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160 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
10617079 3 Tokaramide A, a new cathepsin B inhibitor from the marine sponge Theonella aff. mirabilis.EBI Laboratory of Aquatic Natural Products Chemistry, Graduate School of Agricultural and Life Sciences, The University of Tokyo, Japan.
27994740 41 Dipeptidyl Nitroalkenes as Potent Reversible Inhibitors of Cysteine Proteases Rhodesain and Cruzain.EBI Universitat Jaume I
27214508 43 Straightforward synthesis of 2,4,6-trisubstituted 1,3,5-triazine compounds targeting cysteine cathepsins K and S.EBI CNRS
27690432 75 Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986).EBI CHARLES RIVER DISCOVERY RESEARCH SERVICES UK LIMITED
26985310 8 Synthesis and Evaluation of Macrocyclic Peptide Aldehydes as Potent and Selective Inhibitors of the 20S Proteasome.EBI Whitman College
26985300 110 Cathepsin B Inhibitors: Combining Dipeptide Nitriles with an Occluding Loop Recognition Element by Click Chemistry.EBI University of Bonn
26462052 29 Synthesis and biochemical evaluation of benzoylbenzophenone thiosemicarbazone analogues as potent and selective inhibitors of cathepsin L.EBI Baylor University
25865131 40 Synthesis and biological evaluation of open-chain analogs of cyclic peptides as inhibitors of cellular Shp2 activity.EBI Hebei University of Science& Technology
24913985 73 SAR studies of differently functionalized chalcones based hydrazones and their cyclized derivatives as inhibitors of mammalian cathepsin B and cathepsin H.EBI Kurukshetra University
25571794 40 Structure-based design and optimization of potent inhibitors of the adenoviral protease.EBI Novartis Institute for Biomedical Research
25411915 54 8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors.EBI Array BioPharma
25375026 14 Structures and bioactivities of dihydrochalcones from Metrodorea stipularis.EBI Universidade Federal de S£o Carlos
25365789 83 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.EBI Domainex Ltd.
25313316 20 3-Cyano-3-aza--amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins.EBI University of Bonn
24915003 34 Probing of primed and unprimed sites of calpains: Design, synthesis and evaluation of epoxysuccinyl-peptide derivatives as selective inhibitors.EBI E£tv£s Lor£nd University (ELTE)
24592859 59 Cathepsin C inhibitors: property optimization and identification of a clinical candidate.EBI AstraZeneca
24524217 65 Structurally novel highly potent proteasome inhibitors created by the structure-based hybridization of nonpeptidic belactosin derivatives and peptide boronates.EBI Hokkaido University
24642566 17 Acyl hydrazides and triazoles as novel inhibitors of mammalian cathepsin B and cathepsin H.EBI Kurukshetra University
23252745 86 Development of new cathepsin B inhibitors: combining bioisosteric replacements and structure-based design to explore the structure-activity relationships of nitroxoline derivatives.EBI University of Ljubljana
24900293 78 Discovery of novel cyanamide-based inhibitors of cathepsin C.EBI TBA
19616430 120 Design of selective Cathepsin inhibitors.EBI AstraZeneca
16546382 100 Keto-1,3,4-oxadiazoles as cathepsin K inhibitors.EBI Celera Genomics, Inc.
23122525 9 Fluorescent nitrile-based inhibitors of cysteine cathepsins.EBI University of Bonn
21413808 170 Synopsis of some recent tactical application of bioisosteres in drug design.EBI Bristol-Myers Squibb Pharmaceutical Research and Development
24900408 4 Nonpeptidic lysosomal modulators derived from z-phe-ala-diazomethylketone for treating protein accumulation diseases.EBI TBA
22984809 111 Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors.EBI AstraZeneca
22742641 113 (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.EBI AstraZeneca
22686657 60 Selective nitrile inhibitors to modulate the proteolytic synergism of cathepsins S and F.EBI University of Bonn
22950366 6 Thrombin inhibitors from the freshwater cyanobacterium Anabaena compacta.EBI Hokkaido University
22858142 121 Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.EBI AstraZeneca
24900494 72 Synthesis and biochemical evaluation of thiochromanone thiosemicarbazone analogues as inhibitors of cathepsin L.EBI TBA
22236250 16 Exploring activity cliffs in medicinal chemistry.EBI Rheinische Friedrich-Wilhelms-Universit£t
21128614 76 Structural optimization of azadipeptide nitriles strongly increases association rates and allows the development of selective cathepsin inhibitors.EBI University of Bonn
20598553 38 Constrained peptidomimetics as antiplasmodial falcipain-2 inhibitors.EBI Universit£ di Messina
19709887 25 Novel 2H-isoquinolin-3-ones as antiplasmodial falcipain-2 inhibitors.EBI Universit£ di Messina
19715320 87 Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.EBI University of Florida
18995931 16 Natural polyprenylated benzophenones inhibiting cysteine and serine proteases.EBI Federal University of Alfenas
19419206 77 Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity.EBI Ewha Womans University
17535802 91 Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.EBI Merck Research Laboratories
18420405 26 Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB.EBI University of California
18053726 364 Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.EBI Johnson& Johnson Pharmaceutical Research& Development
18289850 4 Cathepsin B inhibitory activities of phthalates isolated from a marine Pseudomonas strain.EBI Pukyong National University
18232656 30 Development of peptidomimetics with a vinyl sulfone warhead as irreversible falcipain-2 inhibitors.EBI University of Messina
18226527 80 The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.EBI Merck Frosst Centre for Therapeutic Research
16185867 5 Novel cell-penetrating alpha-keto-amide calpain inhibitors as potential treatment for muscular dystrophy.EBI Santhera Pharmaceuticals
10669559 180 Protease inhibitors: current status and future prospects.EBI University of Queensland
9784105 68 Synthesis of peptide aldehyde derivatives as selective inhibitors of human cathepsin L and their inhibitory effect on bone resorption.EBI Takeda Chemical Industries, Ltd.
