A high-throughput, multiplexed assay for superfamily-wide profiling of enzyme activity

[1]  J. Lai,et al.  Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase. , 2013, Journal of medicinal chemistry.

[2]  A. Lambeir,et al.  Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold. , 2013, ACS medicinal chemistry letters.

[3]  R. Stern,et al.  Telaprevir-related dermatitis. , 2013, JAMA dermatology.

[4]  J. Lai,et al.  4-Substituted boro-proline dipeptides: synthesis, characterization, and dipeptidyl peptidase IV, 8, and 9 activities. , 2012, Bioorganic & medicinal chemistry letters.

[5]  L. Hamann,et al.  Potency, selectivity and prolonged binding of saxagliptin to DPP4: maintenance of DPP4 inhibition by saxagliptin in vitro and ex vivo when compared to a rapidly-dissociating DPP4 inhibitor , 2012, BMC pharmacology.

[6]  B. Cravatt,et al.  The pharmacological landscape and therapeutic potential of serine hydrolases , 2012, Nature Reviews Drug Discovery.

[7]  Mindy I. Davis,et al.  Comprehensive analysis of kinase inhibitor selectivity , 2011, Nature Biotechnology.

[8]  Theonie Anastassiadis,et al.  Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity , 2011, Nature Biotechnology.

[9]  J. Long,et al.  The metabolic serine hydrolases and their functions in mammalian physiology and disease. , 2011, Chemical reviews.

[10]  Thomas M Green,et al.  A public genome-scale lentiviral expression library of human ORFs , 2011, Nature Methods.

[11]  J. Lai,et al.  Chemical and biological evaluation of dipeptidyl boronic acid proteasome inhibitors for use in prodrugs and pro-soft drugs targeting solid tumors. , 2011, Journal of medicinal chemistry.

[12]  J. Schlütter.  Therapeutics: New drugs hit the target , 2011, Nature.

[13]  J. Chang,et al.  A potent and selective inhibitor of KIAA1363/AADACL1 that impairs prostate cancer pathogenesis. , 2011, Chemistry & biology.

[14]  T. Spicer,et al.  Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors , 2011, Proceedings of the National Academy of Sciences.

[15]  T. Muchamuel,et al.  Nonproteasomal Targets of the Proteasome Inhibitors Bortezomib and Carfilzomib: a Link to Clinical Adverse Events , 2011, Clinical Cancer Research.

[16]  Sherry L. Niessen,et al.  Superfamily-wide portrait of serine hydrolase inhibition achieved by library-versus-library screening , 2010, Proceedings of the National Academy of Sciences.

[17]  A. Clemens,et al.  Dabigatran: an oral novel potent reversible nonpeptide inhibitor of thrombin. , 2010, Arteriosclerosis, thrombosis, and vascular biology.

[18]  Kenny K. Wong,et al.  Design and synthesis of prolylcarboxypeptidase (PrCP) inhibitors to validate PrCP as a potential target for obesity. , 2010, Journal of medicinal chemistry.

[19]  T. Bhardwaj,et al.  Saxagliptin: a new drug for the treatment of type 2 diabetes. , 2010, Mini-Reviews in Medical Chemistry.

[20]  Sujata Sharma,et al.  Structural definition and substrate specificity of the S28 protease family: the crystal structure of human prolylcarboxypeptidase , 2010, BMC Structural Biology.

[21]  Steven J Brown,et al.  Oxime esters as selective, covalent inhibitors of the serine hydrolase retinoblastoma-binding protein 9 (RBBP9). , 2010, Bioorganic & medicinal chemistry letters.

[22]  J. Long,et al.  Characterization of tunable piperidine and piperazine carbamates as inhibitors of endocannabinoid hydrolases. , 2010, Journal of medicinal chemistry.

[23]  B. Cravatt,et al.  Activity-based probes that target functional subclasses of phospholipases in proteomes. , 2010, Journal of the American Chemical Society.

[24]  D. Tarin,et al.  RBBP9: A tumor-associated serine hydrolase activity required for pancreatic neoplasia , 2009, Proceedings of the National Academy of Sciences.

