338 articles for thisTarget
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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
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.
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
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
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
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.
University of Bari Aldo Moro
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
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
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.
University of Pisa
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.
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
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
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.
Lille University of Science and Technology
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.
University of Montreal
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)
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
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
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
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
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
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.
University of Pisa
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.
University of Pisa
A novel series of matrix metalloproteinase inhibitors for the treatment of inflammatory disorders
TBA
Synthesis of conformationally constrained potential inhibitors of mammalian metalloproteinases
TBA
Mercaptoacyl matrix metalloproteinase inhibitors: The effect of substitution at the mercaptoacyl moiety
TBA
Rapid synthesis of novel dipeptide inhibitors of human collagenase and gelatinase using solid phase chemistry
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
Chromen-based TNF-alpha converting enzyme (TACE) inhibitors: design, synthesis, and biological evaluation.
Yonsei University
Platinum complexes can inhibit matrix metalloproteinase activity: platinum-diethyl[(methylsulfinyl)methyl]phosphonate complexes as inhibitors of matrix metalloproteinases 2, 3, 9, and 12.
Università
Structure-Based Optimization and Biological Evaluation of Potent and Selective MMP-7 Inhibitors for Kidney Fibrosis.
Taisho Pharmaceutical Co.
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
Quinazoline-2-Carboxamides as Selective PET Radiotracers for Matrix Metalloproteinase-13 Imaging in Atherosclerosis.
University of Ottawa
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
Influence of N-arylsulfonamido d-valine N-substituents on the selectivity and potency of matrix metalloproteinase inhibitors.
University of Munster
Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.
Incyte
Discovery of TP0597850: A Selective, Chemically Stable, and Slow Tight-Binding Matrix Metalloproteinase-2 Inhibitor with a Phenylbenzamide-Pentapeptide Hybrid Scaffold.
Taisho Pharmaceutical Co.
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 small molecule inhibitors against MMP-14 via High-Throughput screening.
University of Illinois at Chicago
Novel combretastatin A-4 derivative containing aminophosphonates as dual inhibitors of tubulin and matrix metalloproteinases for lung cancer treatment.
Huaiyin Institute of Technology
Hydroxypyrone derivatives in drug discovery: from chelation therapy to rational design of metalloenzyme inhibitors.
Government College Women University
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
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
Inhibitors of gelatinases (MMP-2 and MMP-9) for the management of hematological malignancies.
Jadavpur University
Recent developments of small molecules with anti-inflammatory activities for the treatment of acute lung injury.
Zhejiang University
Reactive Oxygen Species (ROS)-Responsive Prodrugs, Probes, and Theranostic Prodrugs: Applications in the ROS-Related Diseases.
China Pharmaceutical 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 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
Discovery of Phenolic Matrix Metalloproteinase Inhibitors by Peptide Microarray for Osteosarcoma Treatment.
Chinese Academy of Sciences
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
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
Discovery of Highly Potent and Selective Matrix Metalloproteinase-7 Inhibitors by Hybridizing the S1' Subsite Binder with Short Peptides.
Taisho Pharmaceutical
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
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.
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
Halting colorectal cancer metastasis via novel dual nanomolar MMP-9/MAO-A quinoxaline-based inhibitors; design, synthesis, and evaluation.
Alexandria University
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
Multitargeting application of proline-derived peptidomimetics addressing cancer-related human matrix metalloproteinase 9 and carbonic anhydrase II.
University of Florence
Synthesis and SAR of bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors.
Wyeth-Ayerst Research
Discovery of 7-aminophenanthridin-6-one as a new scaffold for matrix metalloproteinase inhibitors with multitarget neuroprotective activity.
Universidad Complutense
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
Hydroxamate-Based Selective Macrophage Elastase (MMP-12) Inhibitors and Radiotracers for Molecular Imaging.
Yale University
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
Battle tactics against MMP-9; discovery of novel non-hydroxamate MMP-9 inhibitors endowed with PI3K/AKT signaling attenuation and caspase 3/7 activation via Ugi bis-amide synthesis.
Alexandria University
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.
Fragment-Based Discovery of Novel Non-Hydroxamate LpxC Inhibitors with Antibacterial Activity.
Taisho Pharmaceutical
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 a d-pro-lys peptidomimetic inhibitor of MMP9: Addressing the gelatinase selectivity beyond S1' subsite.
University of Florence
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
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
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 Cyclic Boronic Acid QPX7728, an Ultrabroad-Spectrum Inhibitor of Serine and Metallo-β-lactamases.
Qpex Biopharma
Virtual screening identification and chemical optimization of substituted 2-arylbenzimidazoles as new non-zinc-binding MMP-2 inhibitors.
"A. Moro" University of Bari
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
Validating the 1,2-Difluoro Motif As a Hybrid Bioisostere of CF
Westf£Lische Wilhelms-Universit£T M£Nster
Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors.
Roche Pharma Research and Early Development
Structure-based design and synthesis of a potent matrix metalloproteinase-13 inhibitor based on a pyrrolidinone scaffold.
Pfizer
Use of Osmotic Pumps to Establish the Pharmacokinetic-Pharmacodynamic Relationship and Define Desirable Human Performance Characteristics for Aggrecanase Inhibitors.
