105 articles for thisTarget
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Protective effect of novel substituted nicotine hydrazide analogues against hypoxic brain injury in neonatal rats via inhibition of caspase.
The Fifth Affiliated Hospital of Guangzhou Medical University
Design, synthesis, and structure-activity relationships of novel benzothiazole derivatives bearing the ortho-hydroxy N-carbamoylhydrazone moiety as potent antitumor agents.
Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University) Ministry of Education
In vitro induction of apoptosis by isosclerone from marine-derived fungus Aspergillus fumigatus.
Pukyong National University
Synthesis and evaluation of N-acyl-substituted 1,2-benzisothiazol-3-one derivatives as caspase-3 inhibitors.
TBA
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
1,2-benzisothiazol-3-one derivatives as a novel class of small-molecule caspase-3 inhibitors.
Tianjin University of Science and Technology
Influence of 4- or 5-substituents on the pyrrolidine ring of 5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin derivatives on their inhibitory activities towards caspases-3 and -7.
Westf£Lische Wilhelms-Universit£T M£Nster
Design, synthesis and evaluation of 1,2-benzisothiazol-3-one derivatives as potent caspase-3 inhibitors.
Nankai University
Synthesis, 18F-radiolabeling, and in vivo biodistribution studies of N-fluorohydroxybutyl isatin sulfonamides using positron emission tomography.
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
New description of protein-ligand interactions using a spherical self-organizing map.
Chugai Pharmaceutical
Discovery and structure-activity relationship of potent and selective covalent inhibitors of transglutaminase 2 for Huntington's disease.
Evotec (Uk)
A novel class of small-molecule caspase-3 inhibitors prepared by multicomponent reactions.
Southern Medical University
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
Exploiting differences in caspase-2 and -3 S2 subsites for selectivity: structure-based design, solid-phase synthesis and in vitro activity of novel substrate-based caspase-2 inhibitors.
Chdi Management
Aspartic vinyl sulfones: inhibitors of a caspase-3-dependent pathway.
University of Lisbon
Synthesis and evaluation of isatin analogs as caspase-3 inhibitors: introduction of a hydrophilic group increases potency in a whole cell assay.
Washington University
Synthesis and evaluation of vinyl sulfones as caspase-3 inhibitors. A structure-activity study.
University of Lisbon
Mechanisms, biology and inhibitors of deubiquitinating enzymes.
Institute For Bio-Medical Research
Design, synthesis, and discovery of novel non-peptide inhibitor of Caspase-3 using ligand based and structure based virtual screening approach.
Osmania University College For Women
Fluorinated isatin derivatives. Part 2. New N-substituted 5-pyrrolidinylsulfonyl isatins as potential tools for molecular imaging of caspases in apoptosis.
Westfalische Wilhelms-Universitat
Fluorinated isatin derivatives. Part 1: synthesis of new N-substituted (S)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatins as potent caspase-3 and -7 inhibitors.
WestfäLische Wilhelms-UniversitäT
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
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
Discovery and Crystallographic Studies of Nonpeptidic Piperazine Derivatives as Covalent SARS-CoV-2 Main Protease Inhibitors.
Shandong University
Synthesis and evaluation of novel 8,6-fused bicyclic peptidomimetic compounds as interleukin-1beta converting enzyme inhibitors.
Procter & Gamble Pharmaceuticals
Discovery and structure-activity relationship of 3-aryl-5-aryl-1,2,4-oxadiazoles as a new series of apoptosis inducers and potential anticancer agents.
Maxim Pharmaceuticals
Synthesis and evaluation of tricyclic pyrrolopyrimidinones as dipeptide mimetics: inhibition of interleukin-1beta-converting enzyme.
Procter & Gamble Pharmaceuticals
Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP.
Merck Research Laboratories
Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: peptidomimetic replacement of the P2 alpha-amino acid by a alpha-hydroxy acid.
Maxim Pharmaceuticals
Discovery and Crystallographic Studies of Trisubstituted Piperazine Derivatives as Non-Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity and Low Toxicity.
Shandong University
Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors.
Merck Frosst Centre For Therapeutic Research
Discovery of a Series of 7-Azaindoles as Potent and Highly Selective CDK9 Inhibitors for Transient Target Engagement.
Astrazeneca
Design and synthesis of a potent and selective peptidomimetic inhibitor of caspase-3.
University of Illinois At Chicago
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
Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis.
Galapagos
Structure-activity relationships within a series of caspase inhibitors: effect of leaving group modifications.
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
Quinolone hybrids and their anti-cancer activities: An overview.
Qilu University of Technology (Shandong Academy of Sciences)
Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors.
Roche Pharma Research and Early Development
Caspases as targets for anti-inflammatory and anti-apoptotic drug discovery.
Basf Bioresearch
Synthesis and activity evaluation of the cyclic dipeptides arylidene N-alkoxydiketopiperazines.
Hebei University of Science & Technology
Conformationally constrained inhibitors of caspase-1 (interleukin-1 beta converting enzyme) and of the human CED-3 homologue caspase-3 (CPP32, apopain).
Idun Pharmaceuticals
Development of a potent and selective cell penetrant Legumain inhibitor.
Queen'S University Belfast
Secobatzellines A and B, two new enzyme inhibitors from a deep-water Caribbean sponge of the genus Batzella.
Harbor Branch Oceanographic Institution
Discorhabdin P, a new enzyme inhibitor from a deep-water Caribbean sponge of the genus Batzella.
Harbor Branch Oceanographic Institution
Synthesis and antitumor activities of 1,2,3-triazines and their benzo- and heterofused derivatives.
Universit£
Structure-activity relationship study of a series of caspase inhibitors containing ?-amino acid moiety for treatment of cholestatic liver disease.
Wuxi Apptec (Shanghai)
Rational Drug Design of Topically Administered Caspase 1 Inhibitors for the Treatment of Inflammatory Acne.
Nestl�
Chemical Approaches to Intervening in Ubiquitin Specific Protease 7 (USP7) Function for Oncology and Immune Oncology Therapies.
Progenra
Blockade of Asparagine Endopeptidase Inhibits Cancer Metastasis.
Emory Chemical Biology Discovery Center Emory University School of Medicine Atlanta
In vitro characterization of [3H]MethoxyPyEP, an mGluR5 selective radioligand.
Merck Research Laboratories
The in vitro pharmacology of the beta-adrenergic receptor pet ligand (s)-fluorocarazolol reveals high affinity for cloned beta-adrenergic receptors and moderate affinity for the human 5-HT1A receptor.
Case Western Reserve University
Molecular cloning and characterization of a new receptor for galanin.
Merck Research Laboratories
Virtual screening to successfully identify novel janus kinase 3 inhibitors: a sequential focused screening approach.
Johnson & Johnson Pharmaceutical
The molecular interactions of buspirone analogues with the serotonin transporter.
National Medicines Institute
Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors.
The Scripps Research Institute
Structure-based virtual screening and biological evaluation of Mycobacterium tuberculosis adenosine 5'-phosphosulfate reductase inhibitors.
The Scripps Research 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
Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase.
Glaxosmithkline
Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP.
Merck Research Laboratories
Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors
Shanghaitech University