine on peroxyl radical-mediated ceruloplasmin modification...
- gamma-Secretase activity modulates store-operated Ca2+ entry into rat sensory neuronsCharles R Shideman
Department of Pharmacology, University of Minnesota Medical School, 6 120 Jackson Hall, 321 Church Street SE, Minneapolis, MN 55455 0217, United States
Neurosci Lett 451:124-8. 2009..SKF96365, an inhibitor of store-operated channels, blocked SOCE in cells expressing PS1-D257A. Thus, gamma-secretase proteolytic activity regulates a SOCE pathway in sensory neurons...
- Critical role for cathepsin B in mediating caspase-1-dependent interleukin-18 maturation and caspase-1-independent necrosis triggered by the microbial toxin nigericinH Hentze
Institute of Molecular and Cell Biology, Singapore, Republic of Singapore
Cell Death Differ 10:956-68. 2003..Collectively, our study establishes a critical role for cathepsin B in nigericin-induced caspase-1-dependent IL-18 maturation and caspase-1-independent necrosis...
- Inhibitor of DASH proteases affects expression of adhesion molecules in osteoclasts and reduces myeloma growth and bone diseaseAngela Pennisi
Myeloma Institute for Research and Therapy, University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA
Br J Haematol 145:775-87. 2009..These data demonstrated that DASH proteases are involved in myeloma bone disease and tumour growth...
- Asymmetric conjugate reductions with samarium diiodide: asymmetric synthesis of (2S,3R)- and (2S,3S)-[2-2H,3-2H]-leucine-(S)-phenylalanine dipeptides and (2S,3R)-[2-(2)H,3-2H]-phenylalanine methyl esterStephen G Davies
Department of Organic Chemistry, University of Oxford, Chemistry Research Laboratory, UK
Org Biomol Chem 3:1435-47. 2005..27 in > or = 95% de and >98% ee, and (2S,3R)- or (2S,3S)-dideuterioleucine-(S)-phenylalanine dipeptides 37 and 38 in moderate de, 66% and 74% respectively. A mechanism is proposed to account for this process.
- Discovery metabolite profiling of the prolyl peptidasesAlan Saghatelian; Fiscal Year: 2009..Furthermore, the application of DMP to peptidases will demonstrate the generality of this approach for the future characterization of medically relevant enzymes and signaling pathways. ..
- Pharmacogenetics of ACE inhibitor-associated angioedemaNANCY JOAN BROWN; Fiscal Year: 2013..DPPIV, a cell-surface protease, preferentially cleaves dipeptides from the amino terminus of peptides with a penultimate proline or alanine, including the incretins, vasoactive ..
- Shifts in the Gastrointestinal Metabolome During Clostridium difficile InfectionCASEY THERIOT; Fiscal Year: 2013..in primary bile acids, carbohydrates, and amino acids and decreased free fatty acids, secondary bile acids and dipeptides;reflecting the diminished metabolic activity of the gut microbiome. Subsequently, we demonstrated that C...
- HIV integrase/DNA complexes and concerted integrationDuane P Grandgenett; Fiscal Year: 2010..responsible for formation of the tetramer, as determined by mass spectrometry studies of cross-linked tryptic dipeptides. In- gel fluorescence resonance energy transfer-derived distance measurements and atomic force microscopy will ..
- Species selective dipeptide inhibitors for Mtb proteasomeGang Lin; Fiscal Year: 2013..In our recent screening of 1600 capped dipeptides, we identified a lead compound that potently and species-selectively inhibited the Mtb proteasome over the human ..
- ASF/SF2: Phosphorylation and RNA BindingGourisankar Ghosh; Fiscal Year: 2012..cycle of phosphorylation and dephosphorylation of the C-terminal region enriched in arginine-serine (RS) dipeptides during splicing is also critical for splicing...
- Optimization of dipeptide-linked benzimidazole topoisomerase 1 poisonsCraig Beeson; Fiscal Year: 2009..Structural insights from Top1-DNA crystal structures were used to design a small library of N-acetyl dipeptides linked to Hoechst 33258, a DNA minor groove binder...
- ANALYSIS OF ENDORPHINS BY LC-ELECTROCHEMISTRYNorman Reynolds; Fiscal Year: 1990..of amino acid sequence upon the electroactivity of the N-terminal tyrosyl will be evaluated in a variety of dipeptides and longer peptide sequences to examine both steric and inductive effects upon redox activity...
