149 articles for thisTarget
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A Highly Selective Hydantoin Inhibitor of Aggrecanase-1 and Aggrecanase-2 with a Low Projected Human Dose.
Eli Lilly
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.
University of Pisa
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 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
N-O-Isopropyl Sulfonamido-Based Hydroxamates as Matrix Metalloproteinase Inhibitors: Hit Selection and in Vivo Antiangiogenic Activity.
University of Pisa
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
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
Discovery of a benzimidazole series of ADAMTS-5 (aggrecanase-2) inhibitors by scaffold hopping.
Asahi Kasei Pharma
Arylamino methylene bisphosphonate derivatives as bone seeking matrix metalloproteinase inhibitors.
University of Bari Aldo Moro
O-phenyl carbamate and phenyl urea thiiranes as selective matrix metalloproteinase-2 inhibitors that cross the blood-brain barrier.
University of Notre Dame
Selective arylsulfonamide inhibitors of ADAM-17: hit optimization and activity in ovarian cancer cell models.
UniversitÀ
Design and synthesis of MMP inhibitors with appended fluorescent tags for imaging and visualization of matrix metalloproteinase enzymes.
Mallinckrodt Pharmaceuticals
Matrix metalloproteinase inhibitors based on the 3-mercaptopyrrolidine core.
Florida State University
A series of thiazole derivatives bearing thiazolidin-4-one as non-competitive ADAMTS-5 (aggrecanase-2) inhibitors.
Asahi Kasei Pharma
Arylsulfonamide inhibitors of aggrecanases as potential therapeutic agents for osteoarthritis: synthesis and biological evaluation.
University of Pisa
Synthesis and preliminary evaluation in tumor bearing mice of new (18)F-labeled arylsulfone matrix metalloproteinase inhibitors as tracers for positron emission tomography.
University of Eastern Piedmont
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
A one-pot synthesis and biological activity of ageladine A and analogues.
Macquarie University
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
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.
University of Florida
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
N-hydroxy-2-(naphthalene-2-ylsulfanyl)-acetamide, a novel hydroxamic acid-based inhibitor of aminopeptidase N and its anti-angiogenic activity.
Sejong University
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
Pyran-containing sulfonamide hydroxamic acids: potent MMP inhibitors that spare MMP-1.
Pfizer
In silico scaffold evaluation and solid phase approach to identify new gelatinase inhibitors.
Colosseum Combinatorial Chemistry Centre For Technology (C4T Scarl)
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
Identification of novel molecular scaffolds for the design of MMP-13 inhibitors: a first round of lead optimization.
University of Naples Federico II
Design, synthesis, docking, and biological evaluation of novel diazide-containing isoxazole- and pyrazole-based histone deacetylase probes.
University of Illinois At Chicago
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.
University of Pisa
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
The design and synthesis of novel N-hydroxyformamide inhibitors of ADAM-TS4 for the treatment of osteoarthritis.
Astrazeneca
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.
University of Pisa
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
Design, synthesis, biological evaluation, and NMR studies of a new series of arylsulfones as selective and potent matrix metalloproteinase-12 inhibitors.
University of Pisa
3,4-Disubstituted benzofuran P1' MMP-13 inhibitors: optimization of selectivity and reduction of protein binding.
Wyeth Research
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
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
Synthesis and biological evaluation of ((4-keto)-phenoxy)methyl biphenyl-4-sulfonamides: a class of potent aggrecanase-1 inhibitors.
Wyeth Research
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
Discovery and characterization of a novel inhibitor of matrix metalloprotease-13 that reduces cartilage damage in vivo without joint fibroplasia side effects.
Pfizer
Are inhibitors of histone deacetylase 8 (HDAC8) effective in hematological cancers especially acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL)?
Jadavpur University
Discovery of TP0628103: A Highly Potent and Selective MMP-7 Inhibitor with Reduced OATP-Mediated Clearance Designed by Shifting Isoelectric Points.
Taisho Pharmaceutical Co., Ltd.
Structure-Based Optimization and Biological Evaluation of Potent and Selective MMP-7 Inhibitors for Kidney Fibrosis.
