PMID
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Article Title
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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
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
Discovery of beta-benzamido hydroxamic acids as potent, selective, and orally bioavailable TACE inhibitors.

Bristol-Myers Squibb
A molecular modeling analysis of novel non-hydroxamate inhibitors of TACE.

Bristol-Myers Squibb Pharmaceutical Research Institute
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.

University of Pisa
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.

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

Bristol-Myers Squibb Pharmaceutical Research Institute
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
Discovery of novel hydantoins as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).

Bristol-Myers Squibb Pharmaceutical Research Institute
Identification of potent and selective TACE inhibitors via the S1 pocket.

Wyeth Research
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
Discovery of Dimeric Arylsulfonamides as Potent ADAM8 Inhibitors.

University of Pisa
The race to treat COVID-19: Potential therapeutic agents for the prevention and treatment of SARS-CoV-2.

American University of Ras Al Khaimah
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
Zinc enzymes in medicinal chemistry.

Hefei University of Technology
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
Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis.

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

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

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

Glaxosmithkline
-Aryl-3-mercaptosuccinimides as Antivirulence Agents Targeting

Helmholtz Institute For Pharmaceutical Research Saarland (Hips) - Helmholtz Centre For Infection Research (Hzi
Notch Antagonists: Potential Modulators of Cancer and Inflammatory Diseases.

Centre Hospitalier Universitaire Vaudois (Chuv)
Use of Osmotic Pumps to Establish the Pharmacokinetic-Pharmacodynamic Relationship and Define Desirable Human Performance Characteristics for Aggrecanase Inhibitors.

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

Astrazeneca
Beta-aryl-succinic acid hydroxamates as dual inhibitors of matrix metalloproteinases and tumor necrosis factor alpha converting enzyme.

Preclinical Research Novartis Pharma
Discovery and process development of a novel TACE inhibitor for the topical treatment of psoriasis.

Nestle Skin Health
In Search of Selectivity in Inhibition of ADAM10.

University of Notre Dame
Development of a prodrug of hydantoin based TACE inhibitor.

Merck
Idiopathic Pulmonary Fibrosis: Current Status, Recent Progress, and Emerging Targets.

Taipei Medical University
Fused bi-heteroaryl substituted hydantoin compounds as TACE inhibitors.

Merck
First insight into structure-activity relationships of selective meprinβ inhibitors.

Fraunhofer Institute For Cell Therapy and Immunology Izi
Compounds

CTXT PTY
The recent outbreaks of human coronaviruses: A medicinal chemistry perspective.

University of Bonn
Derivatives and methods of treating hepatitis B infections

Novira Therapeutics
Heteroaryl compounds as 5-HT4 receptor ligands

Suven Life Sciences
Tricyclic compounds as inhibitors of immunosuppression mediated by tryptophan metabolization

Newlink Genetics
Triazolo compounds

Hoffmann-La Roche
Thioether-piperidinyl orexin receptor antagonists

Merck Sharp & Dohme
Amidoethyl azole orexin receptor antagonists

Merck Sharp & Dohme
Cyclosporins modified on the MeBmt sidechain by heterocyclic rings

Allergan
Pyrazole substituted imidazopyrazines as casein kinase 1 d/e inhibitors

Bristol-Myers Squibb
Three new aromatic sulfonamide inhibitors of carbonic anhydrases I, II, IV and XII.

Universit�� Di Firenze
Heterocyclic kinase inhibitors

Novartis
Oxadiazole fused heterocyclic derivatives useful for the treatment of multiple sclerosis

Merck Serono
8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions

Boehringer Ingelheim International
Solid phase synthesis of 1,5-diarylpyrazole-4-carboxamides: discovery of antagonists of the CB-1 receptor.

Bristol-Myers Squibb Research and Development
In vitro pharmacological profile of SK-896, a new human motilin analogue.

Sanwa Kagaku Kenkyusho
Aromatic organic compounds as scaffolds for metallocarboxypeptidase inhibitor design.

Universitat AutÒnoma De Barcelona
Novel piperidine derivatives. Synthesis and anti-acetylcholinesterase activity of 1-benzyl-4-[2-(N-benzoylamino)ethyl]piperidine derivatives.

Tsukuba Research Laboratories