174 articles for thisTarget
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Leupeptazin, a highly modified tripeptide isolated from cultures of a Streptomyces sp. inhibits cathepsin K.
University of British Columbia
Affinity Crystallography: A New Approach to Extracting High-Affinity Enzyme Inhibitors from Natural Extracts.
University of British Columbia
Straightforward synthesis of 2,4,6-trisubstituted 1,3,5-triazine compounds targeting cysteine cathepsins K and S.
Cnrs
Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986).
Charles River Discovery Research Services
Cathepsin B Inhibitors: Combining Dipeptide Nitriles with an Occluding Loop Recognition Element by Click Chemistry.
University of Bonn
Development of N-(Functionalized benzoyl)-homocycloleucyl-glycinonitriles as Potent Cathepsin K Inhibitors.
National Institute of Chemistry
Structure-based design and optimization of potent inhibitors of the adenoviral protease.
Novartis Institute For Biomedical Research
Cathepsin C inhibitors: property optimization and identification of a clinical candidate.
Astrazeneca
Docking-based virtual screening of covalently binding ligands: an orthogonal lead discovery approach.
Msd Animal Health Innovation
3D QSAR studies on ketoamides of human cathepsin K inhibitors based on two different alignment methods.
Chinese Academy of Sciences
Use of papain as a model for the structure-based design of cathepsin K inhibitors: crystal structures of two papain-inhibitor complexes demonstrate binding to S'-subsites.
Smithkline Beecham Pharmaceuticals
Structure-based design of cathepsin K inhibitors containing a benzyloxy-substituted benzoyl peptidomimetic.
Smithkline Beecham Pharmaceuticals
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
Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.
Astrazeneca
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
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
Johnson & Johnson Pharmaceutical Research & Development
The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
Merck Frosst Centre For Therapeutic Research
4-Aminophenoxyacetic acids as a novel class of reversible cathepsin K inhibitors.
Sankyo
cis-6-oxo-hexahydro-2-oxa-1,4-diazapentalene and cis-6-oxo-hexahydropyrrolo[3,2-c]pyrazole based scaffolds: design rationale, synthesis and cysteinyl proteinase inhibition.
Amura Therapeutics
Azepanone-based inhibitors of human cathepsin S: optimization of selectivity via the P2 substituent.
Glaxosmithkline
Difluoroethylamines as an amide isostere in inhibitors of cathepsin K.
Merck Frosst Centre For Therapeutic Research
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
Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: improving selectivity over hERG.
Merck Research Laboratories
MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
Merck Research Laboratories
6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors.
Merck Research Laboratories
2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors.
Merck Research Laboratories
4-(3-Trifluoromethylphenyl)-pyrimidine-2-carbonitrile as cathepsin S inhibitors: N3, not N1 is critically important.
Merck Research Laboratories
Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors.
Schering-Plough
The discovery of MK-0674, an orally bioavailable cathepsin K inhibitor.
Merck Frosst Centre For Therapeutic Research
Solid-phase parallel synthesis and SAR of 4-amidofuran-3-one inhibitors of cathepsin S: effect of sulfonamides P3 substituents on potency and selectivity.
Medivir
Investigation of ketone warheads as alternatives to the nitrile for preparation of potent and selective cathepsin K inhibitors.
Merck Frosst Centre For Therapeutic Research
Identification of a nonbasic, nitrile-containing cathepsin K inhibitor (MK-1256) that is efficacious in a monkey model of osteoporosis.
Merck Frosst Centre For Therapeutic Research
Effect of cathepsin K inhibitors on bone resorption.
Novartis Institutes For Biomedical Research
4-Amino-2-cyanopyrimidines: novel scaffold for nonpeptidic cathepsin S inhibitors.
Novartis Institutes For Biomedical Research
Discovery of selective and nonpeptidic cathepsin S inhibitors.
Novartis Institutes For Biomedical Research
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
Haploscleridamine, a novel tryptamine-derived alkaloid from a sponge of the order haplosclerida: an inhibitor of cathepsin K.
Millennium Pharmaceuticals
A new dimeric dihydrochalcone and a new prenylated flavone from the bud covers of Artocarpus altilis: potent inhibitors of cathepsin K.
Millennium Pharmaceuticals
Primary amides as selective inhibitors of cathepsin K.
