The pharmacological landscape and therapeutic potential of serine hydrolases

Fatty Acid Amide Hydrolase Inhibitors – Progress and Potential

(2012) Ish K. Khanna et al.   CNS & Neurological Disorders-Drug Targets

Carbapenems: Past, Present, and Future

(2011) Krisztina M. Papp-Wallace et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Discovery of benzimidazole pyrrolidinyl amides as prolylcarboxypeptidase inhibitors

(2011) Hong C. Shen et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The Metabolic Serine Hydrolases and Their Functions in Mammalian Physiology and Disease

(2011) Jonathan Z. Long et al.   CHEMICAL REVIEWS

A Potent and Selective Inhibitor of KIAA1363/AADACL1 that Impairs Prostate Cancer Pathogenesis

(2011) Jae Won Chang et al.   CHEMISTRY & BIOLOGY

Monoacylglycerol Lipase Exerts Dual Control over Endocannabinoid and Fatty Acid Pathways to Support Prostate Cancer

(2011) Daniel K. Nomura et al.   CHEMISTRY & BIOLOGY

Low molecular weight inhibitors of Prolyl Oligopeptidase: a review of compounds patented from 2003 to 2010

(2011) Abraham López et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Translational research on prolyl oligopeptidase inhibitors: the long road ahead

(2011) Anne-Marie Lambeir   EXPERT OPINION ON THERAPEUTIC PATENTS

Discovery and Optimization of Sulfonyl Acrylonitriles as Selective, Covalent Inhibitors of Protein Phosphatase Methylesterase-1

(2011) Daniel A. Bachovchin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Too many roads not taken

(2011) Aled M. Edwards et al.   NATURE

Therapeutics: New drugs hit the target

(2011) Jana Schlütter   NATURE

Click-generated triazole ureas as ultrapotent in vivo–active serine hydrolase inhibitors

(2011) Alexander Adibekian et al.   Nature Chemical Biology

The resurgence of covalent drugs

(2011) Juswinder Singh et al.   NATURE REVIEWS DRUG DISCOVERY

The HtrA-Like Serine Protease PepD Interacts with and Modulates the Mycobacterium tuberculosis 35-kDa Antigen Outer Envelope Protein

(2011) Mark J. White et al.   PLoS One

Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors

(2011) D. A. Bachovchin et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Adipose Triglyceride Lipase Contributes to Cancer-Associated Cachexia

(2011) S. K. Das et al.   SCIENCE

Endocannabinoid Hydrolysis Generates Brain Prostaglandins That Promote Neuroinflammation

(2011) D. K. Nomura et al.   SCIENCE

Novel Oral Factor Xa and Thrombin Inhibitors in the Management of Thromboembolism

(2010) Bengt I. Eriksson et al.   Annual Review of Medicine

Dabigatran: An Oral Novel Potent Reversible Nonpeptide Inhibitor of Thrombin

(2010) Wolfgang G. Eisert et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Oxime esters as selective, covalent inhibitors of the serine hydrolase retinoblastoma-binding protein 9 (RBBP9)

(2010) Daniel A. Bachovchin et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Loss of TGH/Ces3 in Mice Decreases Blood Lipids, Improves Glucose Tolerance, and Increases Energy Expenditure

(2010) Enhui Wei et al.   Cell Metabolism

A fluopol-ABPP HTS assay to identify PAD inhibitors

(2010) Bryan Knuckley et al.   CHEMICAL COMMUNICATIONS

The future of the β-lactams

(2010) Leticia I Llarrull et al.   CURRENT OPINION IN MICROBIOLOGY

Recent Advances in Targeting Viral Proteases for the Discovery of Novel Antivirals

(2010) Holger Steuber et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Strategies for discovering and derisking covalent, irreversible enzyme inhibitors

(2010) Douglas S Johnson et al.   Future Medicinal Chemistry

Activity-based Proteomics of Enzyme Superfamilies: Serine Hydrolases as a Case Study

(2010) Gabriel M. Simon et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Design and Synthesis of Prolylcarboxypeptidase (PrCP) Inhibitors To Validate PrCP As A Potential Target for Obesity

(2010) Changyou Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Regulation of protein phosphatase 2A methylation by LCMT1 and PME-1 plays a critical role in differentiation of neuroblastoma cells

(2010) Jean-Marie Sontag et al.   JOURNAL OF NEUROCHEMISTRY

Recommended nomenclature for five mammalian carboxylesterase gene families: human, mouse, and rat genes and proteins

(2010) Roger S. Holmes et al.   MAMMALIAN GENOME

Quantitative reactivity profiling predicts functional cysteines in proteomes

(2010) Eranthie Weerapana et al.   NATURE

Selective irreversible inhibition of a protease by targeting a noncatalytic cysteine

(2010) Margit Hagel et al.   Nature Chemical Biology

The discovery and development of rivaroxaban, an oral, direct factor Xa inhibitor

(2010) Elisabeth Perzborn et al.   NATURE REVIEWS DRUG DISCOVERY

Superfamily-wide portrait of serine hydrolase inhibition achieved by library-versus-library screening

(2010) D. A. Bachovchin et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural basis of substrate specificity in the serine proteases