[25]  D. Nomura,et al.  Dual blockade of FAAH and MAGL identifies behavioral processes regulated by endocannabinoid crosstalk in vivo , 2009, Proceedings of the National Academy of Sciences.

[26]  D. Hazuda,et al.  MK-7009, a Potent and Selective Inhibitor of Hepatitis C Virus NS3/4A Protease , 2009, Antimicrobial Agents and Chemotherapy.

[27]  Qian Gao,et al.  Prolylcarboxypeptidase regulates food intake by inactivating alpha-MSH in rodents. , 2009, The Journal of clinical investigation.

[28]  Xinrong Zhu,et al.  Design, synthesis, biological evaluation, and structure-activity relationship (SAR) discussion of dipeptidyl boronate proteasome inhibitors, part I: comprehensive understanding of the SAR of alpha-amino acid boronates. , 2009, Journal of medicinal chemistry.

[29]  R. Stevens,et al.  Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain. , 2009, Chemistry & biology.

[30]  Steven J Brown,et al.  Substrate-Free High-Throughput Screening Identifies Selective Inhibitors for Uncharacterized Enzymes , 2009, Nature Biotechnology.

[31]  J Mallela,et al.  Prolylcarboxypeptidase: a cardioprotective enzyme. , 2009, The international journal of biochemistry & cell biology.

[32]  Sherry L. Niessen,et al.  Selectivity of inhibitors of endocannabinoid biosynthesis evaluated by activity-based protein profiling. , 2008, Bioorganic & medicinal chemistry letters.

[33]  J. Lai,et al.  Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. , 2008, Journal of medicinal chemistry.

[34]  S. Ohta,et al.  Host inactivation of bacterial lipopolysaccharide prevents prolonged tolerance following gram-negative bacterial infection. , 2008, Cell host & microbe.

[35]  Xin Chen,et al.  Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: identification of dipeptide derived leads. , 2008, Bioorganic & medicinal chemistry letters.

[36]  B. Cravatt,et al.  Activity-based protein profiling: from enzyme chemistry to proteomic chemistry. , 2008, Annual review of biochemistry.

[37]  P. Zarrinkar,et al.  High-throughput kinase profiling as a platform for drug discovery , 2008, Nature Reviews Drug Discovery.

[38]  Sum Lam,et al.  Sitagliptin: A Novel Drug for the Treatment of Type 2 Diabetes , 2007, Cardiology in review.

[39]  B. Cravatt,et al.  A functional proteomic strategy to discover inhibitors for uncharacterized hydrolases. , 2007, Journal of the American Chemical Society.

[40]  Ian Collins,et al.  New approaches to molecular cancer therapeutics , 2006, Nature chemical biology.

[41]  B. Cravatt,et al.  Mechanism of carbamate inactivation of FAAH: implications for the design of covalent inhibitors and in vivo functional probes for enzymes. , 2005, Chemistry & biology.

[42]  Y. Hu,et al.  Boro-norleucine as a P1 residue for the design of selective and potent DPP7 inhibitors. , 2005, Bioorganic & medicinal chemistry letters.

[43]  A. Woods,et al.  Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9. , 2005, Diabetes.

[44]  Brent R. Martin,et al.  Mammalian cell–based optimization of the biarsenical-binding tetracysteine motif for improved fluorescence and affinity , 2005, Nature Biotechnology.

[45]  Xia Li,et al.  Lipopolysaccharide deacylation by an endogenous lipase controls innate antibody responses to Gram-negative bacteria , 2005, Nature Immunology.

[46]  Charles M. Rice,et al.  Unravelling hepatitis C virus replication from genome to function , 2005, Nature.

[47]  A. Durand,et al.  Catabolism of intracellular N-terminal acetylated proteins: involvement of acylpeptide hydrolase and acylase. , 2005, Biochimie.

[48]  Andreas Schwienhorst,et al.  Thrombin inhibitors identified by computer-assisted multiparameter design. , 2005, Proceedings of the National Academy of Sciences of the United States of America.

[49]  A. Poso,et al.  Characterization of the sulfhydryl-sensitive site in the enzyme responsible for hydrolysis of 2-arachidonoyl-glycerol in rat cerebellar membranes. , 2005, Chemistry & biology.

