141 articles for thisTarget
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Article Title
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Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach.
Pharmaceutical
Design, synthesis, and biological activity of novel, potent, and highly selective fused pyrimidine-2-carboxamide-4-one-based matrix metalloproteinase (MMP)-13 zinc-binding inhibitors.
Takeda Pharmaceutical
Robust design of some selective matrix metalloproteinase-2 inhibitors over matrix metalloproteinase-9 through in silico/fragment-based lead identification and de novo lead modification: Syntheses and biological assays.
Jadavpur University
Discovery of N-(4-Fluoro-3-methoxybenzyl)-6-(2-(((2S,5R)-5-(hydroxymethyl)-1,4-dioxan-2-yl)methyl)-2H-tetrazol-5-yl)-2-methylpyrimidine-4-carboxamide. A Highly Selective and Orally Bioavailable Matrix Metalloproteinase-13 Inhibitor for the Potential Treatment of Osteoarthritis.
Pfizer
Design and synthesis of an activity-based protein profiling probe derived from cinnamic hydroxamic acid.
University of Minnesota
SAR Studies of Exosite-Binding Substrate-Selective Inhibitors of A Disintegrin And Metalloprotease 17 (ADAM17) and Application as Selective in Vitro Probes.
Florida Atlantic University
Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach.
Takeda Pharmaceutical
Targeting matrix metalloproteinases: exploring the dynamics of the s1' pocket in the design of selective, small molecule inhibitors.
Universidad Ceu San Pablo
Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1¿ binding site.
Takeda Pharmaceutical
O-phenyl carbamate and phenyl urea thiiranes as selective matrix metalloproteinase-2 inhibitors that cross the blood-brain barrier.
University of Notre Dame
Matrix metalloproteinases (MMPs): chemical-biological functions and (Q)SARs.
Pomona College
Remarkable potential of thea-aminophosphonate/phosphinate structural motif in medicinal chemistry.
Wroclaw University of Technology
A one-pot synthesis and biological activity of ageladine A and analogues.
Macquarie University
Design, synthesis and biological evaluation of 5-hydroxy, 5-substituted-pyrimidine-2,4,6-triones as potent inhibitors of gelatinases MMP-2 and MMP-9.
Universit£
A new class of highly potent matrix metalloproteinase inhibitors based on triazole-substituted hydroxamates: (radio)synthesis and in vitro and first in vivo evaluation.
University Hospital M£Nster
Discovery and evaluation of a non-Zn chelating, selective matrix metalloproteinase 13 (MMP-13) inhibitor for potential intra-articular treatment of osteoarthritis.
Alantos Pharmaceuticals
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.
University of Florida
Carbamoylphosphonate matrix metalloproteinase inhibitors 6: cis-2-aminocyclohexylcarbamoylphosphonic acid, a novel orally active antimetastatic matrix metalloproteinase-2 selective inhibitor--synthesis and pharmacodynamic and pharmacokinetic analysis.
The Hebrew University of Jerusalem
Alpha,beta-cyclic-beta-benzamido hydroxamic acids: novel templates for the design, synthesis, and evaluation of selective inhibitors of TNF-alpha converting enzyme (TACE).
Bristol-Myers Squibb Research and Development
Novel fluorinated derivatives of the broad-spectrum MMP inhibitors N-hydroxy-2(R)-[[(4-methoxyphenyl)sulfonyl](benzyl)- and (3-picolyl)-amino]-3-methyl-butanamide as potential tools for the molecular imaging of activated MMPs with PET.
University Hospital of The Westf£Lische Wilhelms-Universit£T M£Nster
N-i-Propoxy-N-biphenylsulfonylaminobutylhydroxamic acids as potent and selective inhibitors of MMP-2 and MT1-MMP.
Universit£
Carbamoylphosphonates, a new class of in vivo active matrix metalloproteinase inhibitors. 1. Alkyl- and cycloalkylcarbamoylphosphonic acids.
The Hebrew University of Jerusalem
Synthesis and structure-activity relationship of N-substituted 4-arylsulfonylpiperidine-4-hydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis.
Wyeth Research
Design, synthesis, and structure-activity relationships of macrocyclic hydroxamic acids that inhibit tumor necrosis factor alpha release in vitro and in vivo.
