PMID

Data

Article Title

Organization

Identification of novel TACE inhibitors compatible with topical application.

Nestl�

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

Bifunctional Inhibitors as a New Tool To Reduce Cancer Cell Invasion by Impairing MMP-9 Homodimerization.

Universit£

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

Selective non-zinc binding MMP-2 inhibitors: Novel benzamide Ilomastat analogs with anti-tumor metastasis.

Fudan University

Discovery of a new selective inhibitor of A Disintegrin And Metalloprotease 10 (ADAM-10) able to reduce the shedding of NKG2D ligands in Hodgkin's lymphoma cell models.

San Raffaele Scientific Institute

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

Synthesis, experimental evaluation and molecular modelling of hydroxamate derivatives as zinc metalloproteinase inhibitors.

Uit The Arctic University Of Norway

Sulfonamide derivatives containing dihydropyrazole moieties selectively and potently inhibit MMP-2/MMP-9: Design, synthesis, inhibitory activity and 3D-QSAR analysis.

Nanjing University

Synthesis of chiral ND-322, ND-364 and ND-364 derivatives as selective inhibitors of human gelatinase.

Shandong University

N-O-Isopropyl Sulfonamido-Based Hydroxamates as Matrix Metalloproteinase Inhibitors: Hit Selection and in Vivo Antiangiogenic Activity.

Universit£

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

New matrix metalloproteinase inhibitors based on¿-fluorinateda-aminocarboxylic anda-aminohydroxamic acids.

Westf£Lische Wilhelms-Universit£T M£Nster

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

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

Synthesis and structure-activity relationship analysis of caffeic acid amides as selective matrix metalloproteinase inhibitors.

Nanjing University Of Chinese Medicine

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£

MMP inhibition by barbiturate homodimers.

Trinity College

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

Pomona College

Selective non zinc binding inhibitors of MMP13.

Astrazeneca

Design and synthesis of procollagen C-proteinase inhibitors.

Fibrogen

Synopsis of some recent tactical application of bioisosteres in drug design.

Bristol-Myers Squibb Pharmaceutical Research And Development

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

Design of barbiturate-nitrate hybrids that inhibit MMP-9 activity and secretion.

Trinity College

Structure-Activity Relationship for Thiirane-Based Gelatinase Inhibitors.

TBA

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

The impact of ionization States of matrix metalloproteinase inhibitors on docking-based inhibitor design.

TBA

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

Panthera Biopharma

Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.

University Of Florida

Discovery of novel selective HER-2 sheddase inhibitors through optimization of P1 moiety.

Incyte

Synthesis and biological evaluation of curcuminoid pyrazoles as new therapeutic agents in inflammatory bowel disease: effect on matrix metalloproteinases.

Uned

Current perspective of TACE inhibitors: a review.

The M. S. University Of Baroda

1-Hydroxy-2-pyridinone-based MMP inhibitors: synthesis and biological evaluation for the treatment of ischemic stroke.

Johnson & Johnson Pharmaceutical Research And Development

Syntheses and in vitro evaluation of arylsulfone-based MMP inhibitors with heterocycle-derived zinc-binding groups (ZBGs).

Johnson & Johnson Pharmaceutical Research And Development

beta-N-Biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors: part 1. Design, synthesis, and lead identification.

Johnson & Johnson Pharmaceutical Research And Development

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

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

Methotrexate gamma-hydroxamate derivatives as potential dual target antitumor drugs.

Instituto Superior T£Cnico

Carbonic anhydrase and matrix metalloproteinase inhibitors. Inhibition of human tumor-associated isozymes IX and cytosolic isozyme I and II with sulfonylated hydroxamates.

Universit£

C-5-disubstituted barbiturates as potential molecular probes for noninvasive matrix metalloproteinase imaging.

University Hospital Of The Westf£Lische Wilhelms-Universit£T

N-i-Propoxy-N-biphenylsulfonylaminobutylhydroxamic acids as potent and selective inhibitors of MMP-2 and MT1-MMP.

Universit£

N-hydroxy-2-(naphthalene-2-ylsulfanyl)-acetamide, a novel hydroxamic acid-based inhibitor of aminopeptidase N and its anti-angiogenic activity.

Sejong University

Fragment-based drug discovery.

