PMID

Data

Article Title

Organization

A Highly Selective Hydantoin Inhibitor of Aggrecanase-1 and Aggrecanase-2 with a Low Projected Human Dose.

Eli Lilly

Identification of novel TACE inhibitors compatible with topical application.

Nestl�

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

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

Imidazopyridines as a source of biological activity and their pharmacological potentials-Infrared and Raman spectroscopic evidence of their content in pharmaceuticals and plant materials.

Wroclaw University of Economics

A dual inhibitor of matrix metalloproteinases and a disintegrin and metalloproteinases, [¹8F]FB-ML5, as a molecular probe for non-invasive MMP/ADAM-targeted imaging.

University Medical Center Groningen

Targeting matrix metalloproteinases: exploring the dynamics of the s1' pocket in the design of selective, small molecule inhibitors.

Universidad Ceu San Pablo

Investigating the selectivity of metalloenzyme inhibitors.

University of California San Diego

Aggrecanase-2 inhibitors based on the acylthiosemicarbazide zinc-binding group.

University of Lille

Hydantoin based inhibitors of MMP13--discovery of AZD6605.

Astrazeneca

Discovery of a New Class of Potent MMP Inhibitors by Structure-Based Optimization of the Arylsulfonamide Scaffold.

University of Florence

Synthesis of derivatives of methyl rosmarinate and their inhibitory activities against matrix metalloproteinase-1 (MMP-1).

Second Military Medical University

Sulphonamides: Deserving class as MMP inhibitors?

Indian Institute of Technology (Bhu)

Synthesis and preliminary evaluation in tumor bearing mice of new (18)F-labeled arylsulfone matrix metalloproteinase inhibitors as tracers for positron emission tomography.

Universit£

Molecular determinants of a selective matrix metalloprotease-12 inhibitor: insights from crystallography and thermodynamic studies.

Cea

Matrix metalloproteinases (MMPs): chemical-biological functions and (Q)SARs.

Pomona College

Selective non zinc binding inhibitors of MMP13.

Astrazeneca

Target-Activated Prodrugs (TAPs) for the Autoregulated Inhibition of MMP12.

TBA

A one-pot synthesis and biological activity of ageladine A and analogues.

Macquarie University

Natural products as a gold mine for selective matrix metalloproteinases inhibitors.

East China University of Science and 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

Antidotes to anthrax lethal factor intoxication. Part 3: Evaluation of core structures and further modifications to the C2-side chain.

Panthera Biopharma

Discovery of (7R)-14-cyclohexyl-7-{[2-(dimethylamino)ethyl](methyl) amino}-7,8-dihydro-6H-indolo[1,2-e][1,5]benzoxazocine-11-carboxylic acid (MK-3281), a potent and orally bioavailable finger-loop inhibitor of the hepatitis C virus NS5B polymerase.

P. Angeletti S.P.A. (Merck Research Laboratories)

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

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

Synthesis and evaluation of novel heterocyclic MMP inhibitors.

North Dakota State University

Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents.

F. Hoffmann-La Roche

Pyran-containing sulfonamide hydroxamic acids: potent MMP inhibitors that spare MMP-1.

Pfizer

Phosphinic acid-based MMP-13 inhibitors that spare MMP-1 and MMP-3.

Pfizer

In silico scaffold evaluation and solid phase approach to identify new gelatinase inhibitors.

Colosseum Combinatorial Chemistry Centre For Technology (C4T Scarl)

Potent inhibitors of LpxC for the treatment of Gram-negative infections.

Pfizer

Lead optimisation of selective non-zinc binding inhibitors of MMP13. Part 2.

Astrazeneca

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

Improvement in aqueous solubility in small molecule drug discovery programs by disruption of molecular planarity and symmetry.

The University of Tokyo

Thiophene and bioisostere derivatives as new MMP12 inhibitors.

Evotec Oai

Structure-based approach to nanomolar, water soluble matrix metalloproteinases inhibitors (MMPIs).

Protera

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

Synthesis of novel ageladine A analogs showing more potent matrix metalloproteinase (MMP)-12 inhibitory activity than the natural product.

Kyorin Pharmaceutical

The identification of beta-hydroxy carboxylic acids as selective MMP-12 inhibitors.

Gsk Medicines Research Centre

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-((8-hydroxy-5-substituted-quinolin-7-yl)(phenyl)methyl)-2-phenyloxy/amino-acetamide inhibitors of ADAMTS-5 (Aggrecanase-2).

Wyeth Research

Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.

University of Athens

Identification of MMP-12 inhibitors by using biosensor-based screening of a fragment library.

Uppsala University

Discovery and characterization of a novel inhibitor of matrix metalloprotease-13 that reduces cartilage damage in vivo without joint fibroplasia side effects.

