42 articles for thisTarget
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Article Title
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Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.
Celera Genomics
Synthesis and evaluation of silanediols as highly selective uncompetitive inhibitors of human neutrophil elastase.
Aarhus University
N-Acyl and N-sulfonyloxazolidine-2,4-diones are pseudo-irreversible inhibitors of serine proteases.
University Of Lisbon
Natural polyprenylated benzophenones inhibiting cysteine and serine proteases.
Federal University Of Alfenas
Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.
Merck Research Laboratories
Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer.
Cephalon
Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor (GW475151).
Gsk
Synthesis, structure-activity relationships, and pharmacokinetic profiles of nonpeptidic difluoromethylene ketones as novel inhibitors of human chymase.
Welfide
Synthesis, structure-activity relationships, and pharmacokinetic profiles of nonpeptidic alpha-keto heterocycles as novel inhibitors of human chymase.
Welfide
Novel anthraquinone inhibitors of human leukocyte elastase and cathepsin G.
Georgia Institute Of Technology
Benzimidazolone as potent chymase inhibitor: modulation of reactive metabolite formation in the hydrophobic (P1) region.
Boehringer Ingelheim Pharmaceuticals
Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.
Aristotle University Of Thessaloniki
Phage-encoded combinatorial chemical libraries based on bicyclic peptides.
Laboratory Of Molecular Biology, Medical Research Council
Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif.
Johnson & Johnson Pharmaceutical Research And Development
Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C.
Merck Frosst Canada
Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB.
National Human Genome Research Institute
Introduction of non-natural amino acid residues into the substrate-specific P1 position of trypsin inhibitor SFTI-1 yields potent chymotrypsin and cathepsin G inhibitors.
University Of Gda£?Sk
Synthesis and elastase-inhibiting activity of 2-pyridinyl-isothiazol-3(2H)-one 1,1-dioxides.
University Of Leipzig
Development of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones as orally active human chymase inhibitors.
Daiichi Asubio Pharma
Identification of 6-substituted 4-arylsulfonyl-1,4-diazepane-2,5-diones as a novel scaffold for human chymase inhibitors.
Daiichi Asubio Pharma
Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase.
Johnson & Johnson Pharmaceutical Research And Development
Inhibitors of serine proteases as potential therapeutic agents: the road from thrombin to tryptase to cathepsin G.
Johnson & Johnson Pharmaceutical Research & Development
Structure-activity relationship of benzo[b]thiophene-2-sulfonamide derivatives as novel human chymase inhibitors.
Toa Eiyo
1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma.
Shionogi
Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors.
Shionogi
Structure-activity relationship studies of chloromethyl ketone derivatives for selective human chymase inhibitors.
Kyoto Pharmaceutical University
Symmetrical anhydride-type serine protease inhibitors: structure-activity relationship studies of human chymase inhibitors.
Nippon Steel
N-[2,2-dimethyl-3-(N-(4-cyanobenzoyl)amino)nonanoyl]-L-phenylalanine ethyl ester as a stable ester-type inhibitor of chymotrypsin-like serine proteases: structural requirements for potent inhibition of alpha-chymotrypsin.
Nippon Steel
Syntheses of trans-5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles and trans-5-oxo-hexahydro-furo[3,2-b]pyrroles (pyrrolidine trans-lactams and trans-lactones): new pharmacophores for elastase inhibition.
Glaxowellcome Medicines Research Centre
Orally active trifluoromethyl ketone inhibitors of human leukocyte elastase.
Zeneca Pharmaceuticals
Anionic- and lipophilic-mediated surface binding inhibitors of human leukocyte elastase.
RhôNe-Poulenc Rorer
Substituted 3-(phenylsulfonyl)-1-phenylimidazolidine-2,4-dione derivatives as novel nonpeptide inhibitors of human heart chymase.
Suntory
Non-peptidic inhibitors of human leukocyte elastase. 4. Design, synthesis, and in vitro and in vivo activity of a series of beta-carbolinone-containing trifluoromethyl ketones.
Zeneca Pharmaceuticals
Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin.
Thrombosis Research Institute
Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 3. In vitro and in vivo potency of a series of peptidyl alpha-ketobenzoxazoles.
Zeneca Pharmaceuticals