Sunesis Pharmaceuticals

Carbamoylphosphonates, a new class of in vivo active matrix metalloproteinase inhibitors. 1. Alkyl- and cycloalkylcarbamoylphosphonic acids.

The Hebrew University Of Jerusalem

Stereospecific synthesis of 5-substituted 2-bisarylthiocyclopentane carboxylic acids as specific matrix metalloproteinase inhibitors.

Institut De Recherches Servier

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

Synthesis and structure-activity relationship of alpha-sulfonylhydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis.

Wyeth Research

New type of metalloproteinase inhibitor: design and synthesis of new phosphonamide-based hydroxamic acids.

Nippon Organon K.K.

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

Protease inhibitors: current status and future prospects.

University Of Queensland

Structure-activity relationships and pharmacokinetic analysis for a series of potent, systemically available biphenylsulfonamide matrix metalloproteinase inhibitors.

Parke-Davis Pharmaceutical Research

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

New heteroarylbenzenesulphonamides as matrix metalloproteinase inhibitors.

Universit£

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

Pfizer

Heterocycle-based MMP inhibitors with P2' substituents.

Procter And Gamble Pharmaceuticals

The discovery of anthranilic acid-based MMP inhibitors. Part 3: incorporation of basic amines.

Wyeth-Ayerst Research

Heteroaryl and cycloalkyl sulfonamide hydroxamic acid inhibitors of matrix metalloproteinases.

Wyeth-Ayerst Research

The discovery of anthranilic acid-based MMP inhibitors. Part 1: SAR of the 3-position.

Wyeth-Ayerst Research

The discovery of anthranilic acid-based MMP inhibitors. Part 2: SAR of the 5-position and P1(1) groups.

Wyeth-Ayerst Research

Arylsulphonyl hydroxamic acids: potent and selective matrix metalloproteinase inhibitors.

Celltech-Chiroscience

Macrocyclic hydroxamate inhibitors of matrix metalloproteinases and TNF-alpha production.

Dupont Pharmaceuticals

Synthesis of an array of potential matrix metalloproteinase inhibitors using a sequence of polymer-supported reagents.

University Of Cambridge

Picking the S1, S1' and S2' pockets of matrix metalloproteinases. A niche for potent acyclic sulfonamide inhibitors.

Universit£

The synthesis and biological activity of a novel series of diazepine MMP inhibitors.

Wyeth-Ayerst Research

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

A new generation of radiofluorinated pyrimidine-2,4,6-triones as MMP-targeted radiotracers for positron emission tomography.

University Hospital M£Nster

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

Time-dependent botulinum neurotoxin serotype A metalloprotease inhibitors.

Microbiotix

Virtual screening targeting the urokinase receptor, biochemical and cell-based studies, synthesis, pharmacokinetic characterization, and effect on breast tumor metastasis.

Indiana University School Of Medicine

Discovery of novel Cobactin-T based matrix metalloproteinase inhibitors via a ring closing metathesis strategy.

Johnson & Johnson Pharmaceutical Research & Development

Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.

University Of Illinois At Chicago

Selective water-soluble gelatinase inhibitor prodrugs.

University Of Notre Dame

N-substituted homopiperazine barbiturates as gelatinase inhibitors.

Trinity College

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£

Orally active achiral N-hydroxyformamide inhibitors of ADAM-TS4 (aggrecanase-1) and ADAM-TS5 (aggrecanase-2) for the treatment of osteoarthritis.

Astrazeneca

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

MMP-13 selective alpha-sulfone hydroxamates: identification of selective P1' amides.

Pfizer

2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors.

Merck Research Laboratories

Discovery of (1S,2R,3R)-2,3-dimethyl-2-phenyl-1-sulfamidocyclopropanecarboxylates: novel and highly selective aggrecanase inhibitors.

Central Pharmaceutical Research Institute

Sulfonate-Containing Thiiranes as Selective Gelatinase Inhibitors

TBA

Structure based optimization of chromen-based TNF-a converting enzyme (TACE) inhibitors on S1' pocket and their quantitative structure-activity relationship (QSAR) study.

Yonsei University

Novel TNF-a converting enzyme (TACE) inhibitors as potential treatment for inflammatory diseases.

Merck Research Laboratories

MMP-13 selective isonipecotamide alpha-sulfone hydroxamates.

