PMID

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Article Title

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Variation of the aryl substituent on the piperazine ring within the 4-(piperazin-1-yl)-2,6-di(pyrrolidin-1-yl)pyrimidine scaffold unveils potent, non-competitive inhibitors of the inflammatory caspases.

Depaul University

Inhibiting the Inflammasome: A Chemical Perspective.

The University of Manchester

Azaphilones from an Acid Mine Extremophile Strain of a Pleurostomophora sp.

Memorial Sloan-Kettering Cancer Center

Electrophilic warhead-based design of compounds preventing NLRP3 inflammasome-dependent pyroptosis.

Universit£

Synthesis of 7-halogenated isatin sulfonamides: nonradioactive counterparts of caspase-3/-7 inhibitor-based potential radiopharmaceuticals for molecular imaging of apoptosis.

Westf£Lische Wilhelms-Universit£T M£Nster

Synthesis of new fluorinated, 2-substituted 5-pyrrolidinylsulfonyl isatin derivatives as caspase-3 and caspase-7 inhibitors: nonradioactive counterparts of putative PET-compatible apoptosis imaging agents.

Westf£Lische Wilhelms-Universit£T M£Nster

Irreversible inhibitors of cysteine proteases.

Dart Neuroscience

Caspase-1 and -3 inhibiting drimane sesquiterpenoids from the extremophilic fungus Penicillium solitum.

University of Montana

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

Protease inhibitors: current status and future prospects.

University of Queensland

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

Maxim Pharmaceuticals

Peptidyl beta-homo-aspartals: specific inhibitors of interleukin-1 beta converting enzyme and its homologues (caspases).

Institute For Drug Research

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

Washington University

Inhibition of interleukin-1beta converting enzyme (ICE or caspase 1) by aspartyl acyloxyalkyl ketones and aspartyl amidooxyalkyl ketones.

Pfizer

Succinic acid amides as P2-P3 replacements for inhibitors of interleukin-1beta converting enzyme (ICE or caspase 1).

Pfizer

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

The University of Queensland

Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB.

National Human Genome Research Institute

 

3-chloro-4-carboxamido-6-arylpyridazines as a non-peptide class of interleukin-1β converting enzyme inhibitor

TBA

 

Structure-based design of non-peptidic pyridone aldehydes as inhibitors of interleukin-1β converting enzyme

TBA

 

PYRIDONE-BASED PEPTIDOMIMETIC INHIBITORS OF INTERLEUKIN-1β-CONVERTING ENZYME (ICE)

TBA

 

Structural and stereochemical requirements of time-dependent inactivators of the interleukin-1β converting enzyme

TBA

 

Inhibition of interleukin-1β converting enzyme by N-acyl-aspartyl aryloxymethyl ketones

TBA

 

Inhibition of interleukin-1β converting enzyme by N-Acyl-aspartic acid ketones

TBA

 

The synthesis and evaluation of peptidyl aspartyl aldehydes as inhibitors of ice.

TBA

 

Activated ketones as potent reversible inhibitors of interleukin-Iβ converting enzyme

TBA

 

Synthesis of a peptidyl 2,2-difluoro-4-phenylbutyl ketone and its evaluation as an inhibitor of interleukin-1β converting enzyme.

TBA

 

Phenylalkyl ketones as potent reversible inhibitors of interleukin-1β converting enzyme

TBA

 

Synthesis of a potent, reversible inhibitor of interleukin-1β converting enzyme

TBA

Fluorinated isatin derivatives. Part 2. New N-substituted 5-pyrrolidinylsulfonyl isatins as potential tools for molecular imaging of caspases in apoptosis.

Westfalische Wilhelms-Universitat

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

Imperial College

Recent developments in fragment-based drug discovery.

Astex Therapeutics

The berkeleyamides, amides from the acid lake fungus Penicillum rubrum.

Montana Tech of The University of Montana

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

Design, synthesis and biological evaluation of 1,5-disubstituted ?-amino tetrazole derivatives as non-covalent inflammasome-caspase-1 complex inhibitors with potential application against immune and inflammatory disorders.

National Research Council (Cnr)

Tethering identifies fragment that yields potent inhibitors of human caspase-1.

Sunesis 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

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

Merck Frosst Centre For Therapeutic Research

Discovery of a Series of Pyrimidine Carboxamides as Inhibitors of Vanin-1.

Pfizer

Cannabidiol Protects Human Skin Keratinocytes from Hydrogen-Peroxide-Induced Oxidative Stress via Modulation of the Caspase-1-IL-1? Axis.

University of Rhode Island

The design and synthesis of sulfonamides as caspase-1 inhibitors.

Pfizer

Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor.

Senju Pharmaceutical

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

A practical synthesis of (S) 3-tert-butoxycarbonylamino-2-oxo-2,3,4,5-tetrahydro-1,5-benzodiazepine-1-acetic acid methyl ester as a conformationally restricted dipeptido-mimetic for caspase-1 (ICE) inhibitors.

Vertex Pharmaceuticals

Caspases as targets for anti-inflammatory and anti-apoptotic drug discovery.

Basf Bioresearch

Rapid optimization of an ICE inhibitor synthesis using multiple reaction conditions in a parallel array.

Warner-Lambert

Novel cytokine release inhibitors. Part I: Triterpenes.

RhóNe-Poulenc Rorer Central Research

Peptidomimetic aminomethylene ketone inhibitors of interleukin-1 beta-converting enzyme (ICE).

Ferring Research Institute

Pyridazinodiazepines as a high-affinity, P2-P3 peptidomimetic class of interleukin-1 beta-converting enzyme inhibitor.

Sanofi Winthrop

Synthesis and antitumor activities of 1,2,3-triazines and their benzo- and heterofused derivatives.

Universit£

New Caspase-1 inhibitor by scaffold hopping into bio-inspired 3D-fragment space.

Edelris

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

Nestl�

Molecular cloning and characterization of a new receptor for galanin.

Merck Research Laboratories

Design of HIV-1 protease inhibitors with pyrrolidinones and oxazolidinones as novel P1'-ligands to enhance backbone-binding interactions with protease: synthesis, biological evaluation, and protein-ligand X-ray studies.

Purdue University

Apogossypol derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.

Burnham Institute For Medical Research

The molecular interactions of buspirone analogues with the serotonin transporter.

National Medicines Institute

Discovery of selective aminothiazole aurora kinase inhibitors.

Novartis

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

Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors

Shanghaitech University

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

Bristol-Myers Squibb