Taisho Pharmaceutical Co.
Design and synthesis of 3,3-piperidine hydroxamate analogs as selective TACE inhibitors.
Wyeth Research
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
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.
Identification of small molecule inhibitors against MMP-14 via High-Throughput screening.
University of Illinois at Chicago
alpha-Biphenylsulfonylamino 2-methylpropyl phosphonates: enantioselective synthesis and selective inhibition of MMPs.
Università
Outline of gelatinase inhibitors as anti-cancer agents: A patent mini-review for 2010-present.
Jadavpur University
Identification of potent and selective TACE inhibitors via the S1 pocket.
Wyeth Research
Targeting Aggrecanases for Osteoarthritis Therapy: From Zinc Chelation to Exosite Inhibition.
University of Pisa
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
Design and synthesis of butynyloxyphenyl beta-sulfone piperidine hydroxamates as TACE inhibitors.
Wyeth 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
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
Discovery of 3-OH-3-methylpipecolic hydroxamates: potent orally active inhibitors of aggrecanase and MMP-13.
Pfizer
Selective Inhibitors of Medium-Size S1' Pocket Matrix Metalloproteinases: A Stepping Stone of Future Drug Discovery.
Jadavpur University
A new development of matrix metalloproteinase inhibitors: twin hydroxamic acids as potent inhibitors of MMPs.
Università
Potent pyrimidinetrione-based inhibitors of MMP-13 with enhanced selectivity over MMP-14.
Pfizer
-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
-Aryl Mercaptopropionamides as Broad-Spectrum Inhibitors of Metallo-β-Lactamases.
Helmholtz Institute For Pharmaceutical Research Saarland
3-Hydroxy-4-arylsulfonyltetrahydropyranyl-3-hydroxamic acids are novel inhibitors of MMP-13 and aggrecanase.
Pfizer
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
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
Oxal hydroxamic acid derivatives with inhibitory activity against matrix metalloproteinases.
University of Bielefeld
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
Structure-based design and synthesis of potent matrix metalloproteinase inhibitors derived from a 6H-1,3,4-thiadiazine scaffold.
UniversitäT Bielefeld
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
Use of Osmotic Pumps to Establish the Pharmacokinetic-Pharmacodynamic Relationship and Define Desirable Human Performance Characteristics for Aggrecanase Inhibitors.
Eli Lilly
Phosphinic pseudo-tripeptides as potent inhibitors of matrix metalloproteinases: a structure-activity study.
Cea
Design, synthesis and biological evaluation of bifunctional inhibitors of membrane type 1 matrix metalloproteinase (MT1-MMP).
University of Pisa
Inhibition of membrane-type 1 matrix metalloproteinase by hydroxamate inhibitors: an examination of the subsite pocket.
Kanebo
Callysponginol sulfate A, an MT1-MMP inhibitor isolated from the marine sponge Callyspongia truncata.
The University of Tokyo
Validation of Matrix Metalloproteinase-9 (MMP-9) as a Novel Target for Treatment of Diabetic Foot Ulcers in Humans and Discovery of a Potent and Selective Small-Molecule MMP-9 Inhibitor That Accelerates Healing.
University of Notre Dame
Development of Thioaryl-Based Matrix Metalloproteinase-12 Inhibitors with Alternative Zinc-Binding Groups: Synthesis, Potentiometric, NMR, and Crystallographic Studies.
University of Pisa
Discovery and process development of a novel TACE inhibitor for the topical treatment of psoriasis.
Nestle Skin Health
Development of matrix metalloproteinase-13 inhibitors - A structure-activity/structure-property relationship study.
Graz University of Technology
A pentanoic acid derivative targeting matrix metalloproteinase-2 (MMP-2) induces apoptosis in a chronic myeloid leukemia cell line.
Jadavpur University
Structure-Based Design and Synthesis of Potent and Selective Matrix Metalloproteinase 13 Inhibitors.
Scripps Florida
Isoindolinone substituted indoles and derivatives as RAS inhibitors
Boehringer Ingelheim International
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