Dupont Pharmaceuticals
Potent and selective carboxylic acid-based inhibitors of matrix metalloproteinases.
TBA
Design, synthesis, and biological evaluation of potent thiazine- and thiazepine-based matrix metalloproteinase inhibitors.
Procter and Gamble Pharmaceuticals
Quantitative structure-activity relationship of human neutrophil collagenase (MMP-8) inhibitors using comparative molecular field analysis and X-ray structure analysis.
Hoechst Marion Roussel
Design and synthesis of phosphinamide-based hydroxamic acids as inhibitors of matrix metalloproteinases.
Procter and Gamble Pharmaceuticals
Pyran-containing sulfonamide hydroxamic acids: potent MMP inhibitors that spare MMP-1.
Pfizer
Heterocycle-based MMP inhibitors with P2' substituents.
Procter and Gamble Pharmaceuticals
Arylsulphonyl hydroxamic acids: potent and selective matrix metalloproteinase inhibitors.
Celltech-Chiroscience
In silico scaffold evaluation and solid phase approach to identify new gelatinase inhibitors.
Colosseum Combinatorial Chemistry Centre For Technology (C4T Scarl)
A new generation of radiofluorinated pyrimidine-2,4,6-triones as MMP-targeted radiotracers for positron emission tomography.
University Hospital M£Nster
Identification of novel, exosite-binding matrix metalloproteinase-13 inhibitor scaffolds.
Scripps Florida
Fragment-based discovery of indole inhibitors of matrix metalloproteinase-13.
Boehringer Ingelheim Pharmaceuticals
Novel 1-hydroxypiperazine-2,6-diones as new leads in the inhibition of metalloproteinases.
Instituto Superior T£Cnico
Discovery of potent and selective matrix metalloprotease 12 inhibitors for the potential treatment of chronic obstructive pulmonary disease (COPD).
Pfizer
Orally active MMP-1 sparinga-tetrahydropyranyl anda-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
Pfizer
Synthesis and biological evaluation in U87MG glioma cells of (ethynylthiophene)sulfonamido-based hydroxamates as matrix metalloproteinase inhibitors.
Universit£
MMP-13 selectivea-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.
Pfizer
MMP-13 selective alpha-sulfone hydroxamates: identification of selective P1' amides.
Pfizer
Structure-based approach to nanomolar, water soluble matrix metalloproteinases inhibitors (MMPIs).
Protera
Orally bioavailable dual MMP-1/MMP-14 sparing, MMP-13 selective alpha-sulfone hydroxamates.
Pfizer
Discovery of (pyridin-4-yl)-2H-tetrazole as a novel scaffold to identify highly selective matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis.
Pfizer
Design, synthesis, biological evaluation, and NMR studies of a new series of arylsulfones as selective and potent matrix metalloproteinase-12 inhibitors.
Universit£
Identification of an orally efficacious matrix metalloprotease 12 inhibitor for potential treatment of asthma.
Wyeth Research
N-O-isopropyl sulfonamido-based hydroxamates: design, synthesis and biological evaluation of selective matrix metalloproteinase-13 inhibitors as potential therapeutic agents for osteoarthritis.
Universit£
Mercaptoacyl matrix metalloproteinase inhibitors: The effect of substitution at the mercaptoacyl moiety
TBA
Hydroxamate inhibitors of the matrix metallo-proteinases (MMPs) containing novel P1′ heteroatom based modifications
TBA
Dual inhibitors of matrix metalloproteinases and carbonic anhydrases: iminodiacetyl-based hydroxamate-benzenesulfonamide conjugates.
Instituto Superior TéCnico
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
University of Athens
Ranking the selectivity of PubChem screening hits by activity-based protein profiling: MMP13 as a case study.
The Scripps Research Institute
Peptidyl 3-substituted 1-hydroxyureas as isosteric analogues of succinylhydroxamate MMP inhibitors.
Università
Discovery and characterization of a novel inhibitor of matrix metalloprotease-13 that reduces cartilage damage in vivo without joint fibroplasia side effects.
Pfizer
Simultaneous presence of unsaturation and long alkyl chain at P'1 of Ilomastat confers selectivity for gelatinase A (MMP-2) over gelatinase B (MMP-9) inhibition as shown by molecular modelling studies.
Université
A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1' group for the beta-amino hydroxamic acid derived TACE inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and in vitro evaluation of targeted tetracycline derivatives: effects on inhibition of matrix metalloproteinases.