- REGULATION OF B-ALANINE METABOLISMTHOMAS TRAUT; Fiscal Year: 1990Beta-Alanine is an amino acid that functions as a neurotransmitter, and also in the biosynthesis of the abundant dipeptides carnosine and anserine in brain and muscle...
- Novel glutamate conjugates for radiotargeting PSMAJohn Babich; Fiscal Year: 2004..based on two fundamental structures, phosphonate and phosphinate containing transition state analogues and novel dipeptides connected through a simple urea linkage...
- STRUCTURALLY NEW BIOPOLYMERS DERIVED FROM AMINO ACIDSJoachim Kohn; Fiscal Year: 1992..b) Polymerization of suitably protected dipeptides by reaction schemes that include the peptide side chains...
- METABOLISM AND CLINICAL APPLICATION OF OLIGOPEPTIDESSIAMAK ADIBI; Fiscal Year: 1991..These investigations have included transport and hydrolysis of dipeptides and metabolism of their amino acid residues...
- ENDOGENOUS LIGANDS FOR GLUTAMATE RECEPTORS IN BRAINPeter Petrusz; Fiscal Year: 1991..1)Glu and Asp, (2) dipeptides with C- terminal Glu and Asp residues, (3) nonendogenous compounds which can discriminate between subclasses of ..
- TRYPANOSOMA CRUZI SIGNALING FACTORNorma Andrews; Fiscal Year: 1999..emerged prolyl oligopeptidase family of serine hydrolases, several of which are processing enzymes which remove dipeptides from N-terminal extentions of immature precursor peptides...
- EFFICACY OF GLUTAMINE DIPEPTIDE IN CATABOLIC PATIENTSThomas Ziegler; Fiscal Year: 2000..As an alternative, GLN dipeptides such as alanyl-GLN (ALA-GLN) confer both stability and solubility, and the dipeptides, are rapidly hydrolyzed to ..
- PROTEIN PRIMARY STRUCTURE THROUGH DIPEPTIDE ANALYSISRichard Caprioli; Fiscal Year: 1980Dipeptidyl aminopeptidases (DAP's) are a family of exopeptidases which hydrolize dipeptides from the N-termini of various peptides...
- CMICHAEL SMAR; Fiscal Year: 1992..These isosteres, which more accurately mimic dipeptides, have not yet been used to produce enzyme inhibitors...
- ENZYMATIC SYNTHESIS OF SPECIFIC DIPEPTIDES FOR NUTRITIONJames West; Fiscal Year: 1992DESCRIPTION: (Adapted from the investigator's abstract.) Recent investigations indicate that dipeptides may have several advantages over free amino acids as the nitrogen source in therapeutic enteral and parenteral nutrition...
- REVERSE TURN RECOGNITION AND MIMETIC PROPENSITYGARLAND MARSHALL; Fiscal Year: 2002..We propose to continue the design and synthesis of novel reverse turn mimics derived from simple dipeptides. Computational tools will be used to predict the reverse-turn propensities of potential mimetics prior to their ..
- STRUCTURAL BASIS OF RNA-CATALYZED AMINOACYLATION OF RNAJohn Arnez; Fiscal Year: 2007..Ribozymes of the third class also catalyze the formation of dipeptides, a reaction analogous to that catalyzed by a large ribozyme, the ribosome...
- NOVEL 199HG NMR METHODS FOR MONITORING PROTEIN FOLDINGDEBORAH BEBOUT; Fiscal Year: 1999..Finally, the Hg(II) coordination chemistry of a variety of potentially metal-coordinating cyclic dipeptides will be examined using X-ray crystallography and NMR as a prelude to the application of these new techniques to ..
- ABC Transport Components: Structures and FunctionsFlorante Quiocho; Fiscal Year: 2006..The structures of the dipeptide-binding protein with bound dipeptides may provide fruitful leads in the development of antibacterial drugs (including impermeant peptidomimetric drugs)..
- Predoctoral Fellowship for Students with DisabilitiesTIMOTHY CLICK; Fiscal Year: 2006..I will test the free energy calculation method with small organic molecules, dipeptides, and helix-forming and sheet-forming proteins...
- Heterochiral Dipeptides of Chimeric Cyclic Amino AcidsGARLAND MARSHALL; Fiscal Year: 2008..The therapeutic target for development of specific inhibition is the CXCR4 receptor with potential applications as an antiviral and in oncology. ..
