80 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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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.
University of Turin
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 α-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
Oxamyl dipeptide caspase inhibitors developed for the treatment of stroke.
Idun Pharmaceuticals
Cannabidiol Protects Human Skin Keratinocytes from Hydrogen-Peroxide-Induced Oxidative Stress via Modulation of the Caspase-1-IL-1β Axis.
University of Rhode Island
Structure-activity relationships within a series of caspase inhibitors: effect of leaving group modifications.
Idun Pharmaceuticals
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
Conformationally constrained inhibitors of caspase-1 (interleukin-1 beta converting enzyme) and of the human CED-3 homologue caspase-3 (CPP32, apopain).
Idun Pharmaceuticals
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�
3-substituted 5-amino-6H-thiazolo[4,5-d]pyrimidine-2,7-dione compounds for the treatment and prophylaxis of virus infection
Hoffmann-La Roche
Evolution of Src Homology 2 (SH2) Domain to Recognize Sulfotyrosine.
University of Nebraska-Lincoln
N-[9-(ortho-fluorobenzyl)-2-phenyl-8-azapurin-6-yl]-amides as potent and selective ligands for A1 adenosine receptors.
University of Pisa
Novel amidino-substituted benzimidazoles: synthesis of compounds and inhibition of dipeptidyl peptidase III.
The Josip Juraj Strossmayer University
Synthesis and biological evaluation of phenolic Mannich bases of benzaldehyde and (thio)semicarbazone derivatives against the cysteine protease falcipain-2 and a chloroquine resistant strain of Plasmodium falciparum.
University of Cape Town
Novel Indolocarbazole protein kinase C inhibitors with improved biochemical and physicochemical properties.
Tumor Biology Center
4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.
Dupont Pharmaceuticals