Merck Frosst Centre For Therapeutic Research
Discovery of CMX990: A Potent SARS-CoV-2 3CL Protease Inhibitor Bearing a Novel Warhead.
Calibr At Scripps Research Institute
Identification of Ebselen derivatives as novel SARS-CoV-2 main protease inhibitors: Design, synthesis, biological evaluation, and structure-activity relationships exploration.
Shandong University
Dipeptide-Derived Alkynes as Potent and Selective Irreversible Inhibitors of Cysteine Cathepsins.
Helmholtz-Zentrum Dresden-Rossendorf
Bicyclic carbamates as inhibitors of papain-like cathepsin proteases.
The Genomics Institute of The Novartis Research Foundation
Design and synthesis of dual cathepsin L and S inhibitors and antimetastatic activity evaluation in pancreatic cancer cells.
Shenyang Pharmaceutical University
Discovery of selective covalent cathepsin K inhibitors containing novel 4-cyanopyrimidine warhead based on quantum chemical calculations and binding mode analysis.
China Pharmaceutical University
Design and synthesis of tetracyclic nonpeptidic biaryl nitrile inhibitors of cathepsin K.
Celera Genomics
Non-peptidyl non-covalent cathepsin C inhibitoEEr bearing a unique thiophene-substituted pyridine: Design, structure-activity relationship and anti-inflammatory activity in vivo.
Anhui Medical University
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
The University of Sydney
Discovery and Crystallographic Studies of Nonpeptidic Piperazine Derivatives as Covalent SARS-CoV-2 Main Protease Inhibitors.
Shandong University
The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities.
Niddk
Novel, potent P2-P3 pyrrolidine derivatives of ketoamide-based cathepsin K inhibitors.
Glaxosmithkline
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
Ketoheterocycle-based inhibitors of cathepsin K: a novel entry into the synthesis of peptidic ketoheterocycles.
Glaxosmithkline
P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K.
Glaxosmithkline
A structural screening approach to ketoamide-based inhibitors of cathepsin K.
Glaxosmithkline
Discovery and Crystallographic Studies of Trisubstituted Piperazine Derivatives as Non-Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity and Low Toxicity.
Shandong University
Novel purine nitrile derived inhibitors of the cysteine protease cathepsin K.
Novartis Institutes For Biomedical Research
Ketoamide-based inhibitors of cysteine protease, cathepsin K: P3 modifications.
Glaxosmithkline
Potent and selective ketoamide-based inhibitors of cysteine protease, cathepsin K.
Glaxosmithkline
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
Orally bioavailable small molecule ketoamide-based inhibitors of cathepsin K.
Glaxosmithkline
Design and Structure-Activity Relationships of Isothiocyanates as Potent and Selective
Northeastern University
Design of potent, selective, and orally bioavailable inhibitors of cysteine protease cathepsin k.
Glaxosmithkline
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
3,4-disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P2 elements for selectivity.
Ligand Pharmaceuticals
Arylaminoethyl amides as inhibitors of the cysteine protease cathepsin K-investigating P1' substituents.
Novartis Pharma
N-Sulfonyl dipeptide nitriles as inhibitors of human cathepsin S: In silico design, synthesis and biochemical characterization.
University of Bonn
3-Acylamino-azetidin-2-one as a novel class of cysteine proteases inhibitors.
Currently Naeja 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
1,2,4-Thiadiazole acyclic nucleoside phosphonates as inhibitors of cysteine dependent enzymes cathepsin K and GSK-3β.
Charles University
Design, synthesis and stepwise optimization of nitrile-based inhibitors of cathepsins B and L.
University of S£O Paulo
Discovery and parallel synthesis of a new class of cathepsin K inhibitors.
Bayer Research Center
Green asymmetric synthesis of epoxypeptidomimetics and evaluation as human cathepsin K inhibitors.
Federal University of S£O Carlos
Diastereoselective synthesis, activity and chiral stability of cyclic alkoxyketone inhibitors of cathepsin K.
Smithkline Beecham Pharmaceuticals
Solid-phase synthesis of cyclic alkoxyketones, inhibitors of the cysteine protease cathepsin K.
Smithkline Beecham Pharmaceuticals
Novel, nonpeptidic cyanamides as potent and reversible inhibitors of human cathepsins K and L.