[50]  J. Lai,et al.  Autochelation in dipeptide boronic acids: pH-dependent structures and equilibria of Asp-boroPro and His-boroPro by NMR spectroscopy. , 2005, Journal of the American Chemical Society.

[51]  K. Schlemmer,et al.  In vitro and in vivo studies of the novel antithrombotic agent BAY 59‐7939—an oral, direct Factor Xa inhibitor , 2005, Journal of thrombosis and haemostasis : JTH.

[52]  L. Wodicka,et al.  A small molecule–kinase interaction map for clinical kinase inhibitors , 2005, Nature Biotechnology.

[53]  R. Pertwee,et al.  Inhibition of monoacylglycerol lipase and fatty acid amide hydrolase by analogues of 2‐arachidonoylglycerol , 2004, British journal of pharmacology.

[54]  J. Adams.  The development of proteasome inhibitors as anticancer drugs. , 2004, Cancer cell.

[55]  S. Nakanishi,et al.  K579, a slow-binding inhibitor of dipeptidyl peptidase IV, is a long-acting hypoglycemic agent. , 2004, European journal of pharmacology.

[56]  A. Lambeir,et al.  Design, synthesis, and SAR of potent and selective dipeptide-derived inhibitors for dipeptidyl peptidases. , 2003, Journal of medicinal chemistry.

[57]  T. Hughes,et al.  1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties. , 2003, Journal of medicinal chemistry.

[58]  Dale L Boger,et al.  Discovering potent and selective reversible inhibitors of enzymes in complex proteomes , 2003, Nature Biotechnology.

[59]  C. Zechel,et al.  Solid-phase synthesis of thrombin inhibitors. , 2002, Bioorganic & medicinal chemistry letters.

[60]  T. Hughes,et al.  1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties. , 2002, Journal of medicinal chemistry.

[61]  M. Aubert,et al.  Chronic inhibition of circulating dipeptidyl peptidase IV by FE 999011 delays the occurrence of diabetes in male zucker diabetic fatty rats. , 2002, Diabetes.

[62]  S. Ōmura,et al.  Separation of cathepsin A-like enzyme and the proteasome: evidence that lactacystin/beta-lactone is not a specific inhibitor of the proteasome. , 2000, The international journal of biochemistry & cell biology.

[63]  B. Cravatt,et al.  Activity-based protein profiling: the serine hydrolases. , 1999, Proceedings of the National Academy of Sciences of the United States of America.

[64]  M. Gaca,et al.  Inhibitors of chymase as mast cell-stabilizing agents: contribution of chymase in the activation of human mast cells. , 1999, The Journal of pharmacology and experimental therapeutics.

[65]  S. Thorgeirsson,et al.  A retinoblastoma-binding protein that affects cell-cycle control and confers transforming ability , 1998, Nature Genetics.

[66]  S. Schreiber,et al.  Lactacystin, Proteasome Function, and Cell Fate* , 1998, The Journal of Biological Chemistry.

[67]  L. Dick,et al.  Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids. , 1998, Bioorganic & medicinal chemistry letters.

[68]  S. Ōmura,et al.  Lactacystin, a specific inhibitor of the proteasome, inhibits human platelet lysosomal cathepsin A-like enzyme. , 1997, Biochemical and biophysical research communications.

[69]  D. Deutsch,et al.  Methyl arachidonyl fluorophosphonate: a potent irreversible inhibitor of anandamide amidase. , 1997, Biochemical pharmacology.

[70]  M. Vincent,et al.  New prolyl endopeptidase inhibitors: in vitro and in vivo activities of azabicyclo[2.2.2]octane, azabicyclo[2.2.1]heptane, and perhydroindole derivatives. , 1996, Journal of medicinal chemistry.

[71]  Paul D. Jenkins,et al.  2-cyanopyrrolidides as potent, stable inhibitors of dipeptidyl peptidase IV , 1996 .

[72]  S. J. Campbell,et al.  Structure-activity relationships of boronic acid inhibitors of dipeptidyl peptidase IV. 1. Variation of the P2 position of Xaa-boroPro dipeptides. , 1996, Journal of medicinal chemistry.