(2010) John J. Perona et al.   PROTEIN SCIENCE

Suppression of Antitumor Immunity by Stromal Cells Expressing Fibroblast Activation Protein- 

(2010) M. Kraman et al.   SCIENCE

Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor

(2010) Douglas S. Johnson et al.   ACS Medicinal Chemistry Letters

Peptidomics of Prolyl Endopeptidase in the Central Nervous System

(2009) Whitney M. Nolte et al.   BIOCHEMISTRY

HCV-NS3 inhibitors: Determination of their kinetic parameters and mechanism

(2009) María Victoria Flores et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

PME-1 Protects Extracellular Signal-Regulated Kinase Pathway Activity from Protein Phosphatase 2A-Mediated Inactivation in Human Malignant Glioma

(2009) P. Puustinen et al.   CANCER RESEARCH

Monoacylglycerol Lipase Regulates a Fatty Acid Network that Promotes Cancer Pathogenesis

(2009) Daniel K. Nomura et al.   CELL

Characterization of Monoacylglycerol Lipase Inhibition Reveals Differences in Central and Peripheral Endocannabinoid Metabolism

(2009) Jonathan Z. Long et al.   CHEMISTRY & BIOLOGY

Discovery and Characterization of a Highly Selective FAAH Inhibitor that Reduces Inflammatory Pain

(2009) Kay Ahn et al.   CHEMISTRY & BIOLOGY

Differential activity-based gel electrophoresis for comparative analysis of lipolytic and esterolytic activities

(2009) Maria Morak et al.   JOURNAL OF LIPID RESEARCH

Covalent Modifiers: An Orthogonal Approach to Drug Design

(2009) Michele H. Potashman et al.   JOURNAL OF MEDICINAL CHEMISTRY

Blockade of Endocannabinoid-Degrading Enzymes Attenuates Neuropathic Pain

(2009) S. G. Kinsey et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Diversity of Serine Hydrolase Activities of Unchallenged andBotrytis-infectedArabidopsis thaliana

(2009) Farnusch Kaschani et al.   MOLECULAR & CELLULAR PROTEOMICS

Identification of selective inhibitors of uncharacterized enzymes by high-throughput screening with fluorescent activity-based probes

(2009) Daniel A Bachovchin et al.   NATURE BIOTECHNOLOGY

Dabigatran versus Warfarin in the Treatment of Acute Venous Thromboembolism

(2009) Sam Schulman et al.   NEW ENGLAND JOURNAL OF MEDICINE

RBBP9: A tumor-associated serine hydrolase activity required for pancreatic neoplasia

(2009) D. J. Shields et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

DIALIGN-TX: greedy and progressive approaches for segment-based multiple sequence alignment

(2008) Amarendran R Subramanian et al.   Algorithms for Molecular Biology

Enantioselective Nucleophilic Catalysis: The Synthesis of Aza-β-Lactams through [2+2] Cycloadditions of Ketenes with Azo Compounds

(2008) Jacob M. Berlin et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Activity-Based Protein Profiling: From Enzyme Chemistry to Proteomic Chemistry

(2008) Benjamin F. Cravatt et al.   Annual Review of Biochemistry

Fatty Acid Amide Hydrolase Inhibition Heightens Anandamide Signaling Without Producing Reinforcing Effects in Primates

(2008) Zuzana Justinova et al.   BIOLOGICAL PSYCHIATRY

Selectivity of inhibitors of endocannabinoid biosynthesis evaluated by activity-based protein profiling

(2008) Heather S. Hoover et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of potent, selective sulfonylfuran urea endothelial lipase inhibitors

(2008) Krista B. Goodman et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Prolylcarboxypeptidase: A cardioprotective enzyme

(2008) J. Mallela et al.   INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY

Adipose triglyceride lipase and the lipolytic catabolism of cellular fat stores

(2008) Rudolf Zechner et al.   JOURNAL OF LIPID RESEARCH

Mammalian patatin domain containing proteins: a family with diverse lipolytic activities involved in multiple biological functions

(2008) Petra C. Kienesberger et al.   JOURNAL OF LIPID RESEARCH

Optimization of Activity-Based Probes for Proteomic Profiling of Histone Deacetylase Complexes

(2008) Cleo M. Salisbury et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

On The Edge of Validation – Cancer Protease Fibroblast Activation Protein

(2008) Beni Wolf et al.   MINI-REVIEWS IN MEDICINAL CHEMISTRY

Triggers, targets and treatments for thrombosis

(2008) Nigel Mackman   NATURE

Disparate proteome reactivity profiles of carbon electrophiles

(2008) Eranthie Weerapana et al.   Nature Chemical Biology

Selective blockade of 2-arachidonoylglycerol hydrolysis produces cannabinoid behavioral effects

(2008) Jonathan Z Long et al.   Nature Chemical Biology

Inhibition of lipoprotein-associated phospholipase A2 reduces complex coronary atherosclerotic plaque development

(2008) Robert L Wilensky et al.   NATURE MEDICINE

Involvement of DPP-IV catalytic residues in enzyme-saxagliptin complex formation

(2008) William J. Metzler et al.   PROTEIN SCIENCE