- Inhibition of Alcohol Intake by Non-opioid PeptideGARTH RESCH; Fiscal Year: 2005....
- DESIGN AND SYNTHESIS OF NONPEPTIDE PROTEASE INHIBITORSArun K Ghosh; Fiscal Year: 2010..This research integrates organic synthesis, protein-ligand x-ray crystallography, molecular modeling and in-depth virus and cell-biological studies to design the next generation of HIV-1 protease inhibitors. ..
- DEVELOPMENT OF LIGAND ASSISTED ASYMMETRIC SYNTHESESArun Ghosh; Fiscal Year: 2001..Besides the broad range of scope and generality, this line of research will provide excellent opportunities to teach and train graduate and undergraduate students in the laboratory. ..
- H2S PRODUCTION AND VIRULENCE OF TREPONEMA DENTICOLALianrui Chu; Fiscal Year: 2007..denticola to produce H2S from glutathione. The outcomes will elucidate the mechanisms of action that each member of the enzyme pathway plays in the virulence capacity of T. denticola. ..
- NAAG PEPTIDASE AND NEURONAL FUNCTIONJOSEPH NEALE; Fiscal Year: 2008..The influence of elevated NAAG levels in vivo, obtained by inhibition of NAAG peptidase activity, will be tested in rat brain and spinal cord and in transgenic mice expressing GLT-1-GFP and GLAST-GFP fusion proteins. ..
- POMC Processing and Beta-Endorphine-Related Opioid PeptidesVivian Y H Hook; Fiscal Year: 2010..New findings from this project will enhance our knowledge of the complexity of biosynthetic mechanisms for endogenous opioid and neuropeptide systems. ..
- Serpin Protease Inhibitors & Opioid NeuropeptidesVivian Hook; Fiscal Year: 2006..Serpin regulation of opioid peptides that mediate analgesia and stress may lead to development of new therapeutic approaches in pain and neurologic disease. ..
- BIOSYNTHESIS OF ENKEPHALIN OPIOID PEPTIDESVivian Hook; Fiscal Year: 2009..These findings will enhance our knowledge of the complexity of the endogenous opioid system. ..
- p56lck Inhibitors as Potential Immunosuppressive Drugs.ALEXANDER MACKERELL; Fiscal Year: 2004..Following completion of the proposed study compounds that inhibit the p56lck SH2 domain will be available as research tools and as lead compounds for the development of novel immunosuppressant drugs. ..
- INTEGRATED DNA SEQUENCING SYSTEMVivian Hook; Fiscal Year: 2002..abstract_text> ..
- Proteomics/Genomics of Opiate Analgesia and AddictionVivian Hook; Fiscal Year: 2004..Elucidation of distinct pathways will be significant, since it could allow future design of opiate drug regimens that provide effective analgesia, without the tolerance and dependence of addiction. ..
- Developing NAAG Peptidase Inhibitors for NeuroprotectionJOSEPH NEALE; Fiscal Year: 2005....
- Bilirubin oxidation and intracerebral hemorrhageJoseph Clark; Fiscal Year: 2009..These studies are important because we believe that strategies designed to prevent BOXes production in the hematoma should provide a novel and beneficial therapeutic option for patients who have suffered an ICH. ..
- REGULATION OF NA-NUTRIENT CO-TRANSPORTUMA SUNDARAM SUNDARAM; Fiscal Year: 2010..This knowledge will provide the basis for new and more efficacious treatment modalities for the most common morbidities of IBD specifically, malabsorption, diarrhea and malnutrition. ..
- Viral-induced T Cell Responses in COPD ExacerbationFarrah Kheradmand; Fiscal Year: 2009....
- Adenosine Agonists: Potential Antiglaucoma AgentsCraig E Crosson; Fiscal Year: 2010..abstract_text> ..
- Divergent Pathways of Cell Death after Brain InjuryRobert S B Clark; Fiscal Year: 2010..Several unique pathways contribute to overall brain damage. This application seeks to define clinically important pathways, and design novel, sex-based strategies that improve neurological outcome after brain injury. ..
- Designing HTA therapy for drug resistant malariaChristian Wolf; Fiscal Year: 2009..Our long term goal is the identification of novel, inexpensive, efficacious therapy for treating drug resistant malaria. ..