Clermont Auvergne University
alpha-Biphenylsulfonylamino 2-methylpropyl phosphonates: enantioselective synthesis and selective inhibition of MMPs.
Università
Discovery of Aryloxyphenyl-Heptapeptide Hybrids as Potent and Selective Matrix Metalloproteinase-2 Inhibitors for the Treatment of Idiopathic Pulmonary Fibrosis.
Taisho Pharmaceutical
Synthesis and structure-activity relationship of a novel, achiral series of TNF-alpha converting enzyme inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Matrix metalloproteinase target family landscape: a chemometrical approach to ligand selectivity based on protein binding site analysis.
Aventis Pharma Deutschland
N-Hydroxyurea as zinc binding group in matrix metalloproteinase inhibition: mode of binding in a complex with MMP-8.
Università
Structure-based design and synthesis of novel non-zinc chelating MMP-12 inhibitors.
Pfizer
Discovery of 3-OH-3-methylpipecolic hydroxamates: potent orally active inhibitors of aggrecanase and MMP-13.
Pfizer
Selective Inhibitors of Medium-Size S1' Pocket Matrix Metalloproteinases: A Stepping Stone of Future Drug Discovery.
Jadavpur University
Potent pyrimidinetrione-based inhibitors of MMP-13 with enhanced selectivity over MMP-14.
Pfizer
QSAR-by-NMR: quantitative insights into structural determinants for binding affinity by analysis of 1H/15N chemical shift differences in MMP-3 ligands.
Aventis Pharma Deutschland
-Aryl mercaptoacetamides as potential multi-target inhibitors of metallo-?-lactamases (MBLs) and the virulence factor LasB from
Helmholtz Institute For Pharmaceutical Research Saarland (Hips)
Discovery and Characterization of Synthesized and FDA-Approved Inhibitors of Clostridial and Bacillary Collagenases.
Helmholtz Center For Infection Research (Hzi)
Discovery of Highly Potent and Selective Matrix Metalloproteinase-7 Inhibitors by Hybridizing the S1' Subsite Binder with Short Peptides.
Taisho Pharmaceutical
Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis.
Galapagos
Development of a selective matrix metalloproteinase 13 (MMP-13) inhibitor for the treatment of Osteoarthritis.
Bolderbiopath
Evaluation of P1'-diversified phosphinic peptides leads to the development of highly selective inhibitors of MMP-11.
University of Athens
Novel inhibitors of procollagen C-proteinase. Part 2: glutamic acid hydroxamates.
Combichem
Discovery of 7-aminophenanthridin-6-one as a new scaffold for matrix metalloproteinase inhibitors with multitarget neuroprotective activity.
Universidad Complutense
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
Bristol-Myers Squibb
Oxal hydroxamic acid derivatives with inhibitory activity against matrix metalloproteinases.
University of Bielefeld
Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors.
Abbott Laboratories
Discovery of macrocyclic hydroxamic acids containing biphenylmethyl derivatives at P1', a series of selective TNF-alpha converting enzyme inhibitors with potent cellular activity in the inhibition of TNF-alpha release.
Dupont Pharmaceuticals
Design and synthesis of a series of (2R)-N(4)-hydroxy-2-(3-hydroxybenzyl)-N(1)- [(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide derivatives as potent, selective, and orally bioavailable aggrecanase inhibitors.
Dupont Pharmaceuticals
Structure-based design and synthesis of potent matrix metalloproteinase inhibitors derived from a 6H-1,3,4-thiadiazine scaffold.
UniversitäT Bielefeld
Novel 5,5-disubstitutedpyrimidine-2,4,6-triones as selective MMP inhibitors.
Roche Research Center
Virtual screening identification and chemical optimization of substituted 2-arylbenzimidazoles as new non-zinc-binding MMP-2 inhibitors.
"A. Moro" University of Bari
Validating the 1,2-Difluoro Motif As a Hybrid Bioisostere of CF
Westf£Lische Wilhelms-Universit£T M£Nster
Protease inhibitors: synthesis of potent bacterial collagenase and matrix metalloproteinase inhibitors incorporating N-4-nitrobenzylsulfonylglycine hydroxamate moieties.
Università
New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors.