Eli Lilly
Protease inhibitors: synthesis of potent bacterial collagenase and matrix metalloproteinase inhibitors incorporating N-4-nitrobenzylsulfonylglycine hydroxamate moieties.
Università
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
Design and synthesis of piperazine-based matrix metalloproteinase inhibitors.
Procter and Gamble Pharmaceuticals
Design, synthesis and preliminary bioactivity evaluations of 8-hydroxyquinoline derivatives as matrix metalloproteinase (MMP) inhibitors.
Shandong University
Novel Human Aminopeptidase N Inhibitors: Discovery and Optimization of Subsite Binding Interactions.
Monash University
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
Proline-based hydroxamates targeting the zinc-dependent deacetylase LpxC: Synthesis, antibacterial properties, and docking studies.
University of Hamburg
Identification of highly potent and selective MMP2 inhibitors addressing the S1' subsite with d-proline-based compounds.
University of Florence
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
Design and synthesis of thiol containing inhibitors of matrix metalloproteinases.
Novartis Biomedical Research Institute
Hydroxamic Acid Inhibitors Provide Cross-Species Inhibition of Plasmodium M1 and M17 Aminopeptidases.
Monash University
Design, synthesis and biological evaluation of bifunctional inhibitors of membrane type 1 matrix metalloproteinase (MT1-MMP).
University of Pisa
Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.
Bristol-Myers Squibb
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
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
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
Recent developments in the synthesis and applications of phosphinic peptide analogs.
Wroclaw University of Technology
Fluorinated matrix metalloproteinases inhibitors--Phosphonate based potential probes for positron emission tomography.
Westf£Lische Wilhelms-Universit£T
Proteases and Their Modulators in Cancer Therapy: Challenges and Opportunities.
Sichuan University
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
Inverse 1,2,3-triazole-1-yl-ethyl substituted hydroxamates as highly potent matrix metalloproteinase inhibitors: (radio)synthesis, in vitro and first in vivo evaluation.
University Hospital M£Nster
Design, synthesis, and initial evaluation of a high affinity positron emission tomography probe for imaging matrix metalloproteinases 2 and 9.
Eth Zurich
Anti-invasive and anti-angiogenic activities of naturally occurring dibenzodiazepine BU-4664L and its derivatives.
Toyama Prefectural University
Design of antiangiogenic hypoxic cell radiosensitizers: 2-nitroimidazoles containing a 2-aminomethylene-4-cyclopentene-1,3-dione moiety.
The University of Tokushima
Natural inhibitors targeting osteoclast-mediated bone resorption.
Chinese Academy of Sciences
Matrix metalloproteinase-12 inhibitors: synthesis, structure-activity relationships and intestinal absorption of novel sugar-based biphenylsulfonamide carboxylates.
University of Pisa
Synthesis and biological evaluation of novel benzofuroxan-based pyrrolidine hydroxamates as matrix metalloproteinase inhibitors with nitric oxide releasing activity.
Weifang Medical University
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
Lung cancer and matrix metalloproteinases inhibitors of polyphenols from Selaginella tamariscina with suppression activity of migration.
Guangxi Normal University
Discovery of dehydroabietic acid sulfonamide based derivatives as selective matrix metalloproteinases inactivators that inhibit cell migration and proliferation.
Southeast University
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
Tamarixetin 3-O-β-d-Glucopyranoside from Azadirachta indica Leaves: Gastroprotective Role through Inhibition of Matrix Metalloproteinase-9 Activity in Mice.
National Institute of Pharmaceutical Education and Research
Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry.
St. John'S University
First insight into structure-activity relationships of selective meprinβ inhibitors.
Fraunhofer Institute For Cell Therapy and Immunology Izi
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
Sulfonamide or sulfinamide compound having effect of inducing BRD4 protein degradation and pharmaceutical use thereof
Mitsubishi Tanabe Pharma
Bicyclic compounds as autotaxin (ATX) and lysophosphatidic acid (LPA) production inhibitors
Hoffmann-La Roche
Imidazolin-5-one derivative useful as FASN inhibitors for the treatment of cancer
Janssen Pharmaceutica
Treatment of neurodegenerative diseases through inhibition of HSP90
Sloan-Kettering Institute For Cancer Research
Tricyclic compounds as inhibitors of immunosuppression mediated by tryptophan metabolization
Newlink Genetics
CARBOXYLIC ACID AROMATIC AMIDES AS ANTAGONISTS OF BRADYKININ B1 RECEPTOR
Bayer Pharma Aktiengesellschaft
Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase
North Carolina Central University
Pyrazole substituted imidazopyrazines as casein kinase 1 d/e inhibitors
Bristol-Myers Squibb
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 validation of acetyltransferase activity of GlmU as an antibacterial target in Haemophilus influenzae.
Astrazeneca
Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist.
Acadia Pharmaceuticals
In vitro pharmacological profile of SK-896, a new human motilin analogue.
Sanwa Kagaku Kenkyusho
Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors.
Merck Research Laboratories
Novel piperidine derivatives. Synthesis and anti-acetylcholinesterase activity of 1-benzyl-4-[2-(N-benzoylamino)ethyl]piperidine derivatives.
Tsukuba Research Laboratories
Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity.
Wyeth-Ayerst Research