[73]  H. Sugimoto,et al.  Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-[(5,6-dimethoxy-1-oxoindan-2-yl)methyl]piperidine hydrochloride and related compounds. , 1995, Journal of medicinal chemistry.

[74]  J Li,et al.  Aminoacylpyrrolidine-2-nitriles: potent and stable inhibitors of dipeptidyl-peptidase IV (CD 26). , 1995, Archives of biochemistry and biophysics.

[75]  R F Standaert,et al.  Inhibition of proteasome activities and subunit-specific amino-terminal threonine modification by lactacystin , 1995, Science.

[76]  B. Gallwitz,et al.  Dipeptidyl-peptidase IV hydrolyses gastric inhibitory polypeptide, glucagon-like peptide-1(7-36)amide, peptide histidine methionine and is responsible for their degradation in human serum. , 1993, European journal of biochemistry.

[77]  B. Huber,et al.  Inhibition of dipeptidyl aminopeptidase IV (DP-IV) by Xaa-boroPro dipeptides and use of these inhibitors to examine the role of DP-IV in T-cell function. , 1991, Proceedings of the National Academy of Sciences of the United States of America.

[78]  R. Munford,et al.  Purification of acyloxyacyl hydrolase, a leukocyte enzyme that removes secondary acyl chains from bacterial lipopolysaccharides. , 1989, The Journal of biological chemistry.

[79]  Qian-sheng Yu,et al.  Comparative inhibitory effects of various physostigmine analogs against acetyl- and butyrylcholinesterases. , 1989, The Journal of pharmacology and experimental therapeutics.

[80]  J. Greenspoon,et al.  Oral glucose tolerance test. , 1988, Mayo Clinic proceedings.

[81]  J. Ohsumi,et al.  Identification of a novel class of elastase isozyme, human pancreatic elastase III, by cDNA and genomic gene cloning. , 1988, The Journal of biological chemistry.

[82]  S. Wilk,et al.  Prolyl Endopeptidase: Inhibition In Vivo by N‐Benzyloxycarbonyl‐Prolyl‐Prolinal , 1984, Journal of neurochemistry.

[83]  S. Imaoka,et al.  FOY: [ethyl P-(6-guanidinohexanoyloxy) benzoate] methanesulfonate as a serine proteinase inhibitor. I. Inhibition of thrombin and factor Xa in vitro. , 1980, Thrombosis research.

[84]  R. Goldfarb,et al.  Direct fluorescent assay of urokinase and plasminogen activators of normal and malignant cells: kinetics and inhibitor profiles. , 1978, Proceedings of the National Academy of Sciences of the United States of America.

[85]  J. W. Campbell,et al.  The atomic structure of crystalline porcine pancreatic elastase at 2.5 A resolution: comparisons with the structure of alpha-chymotrypsin. , 1976, Journal of molecular biology.

[86]  T. Aoyagi,et al.  Antipain, a new protease inhibitor isolated from actinomycetes. , 1972, The Journal of antibiotics.

[87]  R. Munford,et al.  Chapter 2: Kill the bacteria...and also their messengers? , 2009, Advances in immunology.

[88]  D. Kelsell,et al.  Human elastase 1: evidence for expression in the skin and the identification of a frequent frameshift polymorphism. , 2000, The Journal of investigative dermatology.

[89]  S. Pehrsson,et al.  Effects of Melagatran, a New Low-molecular-weight Thrombin Inhibitor, on Thrombin and Fibrinolytic Enzymes , 1998, Thrombosis and Haemostasis.

[90]  N. Roome,et al.  Inhibition by Argatroban, a Specific Thrombin Inhibitor, of Platelet Activation by Fibrin Clot-associated Thrombin , 1996, Thrombosis and Haemostasis.

[91]  R. Munford,et al.  Eukaryotic lipopolysaccharide deacylating enzyme. , 1992, Methods in enzymology.

[92]  M. Muramatu,et al.  Inhibitory effects of -guanidino acid esters on trypsin, plasmin, plasma kallikrein and thrombin. , 1971, Biochimica et biophysica acta.