Pfizer

Orally bioavailable dual MMP-1/MMP-14 sparing, MMP-13 selective alpha-sulfone hydroxamates.

Pfizer

Potent arylsulfonamide inhibitors of tumor necrosis factor-alpha converting enzyme able to reduce activated leukocyte cell adhesion molecule shedding in cancer cell models.

Universit£

Discovery and SAR of hydantoin TACE inhibitors.

Merck Research Laboratories

Identification of potential and selective collagenase, gelatinase inhibitors from Crataegus pinnatifida.

Wonkwang University Sanbon Medical Center

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

Design, synthesis, biological evaluation, and NMR studies of a new series of arylsulfones as selective and potent matrix metalloproteinase-12 inhibitors.

Universit£

3,4-Disubstituted benzofuran P1' MMP-13 inhibitors: optimization of selectivity and reduction of protein binding.

Wyeth Research

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£

 

Synthesis of conformationally constrained potential inhibitors of mammalian metalloproteinases

TBA

 

Mercaptoacyl matrix metalloproteinase inhibitors: The effect of substitution at the mercaptoacyl moiety

TBA

 

Inhibition of Matrix Metalloproteinases: An examination of the S1′ pocket

TBA

 

Amide surrogates of matrix metalloproteinase inhibitors: Urea and sulfonamide mimics

TBA

 

Design and synthesis of the cartilage protective agent (CPA, Ro32-3555)

TBA

 

Rapid synthesis of novel dipeptide inhibitors of human collagenase and gelatinase using solid phase chemistry

TBA

 

Hydroxamate inhibitors of human gelatinase B (92 kDa)

TBA

 

Inhibition of metalloproteinase by futoenone derivatives

TBA

Compelling P1 substituent affect on metalloprotease binding profile enables the design of a novel cyclohexyl core scaffold with excellent MMP selectivity and HER-2 sheddase inhibition.

Incyte

Dual inhibitors of matrix metalloproteinases and carbonic anhydrases: iminodiacetyl-based hydroxamate-benzenesulfonamide conjugates.

Instituto Superior TéCnico

Succinyl hydroxamates as potent and selective non-peptidic inhibitors of procollagen C-proteinase: design, synthesis, and evaluation as topically applied, dermal anti-scarring agents.

Pfizer

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

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

beta-N-Biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors: part 2. Optimization of alpha-amino substituents.

Johnson & Johnson Pharmaceutical Research And Development

Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P1' permutations.

Incyte

Design and identification of selective HER-2 sheddase inhibitors via P1' manipulation and unconventional P2' perturbations to induce a molecular metamorphosis.

Incyte

A novel series of highly selective inhibitors of MMP-3.

Pfizer

Chromen-based TNF-alpha converting enzyme (TACE) inhibitors: design, synthesis, and biological evaluation.

Yonsei University

Potent and selective nonpeptidic inhibitors of procollagen C-proteinase.

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

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

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 a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.

Incyte

Discovery of novel hydantoins as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

Bristol-Myers Squibb Pharmaceutical Research Institute

alpha-Biphenylsulfonylamino 2-methylpropyl phosphonates: enantioselective synthesis and selective inhibition of MMPs.

Università

Identification of potent and selective TACE inhibitors via the S1 pocket.

Wyeth Research

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

Bristol-Myers Squibb Pharmaceutical Research Institute

Design and synthesis of butynyloxyphenyl beta-sulfone piperidine hydroxamates as TACE inhibitors.

Wyeth Research

Synthesis and SAR of alpha-sulfonylcarboxylic acids as potent matrix metalloproteinase inhibitors.

Johnson & Johnson Pharmaceutical Research And Development

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

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

Chinese Academy Of Sciences

Matrix metalloproteinase target family landscape: a chemometrical approach to ligand selectivity based on protein binding site analysis.

Aventis Pharma Deutschland

Conversion of potent MMP inhibitors into selective TACE inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

A combination of docking, QM/MM methods, and MD simulation for binding affinity estimation of metalloprotein ligands.

North Dakota State University

Acetylenic TACE inhibitors. Part 2: SAR of six-membered cyclic sulfonamide hydroxamates.

Wyeth Research

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

Non-hydroxamate 5-phenylpyrimidine-2,4,6-trione derivatives as selective inhibitors of tumor necrosis factor-alpha converting enzyme.