9667954 47 D-amino acid containing, high-affinity inhibitors of recombinant human calpain I.EBI Cephalon, Inc.
14980679 30 Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid.EBI Maxim Pharmaceuticals
11055335 27 Highly potent and selective peptide-based inhibitors of the hepatitis C virus serine protease: towards smaller inhibitors.EBI Boehringer Ingelheim
 11 Peptidyl aldehyde derivatives as potent and selective inhibitors of cathepsin LEBI TBA
22019466 13 Design, synthesis and biological evaluation of peptidyl-vinylaminophosphonates as novel cysteine protease inhibitors.EBI National Chemical Laboratory (CSIR-NCL)
21420760 8 Peptidomimetics containing a vinyl ketone warhead as falcipain-2 inhibitors.EBI University of Messina
21849222 50 Discovery and kinetic evaluation of 6-substituted 4-benzylthio-1,3,5-triazin-2(1H)-ones as inhibitors of cathepsin B.EBI University of Ljubljana
20823284 9 Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.EBI Boehringer Ingelheim (Canada) Ltd.
21227690 68 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.EBI Merck Research laboratories
21041084 102 Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease.EBI Merck Research Laboratories
21030256 61 Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors.EBI Merck Research Laboratories
20933415 50 Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L.EBI Baylor University
20843687 60 Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: improving selectivity over hERG.EBI Merck Research Laboratories
20690647 33 Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors.EBI Georgia Institute of Technology
19841155 29 MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.EBI Merck Research Laboratories
20692829 21 Allicin and derivates are cysteine protease inhibitors with antiparasitic activity.EBI University of Würzburg
20594841 123 2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors.EBI Merck Research Laboratories
19715342 19 On-bead screening of a combinatorial fumaric acid derived peptide library yields antiplasmodial cysteine protease inhibitors with unusual peptide sequences.EBI University of Duisburg-Essen
20153187 32 Dioxo-triazines as a novel series of cathepsin K inhibitors.EBI Schering-Plough Corporation
20149657 53 Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors.EBI Schering-Plough Corporation
19665376 48 Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C.EBI Merck Frosst Canada& Co.
20089402 72 Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors.EBI Baylor University
19769357 93 Structure-guided development of selective TbcatB inhibitors.EBI University of California
 10 Nonpeptidic inhibitors of recombinant human calpain IEBI TBA
 2 Oligopresentation of protease inhibitors with β-cyclodextrin as templateEBI TBA
 22 Inhibition of human erythrocyte calpain I by novel quinolinecarboxamidesEBI TBA
 4 Design of a new selective cysteine protease inactivator and its mechanistic implicationsEBI TBA
19296600 14 Novel peptidomimetics containing a vinyl ester moiety as highly potent and selective falcipain-2 inhibitors.EBI University of Messina
19231183 44 5-Aminopyrimidin-2-ylnitriles as cathepsin K inhibitors.EBI AstraZeneca
18951789 1 Possible involvement of radical intermediates in the inhibition of cysteine proteases by allenyl esters and amides.EBI University of Toyama
18789705 6 Peptidyl epoxides extended in the P' direction as cysteine protease inhibitors: effect on affinity and mechanism of inhibition.EBI Bar Ilan University
18694642 6 Synthesis and calpain inhibitory activity of peptidomimetic compounds with constrained amino acids at the P2 position.EBI The University of Tennessee Health Science Center
18571402 24 Effect of novel N-cyano-tetrahydro-pyridazine compounds, a class of cathepsin K inhibitors, on the bone resorptive activity of mature osteoclasts.EBI Korea Research Institute of Chemical Technology
18313933 18 Substrate optimization for monitoring cathepsin C activity in live cells.EBI Genomics Institute of the Novartis Research Foundation (GNF)
17845856 1 Novel potent macrocyclic inhibitors of the hepatitis C virus NS3 protease: use of cyclopentane and cyclopentene P2-motifs.EBI Linköping University
17656088 15 Identification and characterization of 3-substituted pyrazolyl esters as alternate substrates for cathepsin B: the confounding effects of DTT and cysteine in biological assays.EBI University of Pennsylvania
17544269 30 Primary amides as selective inhibitors of cathepsin K.EBI Merck Frosst Centre for Therapeutic Research
17196818 90 Bicyclic carbamates as inhibitors of papain-like cathepsin proteases.EBI The Genomics Institute of the Novartis Research Foundation
17049233 82 Design of potent inhibitors of human beta-secretase. Part 2.EBI Pfizer Inc.
