The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
24946214 |
24 |
Optimization of peptidomimetic boronates bearing a P3 bicyclic scaffold as proteasome inhibitors. |
Universit£ |
24561716 |
18 |
Identification of a new series of amides as non-covalent proteasome inhibitors. |
Universit£ |
24102612 |
105 |
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 |
22770607 |
54 |
Potent direct inhibitors of factor Xa based on the tetrahydroisoquinoline scaffold. |
Virginia Commonwealth University |
14640539 |
112 |
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 |
14521410 |
36 |
Identification and prediction of promiscuous aggregating inhibitors among known drugs. |
Northwestern University |
11931626 |
124 |
A common mechanism underlying promiscuous inhibitors from virtual and high-throughput screening. |
Northwestern University |
12190311 |
37 |
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 |
11312927 |
64 |
Synthesis, structure-activity relationships, and pharmacokinetic profiles of nonpeptidic alpha-keto heterocycles as novel inhibitors of human chymase. |
Welfide |
10579821 |
51 |
Design and synthesis of thrombin inhibitors: analogues of MD-805 with reduced stereogenicity and improved potency. |
Novartis Horsham Research Centre |
2296008 |
13 |
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 |
| 24 |
L-373,890, An achiral, noncovalent, subnanomolar thrombin inhibitor |
TBA |
22377673 |
4 |
Proteasome inhibitors for cancer therapy. |
Cephalon |
20945905 |
4 |
Design, synthesis, crystal structures, and antimicrobial activity of sulfonamide boronic acids asß-lactamase inhibitors. |
University of California San Francisco |
20020755 |
2 |
Molassamide, a depsipeptide serine protease inhibitor from the marine cyanobacterium Dichothrix utahensis. |
Smithsonian Marine Station At Ft. Pierce |
| 46 |
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 |
| 9 |
Diphenylborinic acid is a strong inhibitor of serine proteases |
TBA |
| 2 |
Stereochemical approach for enzyme inhibitor design |
TBA |
| 4 |
Engineering of cyclic peptides with novel inhibiting properties to differentiate two serine proteases, chymotrypsin and subtilisin Carlsberg |
TBA |
| 2 |
Boric acid effect ont he hydrolysis of 4-nitrophenyl 2,3-dihydroxybenzoate: mimic of borate inhibition of serine proteases |
TBA |
| 7 |
Janus compounds: dual inhibitors of proteinases |
TBA |
| 12 |
MDL 74147, a novel selective and soluble inhibitor of human renin. Synthesis, structure-activity relationship, species and protease selectivities. |
TBA |
| 5 |
Borinic acid inhibitors as probes of the factors involved in binding at the active sites of subtilisin carlsberg and α-chymotrypsin |
TBA |
14684338 |
44 |
P1 and P3 optimization of novel bicycloproline P2 bearing tetrapeptidyl alpha-ketoamide based HCV protease inhibitors. |
Eli Lilly |
12593666 |
30 |
Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor. |
Senju Pharmaceutical |
11549442 |
6 |
Alpha-ketoester-based photobiological switches: synthesis, peptide chain extension and assay against alpha-chymotrypsin. |
University of Canterbury |
11078188 |
20 |
1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma. |
Shionogi |
10866385 |
13 |
Mass spectrometry reveals elastase inhibitors from the reactive centre loop of alpha1-antitrypsin. |
The Oxford Centre For Molecular Sciences |
10698435 |
150 |
Structure-activity relationship studies of chloromethyl ketone derivatives for selective human chymase inhibitors. |
Kyoto Pharmaceutical University |
9925737 |
57 |
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 |
9871686 |
23 |
Design and synthesis of monocyclic beta-lactams as mechanism-based inhibitors of human cytomegalovirus protease. |
Glaxo Wellcome Research and Development |
9871511 |
54 |
Peptidyl human heart chymase inhibitors. 1. Synthesis and inhibitory activity of difluoromethylene ketone derivatives bearing P' binding subsites. |
Green Cross Research Laboratories |
9804697 |
61 |
Structure-based enhancement of boronic acid-based inhibitors of AmpC beta-lactamase. |
Northwestern University Medical School |
9767628 |
31 |
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 |
9703466 |
35 |
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 |
9667976 |
58 |
beta-Lactam derivatives as inhibitors of human cytomegalovirus protease. |
Boehringer Ingelheim (Canada) |
9406601 |
109 |
Peptidomimetic inhibitors of the human cytomegalovirus protease. |
Boehringer Ingelheim |
9216834 |
153 |
Substituted 3-(phenylsulfonyl)-1-phenylimidazolidine-2,4-dione derivatives as novel nonpeptide inhibitors of human heart chymase. |
Suntory |
31223449 |
18 |
DMSO-Perturbing Assay for Identifying Promiscuous Enzyme Inhibitors. |
Kyushu University |
8691456 |
7 |
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 |
7837244 |
33 |
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 |
7739010 |
118 |
Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin. |
Thrombosis Research Institute |
7629790 |
32 |
New orally active serine protease inhibitors. |
Minase Research Institute |
7562931 |
41 |
Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 3. In vitro and in vivo potency of a series of peptidyl alpha-ketobenzoxazoles. |
Zeneca Pharmaceuticals |
3941405 |
15 |
Carboxyl-modified amino acids and peptides as protease inhibitors. |
TBA |
29039662 |
62 |
Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds. |
Csir-National Chemical Laboratory |
30222343 |
4 |
Dinghupeptins A-D, Chymotrypsin Inhibitory Cyclodepsipeptides Produced by a Soil-Derived Streptomyces. |
Chinese Academy of Sciences |
29463448 |
1 |
Discovery and validation of 2-styryl substituted benzoxazin-4-ones as a novel scaffold for rhomboid protease inhibitors. |
Heinrich-Heine University Duesseldorf |
29936356 |
27 |
Engineering potent mesotrypsin inhibitors based on the plant-derived cyclic peptide, sunflower trypsin inhibitor-1. |
The University of Queensland |
2391691 |
55 |
Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters. |
Merck Sharp and Dohme Research Laboratories |
2187995 |
12 |
O'-(epoxyalkyl)tyrosines and (epoxyalkyl)phenylalanine as irreversible inactivators of serine proteases: synthesis and inhibition mechanism. |
State University |
1447734 |
29 |
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 |
27775715 |
113 |
Design and characterization of bivalent BET inhibitors. |
Dana-Farber Cancer Institute |
10869410 |
62 |
S33084, a novel, potent, selective, and competitive antagonist at dopamine D(3)-receptors: I. Receptorial, electrophysiological and neurochemical profile compared with GR218,231 and L741,626. |
Centre De Recherches De Croissy |