76 articles for thisTarget
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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
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
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
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
Structural and stereochemical requirements of time-dependent inactivators of the interleukin-1β 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
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
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
Cannabidiol Protects Human Skin Keratinocytes from Hydrogen-Peroxide-Induced Oxidative Stress via Modulation of the Caspase-1-IL-1? Axis.
University of Rhode Island
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
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
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