156 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
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Synthesis and Evaluation of Macrocyclic Peptide Aldehydes as Potent and Selective Inhibitors of the 20S Proteasome.
Whitman College
Cathepsin B Inhibitors: Combining Dipeptide Nitriles with an Occluding Loop Recognition Element by Click Chemistry.
University Of Bonn
Synthesis and biochemical evaluation of benzoylbenzophenone thiosemicarbazone analogues as potent and selective inhibitors of cathepsin L.
Baylor University
Synthesis and biological evaluation of open-chain analogs of cyclic peptides as inhibitors of cellular Shp2 activity.
Hebei University Of Science & Technology
SAR studies of differently functionalized chalcones based hydrazones and their cyclized derivatives as inhibitors of mammalian cathepsin B and cathepsin H.
Kurukshetra University
Structure-based design and optimization of potent inhibitors of the adenoviral protease.
Novartis Institute For Biomedical Research
8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors.
Array Biopharma
Structures and bioactivities of dihydrochalcones from Metrodorea stipularis.
Universidade Federal De S£O Carlos
The discovery of potent, selective, and reversible inhibitors of the house dust mite peptidase allergen Der p 1: an innovative approach to the treatment of allergic asthma.
Domainex
3-Cyano-3-aza-ß-amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins.
University Of Bonn
Probing of primed and unprimed sites of calpains: Design, synthesis and evaluation of epoxysuccinyl-peptide derivatives as selective inhibitors.
E£Tv£S Lor£Nd University (Elte)
Cathepsin C inhibitors: property optimization and identification of a clinical candidate.
Astrazeneca
Structurally novel highly potent proteasome inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptide boronates.
Hokkaido University
Acyl hydrazides and triazoles as novel inhibitors of mammalian cathepsin B and cathepsin H.
Kurukshetra University
Development of new cathepsin B inhibitors: combining bioisosteric replacements and structure-based design to explore the structure-activity relationships of nitroxoline derivatives.
University Of Ljubljana
Synopsis of some recent tactical application of bioisosteres in drug design.
Bristol-Myers Squibb Pharmaceutical Research And Development
Nonpeptidic lysosomal modulators derived from z-phe-ala-diazomethylketone for treating protein accumulation diseases.
TBA
Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors.
Astrazeneca
(1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): a potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis.
Astrazeneca
Selective nitrile inhibitors to modulate the proteolytic synergism of cathepsins S and F.
University Of Bonn
Thrombin inhibitors from the freshwater cyanobacterium Anabaena compacta.
Hokkaido University
Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.
Astrazeneca
Synthesis and biochemical evaluation of thiochromanone thiosemicarbazone analogues as inhibitors of cathepsin L.
TBA
Exploring activity cliffs in medicinal chemistry.
Rheinische Friedrich-Wilhelms-Universit£T
Structural optimization of azadipeptide nitriles strongly increases association rates and allows the development of selective cathepsin inhibitors.
University Of Bonn
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.
University Of Florida
Natural polyprenylated benzophenones inhibiting cysteine and serine proteases.
Federal University Of Alfenas
Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity.
Ewha Womans University
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 trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB.
University Of California
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
Johnson & Johnson Pharmaceutical Research & Development
Cathepsin B inhibitory activities of phthalates isolated from a marine Pseudomonas strain.
Pukyong National University
Development of peptidomimetics with a vinyl sulfone warhead as irreversible falcipain-2 inhibitors.
University Of Messina
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
Merck Frosst Centre For Therapeutic Research
Novel cell-penetrating alpha-keto-amide calpain inhibitors as potential treatment for muscular dystrophy.
Santhera Pharmaceuticals
Synthesis of peptide aldehyde derivatives as selective inhibitors of human cathepsin L and their inhibitory effect on bone resorption.
Takeda Chemical Industries
D-amino acid containing, high-affinity inhibitors of recombinant human calpain I.