16913717 42 Synthesis, calpain inhibitory activity, and cytotoxicity of P2-substituted proline and thiaproline peptidyl aldehydes and peptidyl alpha-ketoamides.EBI The University of Tennessee Health Science Center
16750630 28 Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K.EBI Celera Genomics
16686537 165 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.EBI Celera
16647256 16 Dipeptidyl nitriles as human dipeptidyl peptidase I inhibitors.EBI Arpida A/S
16412635 4 A novel series of urea-based peptidomimetic calpain inhibitors.EBI The University of Tennessee Health Science Center
16302794 53 Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K.EBI Celera Genomics, Inc.
16290936 69 Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?EBI GlaxoSmithKline
16250645 35 Azepanone-based inhibitors of human cathepsin L.EBI GlaxoSmithKline
16154747 37 Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.EBI Merck Frosst Centre for Therapeutic Research
15982880 86 P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K.EBI GlaxoSmithKline
15896958 32 Acyclic cyanamide-based inhibitors of cathepsin K.EBI GlaxoSmithKline
15837295 55 A structural screening approach to ketoamide-based inhibitors of cathepsin K.EBI GlaxoSmithKline
15780613 28 Novel and potent cyclic cyanamide-based cathepsin K inhibitors.EBI GlaxoSmithKline
15634028 5 Retro hydrazino-azapeptoids as peptidomimetics of proteasome inhibitors.EBI Université Rennes 1
15588093 3 A systematic approach to the optimization of substrate-based inhibitors of the hepatitis C virus NS3 protease: discovery of potent and specific tripeptide inhibitors.EBI Boehringer Ingelheim (Canada) Ltd.
15380210 18 Inhibition of lysosomal cysteine proteases by chrysotherapeutic compounds: a possible mechanism for the antiarthritic activity of Au(I).EBI University of Southern California
15341970 59 P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors.EBI Lilly Research Laboratory
15341947 57 Potent and selective P2-P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1', P1, and/or P3 substitutions.EBI GlaxoSmithKline
15261289 38 Rational design of potent and selective NH-linked aryl/heteroaryl cathepsin K inhibitors.EBI Merck Frosst Centre for Therapeutic Research
15177446 41 Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors.EBI GlaxoSmithKline
14684338 44 P1 and P3 optimization of novel bicycloproline P2 bearing tetrapeptidyl alpha-ketoamide based HCV protease inhibitors.EBI Lilly Research Laboratory
14684304 41 (4-Piperidinylphenyl)aminoethyl amides as a novel class of non-covalent cathepsin K inhibitors.EBI Amgen Inc.
14592520 41 N-arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B.EBI Novartis Institute of Biomedical Research
12781193 36 3,4-disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P2 elements for selectivity.EBI Ligand Pharmaceuticals
12773044 18 Benzoylalanine-derived ketoamides carrying vinylbenzyl amino residues: discovery of potent water-soluble calpain inhibitors with oral bioavailability.EBI Abbott GmbH & Co. KG
12617890 9 Peptidyl aldehyde inhibitors of calpain incorporating P2-proline mimetics.EBI University of Tennessee Health Science Center
12593666 30 Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor.EBI Senju Pharmaceutical Co.
12431059 27 Design of noncovalent inhibitors of human cathepsin L. From the 96-residue proregion to optimized tripeptides.EBI National Research Council of Canada
12419374 45 6-Acylamino-penam derivatives: synthesis and inhibition of cathepsins B, L, K, and S.EBI currently NAEJA Pharmaceutical Inc.
12419373 18 Design and synthesis of 6-substituted amino-4-oxa-1-azabicyclo[3,2,0]heptan-7-one derivatives as cysteine proteases inhibitors.EBI currently NAEJA Pharmaceutical Inc.