Bristol-Myers Squibb Pharmaceutical Research Institute

A new development of matrix metalloproteinase inhibitors: twin hydroxamic acids as potent inhibitors of MMPs.

Università

Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13).

Pharmaceutical Research Institute

Synthesis and structure-activity relationships of 4-alkynyloxy phenyl sulfanyl, sulfinyl, and sulfonyl alkyl hydroxamates as tumor necrosis factor-alpha converting enzyme and matrix metalloproteinase inhibitors.

Wyeth Research

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

Bristol-Myers Squibb Pharmaceutical Research Institute

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

Reverse hydroxamate-based selective TACE inhibitors.

Kaken Pharmaceutical

Azasugar-based MMP/ADAM inhibitors as antipsoriatic agents.

Hokkaido Collaboration Center N-21

Synthesis and biological activity of selective azasugar-based TACE inhibitors.

Organon K.K.

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

Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 2: lead optimization.

Bristol-Myers Squibb Pharmaceutical Research Institute

Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 1: lead identification.

Bristol-Myers Squibb Pharmaceutical Research Institute

A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers.

Pfizer

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

Acetylenic TACE inhibitors. Part 1. SAR of the acyclic sulfonamide hydroxamates.

Wyeth Research

Design, synthesis and evaluation of novel azasugar-based MMP/ADAM inhibitors.

Hokkaido Collaboration Center

Structure--activity relationships of azasugar-based MMP/ADAM inhibitors.

Hokkaido Collaboration Center

Synthesis of radiolabeled biphenylsulfonamide matrix metalloproteinase inhibitors as new potential PET cancer imaging agents.

Indiana University School Of Medicine

Discovery of N-hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamides as potent and selective inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of selective phosphonamide-based inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

Organon K.K.

Design, synthesis, and evaluation of benzothiadiazepine hydroxamates as selective tumor necrosis factor-alpha converting enzyme inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Synthesis and SAR of bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors.

Wyeth-Ayerst Research

Potent and selective aggrecanase inhibitors containing cyclic P1 substituents.

Bristol-Myers Squibb Pharmaceutical Research Institute

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

Benzodiazepine inhibitors of the MMPs and TACE.

Wyeth Research

Oxal hydroxamic acid derivatives with inhibitory activity against matrix metalloproteinases.

University Of Bielefeld

Anthranilate sulfonamide hydroxamate TACE inhibitors. Part 2: SAR of the acetylenic P1' group.

Wyeth-Ayerst Research

Anthranilate sulfonamide hydroxamate TACE inhibitors. Part 1: Structure-based design of novel acetylenic P1' groups.

Wyeth-Ayerst Research

Encounter with unexpected collagenase-1 selective inhibitor: switchover of inhibitor binding pocket induced by fluorine atom.

Organon K.K.

New strategy for antedrug application: development of metalloproteinase inhibitors as antipsoriatic drugs.

Organon K.K.

Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors.

Abbott Laboratories

Potent P1' biphenylmethyl substituted aggrecanase inhibitors.

Bristol-Myers Squibb Pharma

Design of selective and soluble inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

Glaxosmithkline

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

Design and synthesis of matrix metalloproteinase inhibitors guided by molecular modeling. Picking the S(1) pocket using conformationally constrained inhibitors.

Université

N-Aryl sulfonyl homocysteine hydroxamate inhibitors of matrix metalloproteinases: further probing of the S(1), S(1)', and S(2)' pockets.

Université

N-hydroxyformamide peptidomimetics as TACE/matrix metalloprotease inhibitors: oral activity via P1' isobutyl substitution.

Glaxosmithkline

Discovery and characterization of the potent, selective and orally bioavailable MMP inhibitor ABT-770.

Abbott Laboratories

Design and synthesis of 2-oxo-imidazolidine-4-carboxylic acid hydroxyamides as potent matrix metalloproteinase-13 inhibitors.

Pfizer

Novel 5,5-disubstitutedpyrimidine-2,4,6-triones as selective MMP inhibitors.

Roche Research Center

Discovery of potent and selective succinyl hydroxamate inhibitors of matrix metalloprotease-3 (stromelysin-1).

Pfizer

Selectivity of inhibition of matrix metalloproteases MMP-3 and MMP-2 by succinyl hydroxamates and their carboxylic acid analogues is dependent on P3' group chirality.

