126 articles for thisTarget
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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
Synthesis and binding monitoring of a new nanomolar PAMAM-based matrix metalloproteinases inhibitor (MMPIs).
University of Florence
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
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
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
Aggrecanase-2 inhibitors based on the acylthiosemicarbazide zinc-binding group.
University of Lille
Discovery of a New Class of Potent MMP Inhibitors by Structure-Based Optimization of the Arylsulfonamide Scaffold.
University of Florence
Matrix metalloproteinase inhibitors based on the 3-mercaptopyrrolidine core.
Florida State University
Optimization of peptide hydroxamate inhibitors of insulin-degrading enzyme reveals marked substrate-selectivity.
Mayo Clinic
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
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
Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
Johnson & Johnson Pharmaceutical Research & Development
Quinazolinones and pyrido[3,4-d]pyrimidin-4-ones as orally active and specific matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis.
Pfizer
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
Methotrexate gamma-hydroxamate derivatives as potential dual target antitumor drugs.
Instituto Superior T£Cnico
N-i-Propoxy-N-biphenylsulfonylaminobutylhydroxamic acids as potent and selective inhibitors of MMP-2 and MT1-MMP.
University of Pisa
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
Structure-activity relationships and pharmacokinetic analysis for a series of potent, systemically available biphenylsulfonamide matrix metalloproteinase inhibitors.
Parke-Davis Pharmaceutical Research
Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents.
F. Hoffmann-La Roche
Design, synthesis, and biological evaluation of potent thiazine- and thiazepine-based matrix metalloproteinase inhibitors.
Procter and Gamble Pharmaceuticals
Design and synthesis of phosphinamide-based hydroxamic acids as inhibitors of matrix metalloproteinases.
Procter and Gamble Pharmaceuticals
Discovery of potent, achiral matrix metalloproteinase inhibitors.
Procter and Gamble Pharmaceuticals
Heterocycle-based MMP inhibitors with P2' substituents.
Procter and Gamble Pharmaceuticals
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
Structure and activity relationships of tartrate-based TACE inhibitors.
Merck Research Laboratories
MMP-13 selectivea-sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.
Pfizer
2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors.
Merck Research Laboratories
Structure-based approach to nanomolar, water soluble matrix metalloproteinases inhibitors (MMPIs).
Protera
Novel TNF-a converting enzyme (TACE) inhibitors as potential treatment for inflammatory diseases.
Merck Research Laboratories
Orally bioavailable dual MMP-1/MMP-14 sparing, MMP-13 selective alpha-sulfone hydroxamates.
Pfizer
The discovery of novel tartrate-based TNF-alpha converting enzyme (TACE) inhibitors.
Schering-Plough Research Institute
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
The identification of beta-hydroxy carboxylic acids as selective MMP-12 inhibitors.
Gsk Medicines Research Centre
Regioselective synthesis of methylated epigallocatechin gallate via nitrobenzenesulfonyl (Ns) protecting group.
University of Shizuoka and Global Coe Program
Identification of an orally efficacious matrix metalloprotease 12 inhibitor for potential treatment of asthma.
Wyeth Research
Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors. Part II: optimization of the S3' pocket.
Schering-Plough Research Institute
Design, synthesis, activity, and structure of a novel class of matrix metalloproteinase inhibitors containing a heterocyclic P2′-P3′ amide bond isostere
TBA
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
University of Athens
Introduction of the 4-(4-bromophenyl)benzenesulfonyl group to hydrazide analogs of Ilomastat leads to potent gelatinase B (MMP-9) inhibitors with improved selectivity.
Université
Novel bis-(arylsulfonamide) hydroxamate-based selective MMP inhibitors.
North Dakota State University
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
Synthesis and structure-activity relationship of a novel, non-hydroxamate series of TNF-alpha converting enzyme inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-Based Optimization and Biological Evaluation of Potent and Selective MMP-7 Inhibitors for Kidney Fibrosis.
Taisho Pharmaceutical Co.
Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Bristol-Myers Squibb Pharmaceutical Research Institute
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
Discovery of TP0597850: A Selective, Chemically Stable, and Slow Tight-Binding Matrix Metalloproteinase-2 Inhibitor with a Phenylbenzamide-Pentapeptide Hybrid Scaffold.
Taisho Pharmaceutical Co.
Hydroxypyrone derivatives in drug discovery: from chelation therapy to rational design of metalloenzyme inhibitors.
Government College Women University
alpha-Biphenylsulfonylamino 2-methylpropyl phosphonates: enantioselective synthesis and selective inhibition of MMPs.