12270191 36 General solid-phase method to prepare novel cyclic ketone inhibitors of the cysteine protease cruzain.EBI University of California
12270170 42 Novel route to the synthesis of peptides containing 2-amino-1'-hydroxymethyl ketones and their application as cathepsin K inhibitors.EBI Celera
12213061 23 Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases.EBI University of Gda£?sk
11992771 19 Discovery of phenyl alanine derived ketoamides carrying benzoyl residues as novel calpain inhibitors.EBI Abbott GmbH&Co. KG
11806719 61 Identification of potent and selective mechanism-based inhibitors of the cysteine protease cruzain using solid-phase parallel synthesis.EBI University of California
11741472 45 Identification of dipeptidyl nitriles as potent and selective inhibitors of cathepsin B through structure-based drug design.EBI Novartis Pharmaceuticals Corporation
11356112 175 Potent reversible inhibitors of the protein tyrosine phosphatase CD45.EBI AstraZeneca Pharmaceuticals
11311061 40 Azepanone-based inhibitors of human and rat cathepsin K.EBI GlaxoSmithKline
11141092 85 Novel, nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L.EBI Merck Frosst Centre for Therapeutic Research
11086714 10 Synthesis and calpain inhibitory activity of alpha-ketoamides with 2,3-methanoleucine stereoisomers at the P2 position.EBI The University of Tennessee Health Science Center
11012026 18 Synthesis and biological evaluation of novel piperidine carboxamide derived calpain inhibitors.EBI KNOLL AG
10508448 11 Combinatorial library of serine and cysteine protease inhibitors that interact with both the S and S' binding sites.EBI Brown University
9873610 48 Studies on the C-terminal of hexapeptide inhibitors of the hepatitis C virus serine protease.EBI Boehringer Ingelheim (Canada) Ltd
9873596 18 P2-proline-derived inhibitors of calpain I.EBI Cephalon, Inc.
9871780 85 Inhibition of human cytomegalovirus protease N(o) with monocyclic beta-lactams.EBI Boehringer Ingelheim (Canada) Ltd
9871680 5 Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids.EBI ProScript, Inc.
9733481 31 Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K.EBI SmithKline Beecham Pharmaceuticals
9406601 109 Peptidomimetic inhibitors of the human cytomegalovirus protease.EBI Boehringer Ingelheim Ltd.
8831774 261 Novel peptidyl alpha-keto amide inhibitors of calpains and other cysteine proteases.EBI School of Chemistry and Biochemistry
7650671 15 Vinyl sulfones as mechanism-based cysteine protease inhibitors.EBI Khepri Pharmaceuticals, Inc.
24095934 60 Synthesis and investigation of dihydroxychalcones as calpain and cathepsin inhibitors.BDB Ewha Womans University, Seoul 120-750, Republic of Korea.
14606817 9 Synthesis of a diverse library of mechanism-based cysteine protease inhibitors.BDB University of California-Berkeley
10746010 54 Solid-phase synthesis of a combinatorial array of 1,3-bis(acylamino)-2-butanones, inhibitors of the cysteine proteases cathepsins K and L.BDB SmithKline Beecham Pharmaceuticals
18343903 16 Peptidomimetic 2-cyanopyrrolidines as potent selective cathepsin L inhibitors.BDB The M S University of Baroda
17441903 3 Synthesis of peptidyl ene diones: selective inactivators of the cysteine proteinases.BDB Queen's University of Belfast,
10662686 6 Selective targeting of lysosomal cysteine proteases with radiolabeled electrophilic substrate analogs.BDB University of California, San Francisco
19515558 120 Dipeptidyl nitrile inhibitors of Cathepsin L.BDB AstraZeneca
12904076 158 A novel class of nonpeptidic biaryl inhibitors of human cathepsin K.BDB Merck Frosst Centre for Therapeutic Research
16302795 36 Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity.BDB Merck Frosst Centre for Therapeutic Research
11262083 56 Cyclic ketone inhibitors of the cysteine protease cathepsin K.BDB GSK
17157021 47 Acyclic, orally bioavailable ketone-based cathepsin K inhibitors.BDB GSK
16509577 52 Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors.BDB GSK
16413777 112 Identification of a potent and selective non-basic cathepsin K inhibitor.BDB Merck Frosst Centre for Therapeutic Research
17590332 108 The identification of potent, selective, and bioavailable cathepsin S inhibitors.BDB Merck Frosst Centre for Therapeutic Research
17469812 12 Characterization and optimization of selective, nonpeptidic inhibitors of cathepsin S with an unprecedented binding mode.BDB University of California at Berkeley
17034136 20 Identification of selective, nonpeptidic nitrile inhibitors of cathepsin s using the substrate activity screening method.BDB University of California at Berkeley