- Gender-Specific Treatment of Pediatric Cardiac ArrestRobert Clark; Fiscal Year: 2009..abstract_text> ..
- Molecular Target Focused Discovery of Anticancer DrugsGEORGE PETTIT; Fiscal Year: 2007..In summary, the proposed research will be sharply aimed at the discovery and very rapid development of new anticancer drugs for the NCI programs direct at improving human cancer treatments. ..
- ANTIBIOTIC INHIBITION OF BACTERIAL RIBOSOME FORMATIONWILLIAM CHAMPNEY; Fiscal Year: 2002..The findings from this work will help in assessing the effectiveness of existing antibiotics and in developing new compounds as antimicrobial agents. ..
- CLONOTYPIC PCR FOR MINIMAL RESIDUAL DISEASE IN LYMPHOMAAriela Noy; Fiscal Year: 2002..In addition, the extensive patient population facilitates the execution of a large number of clinical protocols in a timely manner. ..
- Molecular Basis of K+ Current During SecretionKeith Nehrke; Fiscal Year: 2002..Finally, we will look at compensatory changes that occur in the expression of functionally-related ion transport proteins in the transgenic strain. ..
- Na+/H+ exchange in the nematode intestineKeith Nehrke; Fiscal Year: 2004..This multidisciplinary approach will help to define the biological role of individual Na+/H+ exchangers in the nematode intestine. ..
- IMPACT OF AH RECEPTOR DEGRADATION IN VIVO AND IN VITRORICHARD POLLENZ; Fiscal Year: 2005..abstract_text> ..
- Therapeutic Vaccine for EBV-associated Hodgkins DiseaseRajiv Khanna; Fiscal Year: 2005..The long-term aim of this project is to develop a rational basis for the delivery of a curative EBV-specific CTL immunity to not only in HIV patients with HD patients but also for non-HIV HD. ..
- High Throughput Assay for Screening Compounds(RMI)James McKerrow; Fiscal Year: 2005..Computational and informatics capability is in place to acquire, store and cross-reference this data, and provide access to the scientific community through an open-source website. ..
- Leukocyte Mechanotransduction of Fluid Shear StressHAINSWORTH SHIN; Fiscal Year: 2006..These studies will elucidate a possible control mechanism which, in the absence of ' agonists, prevents leukocyte pseudopod formation and migration under physiological conditions. [unreadable] [unreadable]..
- Creatine Transport Across the Blood Brain BarrierJoseph Clark; Fiscal Year: 2006..The goal for Hypothesis 2 is to develop methods and drugs to improve brain energy metabolism by getting creatine into the brain. ..
- Host Protein Degradation by Schistosome ParasitesJames McKerrow; Fiscal Year: 2007..abstract_text> ..
- The Role of Proteases in Lung Inflammation & RemodelingFarrah Kheradmand; Fiscal Year: 2007..This work may serve as the foundation for future therapeutic studies that target a broad range of asthmatic patients. ..
- Altered endothelial heparan sulfate causes diaphragmatic hernias resembling CDHJeffrey Esko; Fiscal Year: 2007..Heparan sulfate-deficient mice will be crossed with Slit3+/- and Robo+/- mice to test if the combination of these mutations potentiates the CDH phenotype (onset, penetrance, and severity). [unreadable] [unreadable] [unreadable]..
- pH Regulation of Fat Storage in the Nematode IntestineKeith Nehrke; Fiscal Year: 2007..The strength of this proposal is that it will use a powerful model system and novel reagents for monitoring pH in living organisms to study fat biology from a unique perspective: that of acid-base homeostasis. ..
- AT1 Receptor Activating Autoantibodies and PreeclampsiaYang Xia; Fiscal Year: 2008..This hypothesis has the ability to explain many features of this complex life threatening condition and immediately suggests diagnostic and therapeutic opportunities. ..
- F. tularensis Virulence Protein Structure and FunctionKARL KLOSE; Fiscal Year: 2008..These studies will dramatically increase our knowledge of this organism and how it causes disease. The results will assist in the development of novel therapeutics and subunit vaccines. [unreadable] [unreadable] [unreadable]..
- KNOCKOUT MODEL FOR CANAVAN DISEASEReuben Matalon; Fiscal Year: 2001..5) The knock-out mouse will be used in future studies for determining the metabolic role of NAA in brain, for experimentation with enzyme therapy and gene therapy. ..