Università
Matrix metalloproteinases inhibitors in idiopathic pulmonary fibrosis: Medicinal chemistry perspectives.
Sichuan University-University of Oxford Huaxi Joint Centre For Gastrointestinal Cancer
Outline of gelatinase inhibitors as anti-cancer agents: A patent mini-review for 2010-present.
Jadavpur University
Targeting Aggrecanases for Osteoarthritis Therapy: From Zinc Chelation to Exosite Inhibition.
University of Pisa
Matrix metalloproteinase-9 (MMP-9) and its inhibitors in cancer: A minireview.
Jadavpur University
Discovery of low nanomolar non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Bristol-Myers Squibb Pharmaceutical Research Institute
Inhibitors of gelatinases (MMP-2 and MMP-9) for the management of hematological malignancies.
Jadavpur University
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
Synthesis and evaluation of succinoyl-caprolactam gamma-secretase 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
Discovery of Phenolic Matrix Metalloproteinase Inhibitors by Peptide Microarray for Osteosarcoma Treatment.
Chinese Academy of Sciences
Selective Inhibitors of Medium-Size S1' Pocket Matrix Metalloproteinases: A Stepping Stone of Future Drug Discovery.
Jadavpur University
-Aryl mercaptoacetamides as potential multi-target inhibitors of metallo-β-lactamases (MBLs) and the virulence factor LasB from
Helmholtz Institute For Pharmaceutical Research Saarland (Hips)
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
Tetrahydroisoquinoline based sulfonamide hydroxamates as potent matrix metalloproteinase inhibitors.
Chinese Academy of Sciences
A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers.
Pfizer
Synthesis of radiolabeled biphenylsulfonamide matrix metalloproteinase inhibitors as new potential PET cancer imaging agents.
Indiana University School of Medicine
Amide Bond Bioisosteres: Strategies, Synthesis, and Successes.
University of Nebraska Medical Center
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
Hydroxamate-Based Selective Macrophage Elastase (MMP-12) Inhibitors and Radiotracers for Molecular Imaging.
Yale University
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
Matrix Metalloproteinases as New Targets in Alzheimer's Disease: Opportunities and Challenges.
Normandie Univ
Asymmetric synthesis of BB-3497--a potent peptide deformylase inhibitor.
British Biotech Pharmaceuticals
The development of new carboxylic acid-based MMP inhibitors derived from a cyclohexylglycine scaffold.
Procter and Gamble Pharmaceuticals
Discovery and characterization of the potent, selective and orally bioavailable MMP inhibitor ABT-770.
Abbott Laboratories
Novel 5,5-disubstitutedpyrimidine-2,4,6-triones as selective MMP inhibitors.
Roche Research Center
Development of new hydroxamate matrix metalloproteinase inhibitors derived from functionalized 4-aminoprolines.
Procter and Gamble Pharmaceuticals
Use of Osmotic Pumps to Establish the Pharmacokinetic-Pharmacodynamic Relationship and Define Desirable Human Performance Characteristics for Aggrecanase Inhibitors.
Eli Lilly
Design and synthesis of piperazine-based matrix metalloproteinase inhibitors.
Procter and Gamble Pharmaceuticals
Design, synthesis, and biological evaluation of matrix metalloproteinase inhibitors derived from a modified proline scaffold.
University of Florida
Phosphinic pseudo-tripeptides as potent inhibitors of matrix metalloproteinases: a structure-activity study.
Cea
Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors.
Abbott Laboratories
The design, synthesis, and structure-activity relationships of a series of macrocyclic MMP inhibitors.
Abbott Laboratories
Rational design and combinatorial evaluation of enzyme inhibitor scaffolds: identification of novel inhibitors of matrix metalloproteinases.
Affymax Research Institute
Highly selective and orally active inhibitors of type IV collagenase (MMP-9 and MMP-2): N-sulfonylamino acid derivatives.
Shionogi
Discovery and process development of a novel TACE inhibitor for the topical treatment of psoriasis.
Nestle Skin Health
Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry.
St. John'S University
Isoindolinone substituted indoles and derivatives as RAS inhibitors
Boehringer Ingelheim International
Imidazolin-5-one derivative useful as FASN inhibitors for the treatment of cancer
Janssen Pharmaceutica
CARBOXYLIC ACID AROMATIC AMIDES AS ANTAGONISTS OF BRADYKININ B1 RECEPTOR
Bayer Pharma Aktiengesellschaft
Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase
North Carolina Central University