Astrazeneca
Affinity and selectivity of matrix metalloproteinase inhibitors: a chemometrical study from the perspective of ligands and proteins.
Hoechst Marion Roussel
The synthesis and biological evaluation of non-peptidic matrix metalloproteinase inhibitors.
British Biotech Pharmaceuticals
Phosphinic pseudo-tripeptides as potent inhibitors of matrix metalloproteinases: a structure-activity study.
Cea
Proline-based hydroxamates targeting the zinc-dependent deacetylase LpxC: Synthesis, antibacterial properties, and docking studies.
University of Hamburg
Synthesis and identification of conformationally constrained selective MMP inhibitors.
Searle Discovery Research
P1, P2'-linked macrocyclic amine derivatives as matrix metalloproteinase inhibitors.
Dupont Pharmaceuticals
Discovery of a novel series of selective MMP inhibitors: identification of the gamma-sulfone-thiols.
Searle Discovery Research
Bis-substituted malonic acid hydroxamate derivatives as inhibitors of human neutrophil collagenase (MMP8).
Boehringer Mannheim
Design and synthesis of malonic acid-based inhibitors of human neutrophil collagenase (MMP8).
Institut FüR Biochemie
Dihydropyrazothiazole derivatives as potential MMP-2/MMP-8 inhibitors for cancer therapy.
Nanjing Agricultural University
Recent developments in the synthesis and applications of phosphinic peptide analogs.
Wroclaw University of Technology
Fluorinated matrix metalloproteinases inhibitors--Phosphonate based potential probes for positron emission tomography.
Westf£Lische Wilhelms-Universit£T
Inverse 1,2,3-triazole-1-yl-ethyl substituted hydroxamates as highly potent matrix metalloproteinase inhibitors: (radio)synthesis, in vitro and first in vivo evaluation.
University Hospital M£Nster
Inhibition of matrix metalloproteinases by hydroxamates containing heteroatom-based modifications of the P1' group.
Sterling Winthrop Pharmaceuticals Research Division
Validation of Matrix Metalloproteinase-9 (MMP-9) as a Novel Target for Treatment of Diabetic Foot Ulcers in Humans and Discovery of a Potent and Selective Small-Molecule MMP-9 Inhibitor That Accelerates Healing.
University of Notre Dame
Discovery of dehydroabietic acid sulfonamide based derivatives as selective matrix metalloproteinases inactivators that inhibit cell migration and proliferation.
Southeast University
Discovery and process development of a novel TACE inhibitor for the topical treatment of psoriasis.
Nestl�
Development of matrix metalloproteinase-13 inhibitors - A structure-activity/structure-property relationship study.
Graz University of Technology
A pentanoic acid derivative targeting matrix metalloproteinase-2 (MMP-2) induces apoptosis in a chronic myeloid leukemia cell line.
Jadavpur University
Exploitation of Conformational Dynamics in Imparting Selective Inhibition for Related Matrix Metalloproteinases.
University of Notre Dame
Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry.
St. John'S University
Structure-Based Design and Synthesis of Potent and Selective Matrix Metalloproteinase 13 Inhibitors.
Scripps Florida
Design, synthesis and pharmacological evaluation of conformationally restricted N-arylsulfonyl-3-aminoalkoxy indoles as a potential 5-HT6 receptor ligands.
Suven Life Sciences
Tyrosinase inhibition: conformational analysis based studies on molecular dynamics calculations of bipiperidine based inhibitors.
University of Karachi
Pharmacologic characterization of the human 5-hydroxytryptamine2B receptor: evidence for species differences.
Eli Lilly
Cloning and pharmacologic characterization of a thromboxane A2 receptor from K562 (human chronic myelogenous leukemia) cells.
University of Cincinnati
Characterization of (+/-)(-)[3H]epibatidine binding to nicotinic cholinergic receptors in rat and human brain.
Georgetown University
Actions of phenylglycine analogs at subtypes of the metabotropic glutamate receptor family.
Novo Nordisk
Pharmacological profile of FK480, a novel cholecystokinin type-A receptor antagonist: comparison to loxiglumide.
Fujisawa Pharmaceutical
Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc.
Chemical Genomics Centre of The Max Planck Society
Small-molecule inhibitors of the MDM2-p53 protein-protein interaction based on an isoindolinone scaffold.
University of Newcastle Upon Tyne