Merck Frosst Centre For Therapeutic Research
Design and synthesis of cyanamides as potent and selective N-acylethanolamine acid amidase inhibitors.
Northeastern University
Allosteric Modulator Discovery: From Serendipity to Structure-Based Design.
Shanghai Jiao-Tong University School of Medicine
Design and synthesis of diaminopyrrolidinone inhibitors of human osteoclast cathepsin K.
Smithkline Beecham Pharmaceuticals
Design, synthesis and biological evaluation of inhibitors of cathepsin K on dedifferentiated chondrocytes.
Jilin University
Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K.
Smithkline Beecham Pharmaceuticals
Proteases and Their Modulators in Cancer Therapy: Challenges and Opportunities.
Sichuan University
Identification of new peptide amides as selective cathepsin L inhibitors: the first step towards selective irreversible inhibitors?
National Institute of Biology
Natural inhibitors targeting osteoclast-mediated bone resorption.
Chinese Academy of Sciences
Substrate-derived triazolo- and azapeptides as inhibitors of cathepsins K and S.
Cnrs Upr 4301
Selective inhibition of human cathepsin S by 2,4,6-trisubstituted 1,3,5-triazine analogs.
Orleans University
Peptidomimetic nitrile inhibitors of malarial protease falcipain-2 with high selectivity against human cathepsins.
Irbm Science Park
Asymmetric synthesis and evaluation of epoxy-α-acyloxycarboxamides as selective inhibitors of cathepsin L.
Federal University of S£O Carlos
Design and synthesis of potent and orally active GPR4 antagonists with modulatory effects on nociception, inflammation, and angiogenesis.
Novartis Institutes For Biomedical Research
Discovery of Novel and Highly Selective Inhibitors of Calpain for the Treatment of Alzheimer's Disease: 2-(3-Phenyl-1H-pyrazol-1-yl)-nicotinamides.
Abbvie Deutschland
Pyranopyrazole and pyrazolopyridine immunomodulators for treatment of autoimmune diseases
Rockefeller University
Imidazopyrimidine and imidazotriazine derivative, and pharmaceutical composition comprising the same
Sk Biopharmaceuticals
Imidazopyrazine compounds, preparation methods and uses thereof
Dongguan Zhenxing-Beite Medicine Technology
Use of small molecule inhibitors targeting EYA tyrosine phosphatase
Cincinnati Childrens Hospital Medical Center
Substituted indazole derivatives active as kinase inhibitiors
Nerviano Medical Sciences
Piperidine substituted tricyclic pyrazolo[1,5-a]pyrimidine derivatives with inhibitory activity on the replication of the respiratory syncytial virus (RSV)
Janssen Ireland
Bicyclic heteroaryl derivatives as CFTR potentiators
Cystic Fibrosis Foundation Therapeutics
Substituted benzothiophenyl derivatives as GPR40 agonists for the treatment of type II diabetes
Janssen Pharmaceutica
Synthesis and biological evaluation of polyhydroxy benzophenone as mushroom tyrosinase inhibitors.
Sun Yat-Sen University
Substituted [1,2,4]triazolo[4,3-A]pyrazines that are BRD4 inhibitors
Boehringer Ingelheim International
Heteroarylimino-4-thiazolidinones as inhibitors of cartilage degradation.
University of Catania
Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1.
University of Toronto
Human gene S31 encodes the pharmacologically defined serotonin 5-hydroxytryptamine1E receptor.
Synaptic Pharmaceutical
Antagonism by antimuscarinic and neuroleptic compounds at the five cloned human muscarinic cholinergic receptors expressed in Chinese hamster ovary cells.
Mayo Clinic
Differential binding of inhibitors to active and inactive CDK2 provides insights for drug design.
Cyclacel
Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis.
Glaxosmithkline
Imidazo[1,2-b]pyridazines: a potent and selective class of cyclin-dependent kinase inhibitors.
Astrazeneca
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: identification and optimisation of substituted 2,4-bis anilino pyrimidines.
Astrazeneca
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines.
Astrazeneca
Cyclin-dependent kinase inhibition by new C-2 alkynylated purine derivatives and molecular structure of a CDK2-inhibitor complex.
Institut Curie
Cinnamaldehydes inhibit cyclin dependent kinase 4/cyclin D1.
Korea Research Institute of Bioscience and Biotechnology