Pfizer

Platinum complexes can inhibit matrix metalloproteinase activity: platinum-diethyl[(methylsulfinyl)methyl]phosphonate complexes as inhibitors of matrix metalloproteinases 2, 3, 9, and 12.

Università

Synthesis and structure-activity relationship of a novel, non-hydroxamate series of TNF-alpha converting enzyme inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Synthesis and matrix metalloproteinase (MMP)-12 inhibitory activity of ageladine A and its analogs.

Kyorin Pharmaceutical

Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of low nanomolar non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

Bristol-Myers Squibb Pharmaceutical Research Institute

Selective inhibition of matrix metalloproteinase isozymes and in vivo protection against emphysema by substituted gamma-keto carboxylic acids.

Chinese Academy of Sciences

Structure-based design and synthesis of novel non-zinc chelating MMP-12 inhibitors.

Pfizer

Potent pyrimidinetrione-based inhibitors of MMP-13 with enhanced selectivity over MMP-14.

Pfizer

Synthesis and evaluation of novel oxazoline MMP inhibitors.

North Dakota State University

3-Hydroxy-4-arylsulfonyltetrahydropyranyl-3-hydroxamic acids are novel inhibitors of MMP-13 and aggrecanase.

Pfizer

Tetrahydroisoquinoline based sulfonamide hydroxamates as potent matrix metalloproteinase inhibitors.

Chinese Academy of Sciences

Development of a water-soluble matrix metalloproteinase inhibitor as an intra-arterial infusion drug for prevention of restenosis after angioplasty.

National Cardiovascular Center Research Institute

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

Structure-based design and synthesis of potent matrix metalloproteinase inhibitors derived from a 6H-1,3,4-thiadiazine scaffold.

UniversitäT Bielefeld

2-(2-Oxo-1,4-dihydro-2H-quinazolin-3-yl)- and 2-(2,2-dioxo-1,4-dihydro-2H-2lambda6-benzo[1,2,6]thiadiazin-3-yl)-N-hydroxy-acetamides as potent and selective peptide deformylase inhibitors.

F. Hoffmann-La Roche

Synthesis and Structural/Functional Characterization of Selective M14 Metallocarboxypeptidase Inhibitors Based on Phosphinic Pseudopeptide Scaffold: Implications on the Design of Specific Optical Probes.

Universitat Aut£Noma De Barcelona

Targeted Treatments for Chronic Obstructive Pulmonary Disease (COPD) Using Low-Molecular-Weight Drugs (LMWDs).

School of Pharmaceutical Sciences & The Fifth Affiliated Hospital

Recent developments in the synthesis and applications of phosphinic peptide analogs.

Wroclaw University of Technology

Matrix metalloproteinase-12 inhibitors: synthesis, structure-activity relationships and intestinal absorption of novel sugar-based biphenylsulfonamide carboxylates.

University of Pisa

Reverse Hydroxamate Inhibitors of Bone Morphogenetic Protein 1.

Glaxosmithkline Pharmaceuticals

Development of Thioaryl-Based Matrix Metalloproteinase-12 Inhibitors with Alternative Zinc-Binding Groups: Synthesis, Potentiometric, NMR, and Crystallographic Studies.

Universit£

Discovery and process development of a novel TACE inhibitor for the topical treatment of psoriasis.

Nestl�

Synthesis of radioiodinated probes targeted toward matrix metalloproteinase-12.

Kobe Pharmaceutical University

Development of matrix metalloproteinase-13 inhibitors - A structure-activity/structure-property relationship study.

Graz University of Technology

In Search of Selectivity in Inhibition of ADAM10.

University of Notre Dame

HTS by NMR for the Identification of Potent and Selective Inhibitors of Metalloenzymes.

University of California-Riverside

A pentanoic acid derivative targeting matrix metalloproteinase-2 (MMP-2) induces apoptosis in a chronic myeloid leukemia cell line.

Jadavpur University

Lipoyl-Homotaurine Derivative (ADM_12) Reverts Oxaliplatin-Induced Neuropathy and Reduces Cancer Cells Malignancy by Inhibiting Carbonic Anhydrase IX (CAIX).

University of Florence

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

Pharmacologic characterization of the human 5-hydroxytryptamine2B receptor: evidence for species differences.

Eli Lilly

Development of a radioligand binding assay for 5-HT4 receptors in guinea-pig and rat brain.

Glaxo Group Research

Characterization of (+/-)(-)[3H]epibatidine binding to nicotinic cholinergic receptors in rat and human brain.

Georgetown University

Cloning and expression of a 5-hydroxytryptamine7 receptor positively coupled to adenylyl cyclase.

Syntex Discovery Research