Cephalon
Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid.
Maxim Pharmaceuticals
Highly potent and selective peptide-based inhibitors of the hepatitis C virus serine protease: towards smaller inhibitors.
Boehringer Ingelheim Pharmaceuticals
Design, synthesis and biological evaluation of peptidyl-vinylaminophosphonates as novel cysteine protease inhibitors.
National Chemical Laboratory (Csir-Ncl)
Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors.
University Of Messina
Discovery and kinetic evaluation of 6-substituted 4-benzylthio-1,3,5-triazin-2(1H)-ones as inhibitors of cathepsin B.
University Of Ljubljana
Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.
Boehringer Ingelheim (Canada)
1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors: separation of desired cellular activity from undesired tissue accumulation through optimization of basic nitrogen pka.
Merck Research Laboratories
Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease.
Merck Research Laboratories
Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors.
Merck Research Laboratories
Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L.
Baylor University
Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: improving selectivity over hERG.
Merck Research Laboratories
Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors.
Georgia Institute Of Technology
MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
Merck Research Laboratories
Allicin and derivates are cysteine protease inhibitors with antiparasitic activity.
University Of WüRzburg
2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors.
Merck Research Laboratories
On-bead screening of a combinatorial fumaric acid derived peptide library yields antiplasmodial cysteine protease inhibitors with unusual peptide sequences.
University Of Duisburg-Essen
Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors.
Schering-Plough
Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C.
Merck Frosst Canada
Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors.
Baylor University
Novel peptidomimetics containing a vinyl ester moiety as highly potent and selective falcipain-2 inhibitors.
University Of Messina
Possible involvement of radical intermediates in the inhibition of cysteine proteases by allenyl esters and amides.
University Of Toyama
Peptidyl epoxides extended in the P' direction as cysteine protease inhibitors: effect on affinity and mechanism of inhibition.
Bar-Ilan University
Synthesis and calpain inhibitory activity of peptidomimetic compounds with constrained amino acids at the P2 position.
The University Of Tennessee Health Science Center
Effect of novel N-cyano-tetrahydro-pyridazine compounds, a class of cathepsin K inhibitors, on the bone resorptive activity of mature osteoclasts.
Korea Research Institute Of Chemical Technology
Substrate optimization for monitoring cathepsin C activity in live cells.
Genomics Institute Of The Novartis Research Foundation
Novel potent macrocyclic inhibitors of the hepatitis C virus NS3 protease: use of cyclopentane and cyclopentene P2-motifs.
LinköPing University
Identification and characterization of 3-substituted pyrazolyl esters as alternate substrates for cathepsin B: the confounding effects of DTT and cysteine in biological assays.
University Of Pennsylvania
Primary amides as selective inhibitors of cathepsin K.
Merck Frosst Centre For Therapeutic Research
Bicyclic carbamates as inhibitors of papain-like cathepsin proteases.
The Genomics Institute Of The Novartis Research Foundation
Synthesis, calpain inhibitory activity, and cytotoxicity of P2-substituted proline and thiaproline peptidyl aldehydes and peptidyl alpha-ketoamides.
The University Of Tennessee Health Science Center
Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K.
Celera Genomics
Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors.
Celera
A novel series of urea-based peptidomimetic calpain inhibitors.
The University Of Tennessee Health Science Center
Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.
Celera Genomics
Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?
Glaxosmithkline
Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.
Merck Frosst Centre For Therapeutic Research
P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K.
Glaxosmithkline
A structural screening approach to ketoamide-based inhibitors of cathepsin K.
Glaxosmithkline
A systematic approach to the optimization of substrate-based inhibitors of the hepatitis C virus NS3 protease: discovery of potent and specific tripeptide inhibitors.
Boehringer Ingelheim (Canada)
Inhibition of lysosomal cysteine proteases by chrysotherapeutic compounds: a possible mechanism for the antiarthritic activity of Au(I).
University Of Southern California
P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors.
