50 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Optimization of peptidomimetic boronates bearing a P3 bicyclic scaffold as proteasome inhibitors.
Universit£
Identification of a new series of amides as non-covalent proteasome inhibitors.
Universit£
Synthesis and biological evaluation of direct thrombin inhibitors bearing 4-(piperidin-1-yl)pyridine at the P1 position with potent anticoagulant activity.
University Of Bari &Quot;Aldo Moro&Quot
Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold.
Virginia Commonwealth University
Discovery of 1-(2-aminomethylphenyl)-3-trifluoromethyl-N- [3-fluoro-2'-(aminosulfonyl)[1,1'-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a potent, selective, and orally bioavailable factor Xa inhibitor(1).
Pharmaceutical Research Institute
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
Northwestern University
A common mechanism underlying promiscuous inhibitors from virtual and high-throughput screening.
Northwestern University
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 alpha-keto heterocycles as novel inhibitors of human chymase.
Welfide
Design and synthesis of thrombin inhibitors: analogues of MD-805 with reduced stereogenicity and improved potency.
Novartis Horsham Research Centre
Alpha-diketone and alpha-keto ester derivatives of N-protected amino acids and peptides as novel inhibitors of cysteine and serine proteinases.
Merrell Dow Research Institute
Design, synthesis, crystal structures, and antimicrobial activity of sulfonamide boronic acids asß-lactamase inhibitors.
University Of California San Francisco
Molassamide, a depsipeptide serine protease inhibitor from the marine cyanobacterium Dichothrix utahensis.
Smithsonian Marine Station At Ft. Pierce
1,3-Oxazino[4,5-b]indole-2,4-(1H,9H)-diones and 5,6-dimethylpyrrolo-[2,3-d]-1,3-oxazin-2,4-(1H,7H)-diones as serine protease inhi...
TBA
Engineering of cyclic peptides with novel inhibiting properties to differentiate two serine proteases, chymotrypsin and subtilisin Carlsberg
TBA
Boric acid effect ont he hydrolysis of 4-nitrophenyl 2,3-dihydroxybenzoate: mimic of borate inhibition of serine proteases
TBA
MDL 74147, a novel selective and soluble inhibitor of human renin. Synthesis, structure-activity relationship, species and protease selectivities.
TBA
Borinic acid inhibitors as probes of the factors involved in binding at the active sites of subtilisin carlsberg and α-chymotrypsin
TBA
P1 and P3 optimization of novel bicycloproline P2 bearing tetrapeptidyl alpha-ketoamide based HCV protease inhibitors.
Eli Lilly
Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor.
Senju Pharmaceutical
Alpha-ketoester-based photobiological switches: synthesis, peptide chain extension and assay against alpha-chymotrypsin.
University Of Canterbury
1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma.
Shionogi
Mass spectrometry reveals elastase inhibitors from the reactive centre loop of alpha1-antitrypsin.
The Oxford Centre For Molecular Sciences
Structure-activity relationship studies of chloromethyl ketone derivatives for selective human chymase inhibitors.
Kyoto Pharmaceutical University
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
Design and synthesis of monocyclic beta-lactams as mechanism-based inhibitors of human cytomegalovirus protease.
Glaxo Wellcome Research And Development
Peptidyl human heart chymase inhibitors. 1. Synthesis and inhibitory activity of difluoromethylene ketone derivatives bearing P' binding subsites.
Green Cross Research Laboratories
Structure-based enhancement of boronic acid-based inhibitors of AmpC beta-lactamase.
Northwestern University Medical School
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
Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position.
Merck Research Laboratories
beta-Lactam derivatives as inhibitors of human cytomegalovirus protease.
Boehringer Ingelheim (Canada)
Substituted 3-(phenylsulfonyl)-1-phenylimidazolidine-2,4-dione derivatives as novel nonpeptide inhibitors of human heart chymase.
Suntory
Esters and amides of 6-(chloromethyl)-2-oxo-2H-1-benzopyran-3-carboxylic acid as inhibitors of alpha-chymotrypsin: significance of the"aromatic" nature of the novel ester-type coumarin for strong inhibitory activity.
Université
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
Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters.
Merck Sharp And Dohme Research Laboratories
O'-(epoxyalkyl)tyrosines and (epoxyalkyl)phenylalanine as irreversible inactivators of serine proteases: synthesis and inhibition mechanism.
State University
Effect of conformational mobility and hydrogen-bonding interactions on the selectivity of some guanidinoaryl-substituted mechanism-based inhibitors of trypsin-like serine proteases.
University Of Illinois