PMID

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Article Title

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Development of novel benzomorpholine class of diacylglycerol acyltransferase I inhibitors.

Merck Research Laboratories

Irreversible inhibitors of cysteine proteases.

Dart Neuroscience

Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.

University of Florida

Synthesis and evaluation of thiazepines as interleukin-1beta converting enzyme (ICE) inhibitors.

Procter and Gamble Pharmaceuticals

Discovery of novel conformationally restricted diazocan peptidomimetics as inhibitors of interleukin-1beta synthesis.

Procter & Gamble Pharmaceuticals

Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid.

Maxim Pharmaceuticals

Synthesis and evaluation of isatin analogs as caspase-3 inhibitors: introduction of a hydrophilic group increases potency in a whole cell assay.

Washington University

Noncovalent tripeptidyl benzyl- and cyclohexyl-amine inhibitors of the cysteine protease caspase-1.

The University of Queensland

Design, synthesis, and biological characterization of a caspase 3/7 selective isatin labeled with 2-[18F]fluoroethylazide.

Imperial College

Structure-based discovery of a novel non-peptidic small molecular inhibitor of caspase-3.

Tokyo University of Science

Planktocyclin, a cyclooctapeptide protease inhibitor produced by the freshwater cyanobacterium Planktothrix rubescens.

University of ZüRich

Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: peptidomimetic replacement of the P(2) amino acid by 2-aminoaryl acids and other non-natural amino acids.

Epicept

Isatin sulfonamide analogs containing a Michael addition acceptor: a new class of caspase 3/7 inhibitors.

Washington University

Solid-phase analogue synthesis of caspase-3 inhibitors via palladium-catalyzed amination of 3-bromopyrazinones.

Merck Frosst Centre For Therapeutic Research

Synthesis of novel caspase inhibitors for characterization of the active caspase proteome in vitro and in vivo.

University of Edinburgh

5-pyrrolidinylsulfonyl isatins as a potential tool for the molecular imaging of caspases in apoptosis.

University Hospital of The WestfäLische Wilhelms-UniversitäT

Synthesis and evaluation of unsaturated caprolactams as interleukin-1beta converting enzyme (ICE) inhibitors.

Procter & Gamble Pharmaceuticals

Synthesis, radiolabeling, and in vivo evaluation of an 18F-labeled isatin analog for imaging caspase-3 activation in apoptosis.

Washington University

Synthesis and evaluation of novel 1-(2-acylhydrazinocarbonyl)-cycloalkyl carboxamides as interleukin-1beta converting enzyme (ICE) inhibitors.

Procter & Gamble Pharmaceuticals

Synthesis and evaluation of novel 8,6-fused bicyclic peptidomimetic compounds as interleukin-1beta converting enzyme inhibitors.

Procter & Gamble Pharmaceuticals

Synthesis and evaluation of tricyclic pyrrolopyrimidinones as dipeptide mimetics: inhibition of interleukin-1beta-converting enzyme.

Procter & Gamble Pharmaceuticals

Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: peptidomimetic replacement of the P2 alpha-amino acid by a alpha-hydroxy acid.

Maxim Pharmaceuticals

Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors.

Merck Frosst Centre For Therapeutic Research

Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: SAR of the N-protecting group.

Maxim Pharmaceuticals

Oxamyl dipeptide caspase inhibitors developed for the treatment of stroke.

Idun Pharmaceuticals

Acyl dipeptides as reversible caspase inhibitors. Part 2: further optimization.

Idun Pharmaceuticals

Acyl dipeptides as reversible caspase inhibitors. Part 1: initial lead optimization.

Idun Pharmaceuticals

Discovery of potent, selective human granzyme B inhibitors that inhibit CTL mediated apoptosis.

Merck Research Laboratories

Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors.

Roche Pharma Research and Early Development

Development of a potent and selective cell penetrant Legumain inhibitor.

Queen'S University Belfast

Rational Drug Design of Topically Administered Caspase 1 Inhibitors for the Treatment of Inflammatory Acne.

Nestl�

Blockade of Asparagine Endopeptidase Inhibits Cancer Metastasis.

Emory Chemical Biology Discovery Center Emory University School of Medicine Atlanta

Molecular cloning and characterization of a new receptor for galanin.

Merck Research Laboratories

The molecular interactions of buspirone analogues with the serotonin transporter.

National Medicines Institute

Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates: a crystallographic and computational investigation.

National Taiwan University

Probing the elusive catalytic activity of vertebrate class IIa histone deacetylases.

Irbm/Merck Research Laboratories

Discovery of 3,3'-(2,4-diaminopteridine-6,7-diyl)diphenol as an isozyme-selective inhibitor of PI3K for the treatment of ischemia reperfusion injury associated with myocardial infarction.

Targegen

The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer .

Piramed Pharma

Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3.

Bristol-Myers Squibb