PMID

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Article Title

Organization

Identification of novel TACE inhibitors compatible with topical application.

Nestl�

Full Sequence Amino Acid Scanning of¿-Defensin RTD-1 Yields a Potent Anthrax Lethal Factor Protease Inhibitor.

State University Of New York

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

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

Discovery of Potent and Selective Inhibitors for ADAMTS-4 through DNA-Encoded Library Technology (ELT).

Glaxosmithkline

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

Identification of potent and selective hydantoin inhibitors of aggrecanase-1 and aggrecanase-2 that are efficacious in both chemical and surgical models of osteoarthritis.

Eli Lilly

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

Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-ß hydrolysis.

University Of Lille

Discovery of a benzimidazole series of ADAMTS-5 (aggrecanase-2) inhibitors by scaffold hopping.

Asahi Kasei Pharma

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

University Of Lille

Selective arylsulfonamide inhibitors of ADAM-17: hit optimization and activity in ovarian cancer cell models.

UniversitÀ

A series of thiazole derivatives bearing thiazolidin-4-one as non-competitive ADAMTS-5 (aggrecanase-2) inhibitors.

Asahi Kasei Pharma

Discovery of highly potent and selective small molecule ADAMTS-5 inhibitors that inhibit human cartilage degradation via encoded library technology (ELT).

Glaxosmithkline

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

Current perspective of TACE inhibitors: a review.

The M. S. University Of Baroda

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

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

Protease inhibitors: current status and future prospects.

University Of Queensland

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

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

Pfizer

Novel 1-hydroxypiperazine-2,6-diones as new leads in the inhibition of metalloproteinases.

Instituto Superior T£Cnico

Synthesis, preliminary biological evaluation and molecular modeling of some new heterocyclic inhibitors of TACE.

Sun Pharma Advanced Research

Structure and activity relationships of tartrate-based TACE inhibitors.

Merck Research Laboratories

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

The design and synthesis of novel N-hydroxyformamide inhibitors of ADAM-TS4 for the treatment of osteoarthritis.

Astrazeneca

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

Biaryl substituted hydantoin compounds as TACE inhibitors.

Merck Research Laboratories

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

Synthesis and SAR of 2-phenyl-1-sulfonylaminocyclopropane carboxylates as ADAMTS-5 (Aggrecanase-2) inhibitors.

Central Pharmaceutical Research Institute

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

Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB.

National Human Genome Research Institute

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

Gsk Medicines Research Centre

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£

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

Synthesis and activity of tryptophan sulfonamide derivatives as novel non-hydroxamate TNF-alpha converting enzyme (TACE) inhibitors.

Wyeth Research

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

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

Yonsei University

Design and synthesis of 3,3-piperidine hydroxamate analogs as selective TACE inhibitors.

Wyeth Research

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

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

Wyeth Research

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

Wyeth Research

A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors.

Novartis Institutes For Biomedical Research

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

Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates.

Wyeth Research

Conversion of potent MMP inhibitors into selective TACE inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Synthesis and SAR of highly selective MMP-13 inhibitors.

Wyeth Research

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

Wyeth Research

Discovery of 3-OH-3-methylpipecolic hydroxamates: potent orally active inhibitors of aggrecanase and MMP-13.

Pfizer

Discovery of 3,3-dimethyl-5-hydroxypipecolic hydroxamate-based 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

Synthesis and SAR of diazepine and thiazepine TACE and MMP inhibitors.

Wyeth Research

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

Structure-based virtual screening and biological evaluation of potent and selective ADAM12 inhibitors.

Department Of Life Science And National Research Laboratory Of Proteolysis

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

Bristol-Myers Squibb Pharmaceutical Research Institute

Benzodiazepine inhibitors of the MMPs and TACE. Part 2.

Wyeth Research

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.

Synthesis and biological activity of piperazine-based dual MMP-13 and TNF-alpha converting enzyme inhibitors.

Pfizer

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

Pfizer

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

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

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

Synthesis and biological activity of selective pipecolic acid-based TNF-alpha converting enzyme (TACE) inhibitors.

Pfizer

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

Wyeth-Ayerst Research

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

Organon K.K.

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

Glaxosmithkline

Discovery of selective hydroxamic acid inhibitors of tumor necrosis factor-alpha converting enzyme.

Abbott Laboratories

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

Glaxosmithkline

New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors.

Astrazeneca

[3H]RY 80: A high-affinity, selective ligand for gamma-aminobutyric acidA receptors containing alpha-5 subunits.

National Institute Of Diabetes And Digestive And Kidney Diseases