Eli Lilly
Potent and selective P2-P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1', P1, and/or P3 substitutions.
Glaxosmithkline
Rational design of potent and selective NH-linked aryl/heteroaryl cathepsin K inhibitors.
Merck Frosst Centre For Therapeutic Research
P1 and P3 optimization of novel bicycloproline P2 bearing tetrapeptidyl alpha-ketoamide based HCV protease inhibitors.
Eli Lilly
(4-Piperidinylphenyl)aminoethyl amides as a novel class of non-covalent cathepsin K inhibitors.
Amgen
N-arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B.
Novartis Institute Of Biomedical Research
3,4-disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P2 elements for selectivity.
Ligand Pharmaceuticals
Benzoylalanine-derived ketoamides carrying vinylbenzyl amino residues: discovery of potent water-soluble calpain inhibitors with oral bioavailability.
Abbott
Peptidyl aldehyde inhibitors of calpain incorporating P2-proline mimetics.
University Of Tennessee Health Science Center
Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor.
Senju Pharmaceutical
Design of noncovalent inhibitors of human cathepsin L. From the 96-residue proregion to optimized tripeptides.
National Research Council Of Canada
6-Acylamino-penam derivatives: synthesis and inhibition of cathepsins B, L, K, and S.
Currently Naeja Pharmaceutical
Design and synthesis of 6-substituted amino-4-oxa-1-azabicyclo[3,2,0]heptan-7-one derivatives as cysteine proteases inhibitors.
Currently Naeja Pharmaceutical
General solid-phase method to prepare novel cyclic ketone inhibitors of the cysteine protease cruzain.
University Of California
Novel route to the synthesis of peptides containing 2-amino-1'-hydroxymethyl ketones and their application as cathepsin K inhibitors.
Celera
Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases.
University Of Gda£?Sk
Discovery of phenyl alanine derived ketoamides carrying benzoyl residues as novel calpain inhibitors.
Abbott
Identification of potent and selective mechanism-based inhibitors of the cysteine protease cruzain using solid-phase parallel synthesis.
University Of California
Identification of dipeptidyl nitriles as potent and selective inhibitors of cathepsin B through structure-based drug design.
Novartis Pharmaceuticals
Potent reversible inhibitors of the protein tyrosine phosphatase CD45.
Astrazeneca Pharmaceuticals
Novel, nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L.
Merck Frosst Centre For Therapeutic Research
Synthesis and calpain inhibitory activity of alpha-ketoamides with 2,3-methanoleucine stereoisomers at the P2 position.
The University Of Tennessee Health Science Center
Synthesis and biological evaluation of novel piperidine carboxamide derived calpain inhibitors.
Knoll
Combinatorial library of serine and cysteine protease inhibitors that interact with both the S and S' binding sites.
Brown University
Studies on the C-terminal of hexapeptide inhibitors of the hepatitis C virus serine protease.
Boehringer Ingelheim (Canada)
Inhibition of human cytomegalovirus protease N(o) with monocyclic beta-lactams.
Boehringer Ingelheim (Canada)
Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K.
Smithkline Beecham Pharmaceuticals
Novel peptidyl alpha-keto amide inhibitors of calpains and other cysteine proteases.
Georgia Institute Of Technology
In vitro effects of some anabolic compounds on erythrocyte carbonic anhydrase I and II.
Balikesir University
Design, synthesis and evaluation of trisubstituted thiazoles targeting plasmodium falciparum cysteine proteases
University, Mississippi
Pharmacological properties of ABT-239 [4-(2-{2-[(2R)-2-Methylpyrrolidinyl]ethyl}-benzofuran-5-yl)benzonitrile]: I. Potent and selective histamine H3 receptor antagonist with drug-like properties.
Abbott Laboratories
Preclinical pharmacology of fiduxosin, a novel alpha(1)-adrenoceptor antagonist with uroselective properties.
Abbott Laboratories