Pfizer

General synthesis of alpha-substituted 3-bisaryloxy propionic acid derivatives as specific MMP inhibitors.

Institut De Recherches Servier

Structure-based design and synthesis of a potent matrix metalloproteinase-13 inhibitor based on a pyrrolidinone scaffold.

Pfizer

Protease inhibitors: synthesis of potent bacterial collagenase and matrix metalloproteinase inhibitors incorporating N-4-nitrobenzylsulfonylglycine hydroxamate moieties.

Università

Design and synthesis of piperazine-based matrix metalloproteinase inhibitors.

Procter And Gamble Pharmaceuticals

Selective inhibition of low affinity IgE receptor (CD23) processing: P1' bicyclomethyl substituents.

Smithkline Beecham Pharmaceuticals

Phosphinic pseudo-tripeptides as potent inhibitors of matrix metalloproteinases: a structure-activity study.

Cea

P1, P2'-linked macrocyclic amine derivatives as matrix metalloproteinase inhibitors.

Dupont Pharmaceuticals

Homology modeling of gelatinase catalytic domains and docking simulations of novel sulfonamide inhibitors.

Shionogi

Identification of highly selective inhibitors of collagenase-1 from combinatorial libraries of diketopiperazines.

Affymax Research Institute

The asymmetric synthesis and in vitro characterization of succinyl mercaptoalcohol and mercaptoketone inhibitors of matrix metalloproteinases.

Wyeth-Ayerst Research

Malonyl alpha-mercaptoketones and alpha-mercaptoalcohols, a new class of matrix metalloproteinase inhibitors.

Affymax Research Institute

Structure-based design and synthesis of a series of hydroxamic acids with a quaternary-hydroxy group in P1 as inhibitors of matrix metalloproteinases.

Dupont Pharmaceuticals

Rational design and combinatorial evaluation of enzyme inhibitor scaffolds: identification of novel inhibitors of matrix metalloproteinases.

Affymax Research Institute

Macrocyclic amino carboxylates as selective MMP-8 inhibitors.

Dupont Pharmaceuticals

Design and synthesis of cyclic inhibitors of matrix metalloproteinases and TNF-alpha production.

Dupont Pharmaceuticals

Inhibition of membrane-type 1 matrix metalloproteinase by hydroxamate inhibitors: an examination of the subsite pocket.

Kanebo

Highly selective and orally active inhibitors of type IV collagenase (MMP-9 and MMP-2): N-sulfonylamino acid derivatives.

Shionogi

Matrix metalloproteinase inhibitors: a structure-activity study.

Glycomed

Dual inhibition of human leukocyte elastase and lipid peroxidation: in vitro and in vivo activities of azabicyclo[2.2.2]octane and perhydroindole derivatives.

Institut De Recherche Servier

Inhibition of matrix metalloproteinases by N-carboxyalkyl peptides.

Merck Research Laboratories

Matrix metalloproteinase inhibitors containing a (carboxyalkyl)amino zinc ligand: modification of the P1 and P2' residues.

Glaxo Inc. Research Institute

Three new aromatic sulfonamide inhibitors of carbonic anhydrases I, II, IV and XII.

Universit?? Di Firenze

Design, synthesis and pharmacological evaluation of conformationally restricted N-arylsulfonyl-3-aminoalkoxy indoles as a potential 5-HT6 receptor ligands.

Suven Life Sciences

DL-threo-beta-benzyloxyaspartate, a potent blocker of excitatory amino acid transporters.

Suntory Institute For Bioorganic Research

D4 dopamine receptor binding affinity does not distinguish between typical and atypical antipsychotic drugs.

Case Western Reserve University

Cloning and expression of a novel serotonin receptor with high affinity for tricyclic psychotropic drugs.

National Institute Of Neurological Disorders And Stroke

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

Antagonists of the human A(2A) receptor. Part 6: Further optimization of pyrimidine-4-carboxamides.

Vernalis (R&D)

Small-molecule inhibitors of the MDM2-p53 protein-protein interaction based on an isoindolinone scaffold.

University Of Newcastle Upon Tyne

Synthesis and PKCtheta inhibitory activity of a series of 4-indolylamino-5-phenyl-3-pyridinecarbonitriles.

Wyeth Research

Novel tricyclic inhibitors of IkappaB kinase.

Bristol-Myers Squibb