241 articles for thisTarget
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Article Title
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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
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
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
Discovery of Potent and Selective Inhibitors for ADAMTS-4 through DNA-Encoded Library Technology (ELT).
Glaxosmithkline
N-O-Isopropyl Sulfonamido-Based Hydroxamates as Matrix Metalloproteinase Inhibitors: Hit Selection and in Vivo Antiangiogenic Activity.
Universit£
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
2-Benzisothiazolylimino-5-benzylidene-4-thiazolidinones as protective agents against cartilage destruction.
University of Catania
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
Characterization of selective exosite-binding inhibitors of matrix metalloproteinase 13 that prevent articular cartilage degradation in vitro.
Translational Research Institute
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
Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-ß hydrolysis.
University of Lille
Arylsulfonamide inhibitors of aggrecanases as potential therapeutic agents for osteoarthritis: synthesis and biological evaluation.
Universit£
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.
Universit£
Matrix metalloproteinases (MMPs): chemical-biological functions and (Q)SARs.
Pomona College
Discovery of highly potent and selective small molecule ADAMTS-5 inhibitors that inhibit human cartilage degradation via encoded library technology (ELT).
Glaxosmithkline
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
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
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
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.
University of Florida
High throughput screening of potentially selective MMP-13 exosite inhibitors utilizing a triple-helical FRET substrate.
Florida Atlantic University
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
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
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
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
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
Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents.
F. Hoffmann-La Roche
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
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
alpha-Alkyl-alpha-amino-beta-sulphone hydroxamates as potent MMP inhibitors that spare MMP-1.
Pfizer
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
Picking the S1, S1' and S2' pockets of matrix metalloproteinases. A niche for potent acyclic sulfonamide inhibitors.
Universit£
The synthesis and biological activity of a novel series of diazepine MMP inhibitors.
Wyeth-Ayerst Research
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
Identification of novel, exosite-binding matrix metalloproteinase-13 inhibitor scaffolds.
Scripps Florida
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
Identification of novel molecular scaffolds for the design of MMP-13 inhibitors: a first round of lead optimization.
Universit£
Potent and selective 2-naphthylsulfonamide substituted hydroxamic acid inhibitors of matrix metalloproteinase-13.
Novartis Institutes For Biomedical Research
Discovery of novel Cobactin-T based matrix metalloproteinase inhibitors via a ring closing metathesis strategy.
Johnson & Johnson Pharmaceutical Research & Development
Continued exploration of biphenylsulfonamide scaffold as a platform for aggrecanase-1 inhibition.
Pfizer
Orally active MMP-1 sparinga-tetrahydropyranyl anda-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
Pfizer
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
Structure-based approach to nanomolar, water soluble matrix metalloproteinases inhibitors (MMPIs).
Protera
Novel TNF-a converting enzyme (TACE) inhibitors as potential treatment for inflammatory diseases.
Merck Research Laboratories
SAR studies of non-zinc-chelating MMP-13 inhibitors: improving selectivity and metabolic stability.
Boehringer Ingelheim Pharmaceuticals
Orally bioavailable dual MMP-1/MMP-14 sparing, MMP-13 selective alpha-sulfone hydroxamates.
Pfizer
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
Phosphinic tripeptides as dual angiotensin-converting enzyme C-domain and endothelin-converting enzyme-1 inhibitors.
Cea
The identification of beta-hydroxy carboxylic acids as selective MMP-12 inhibitors.
Gsk Medicines Research Centre
Design, synthesis, biological evaluation, and NMR studies of a new series of arylsulfones as selective and potent matrix metalloproteinase-12 inhibitors.
Universit£
3,4-Disubstituted benzofuran P1' MMP-13 inhibitors: optimization of selectivity and reduction of protein binding.
Wyeth Research
Identification of an orally efficacious matrix metalloprotease 12 inhibitor for potential treatment of asthma.
Wyeth Research
N-O-isopropyl sulfonamido-based hydroxamates: design, synthesis and biological evaluation of selective matrix metalloproteinase-13 inhibitors as potential therapeutic agents for osteoarthritis.
Universit£
Synthesis 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
Calculation of binding free energies for non-zinc chelating pyrimidine dicarboxamide inhibitors with MMP-13.
Stony Brook University
N-((8-hydroxy-5-substituted-quinolin-7-yl)(phenyl)methyl)-2-phenyloxy/amino-acetamide inhibitors of ADAMTS-5 (Aggrecanase-2).
Wyeth Research
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
University of Athens
Ranking the selectivity of PubChem screening hits by activity-based protein profiling: MMP13 as a case study.
The Scripps Research Institute
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
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
Simultaneous presence of unsaturation and long alkyl chain at P'1 of Ilomastat confers selectivity for gelatinase A (MMP-2) over gelatinase B (MMP-9) inhibition as shown by molecular modelling studies.
Université
Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Bristol-Myers Squibb Pharmaceutical Research Institute
A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1' group for the beta-amino hydroxamic acid derived TACE inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and in vitro evaluation of targeted tetracycline derivatives: effects on inhibition of matrix metalloproteinases.
Clermont Auvergne University
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
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
Matrix metalloproteinases inhibitors in idiopathic pulmonary fibrosis: Medicinal chemistry perspectives.
Sichuan University-University of Oxford Huaxi Joint Centre For Gastrointestinal Cancer
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
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
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
Targeting osteoarthritis-associated galectins and an induced effector class by a ditopic bifunctional reagent: Impact of its glycan part on binding measured in the tissue context.
Ludwig-Maximilians-University Munich
Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates.
Wyeth Research
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
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 3,3-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
Selective Inhibitors of Medium-Size S1' Pocket Matrix Metalloproteinases: A Stepping Stone of Future Drug Discovery.
Jadavpur University
Potent pyrimidinetrione-based inhibitors of MMP-13 with enhanced selectivity over MMP-14.
Pfizer
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
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
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
Synthesis of radiolabeled biphenylsulfonamide matrix metalloproteinase inhibitors as new potential PET cancer imaging agents.
Indiana University School of Medicine
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
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
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
Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors.
Abbott Laboratories
alpha-Amino-beta-sulphone hydroxamates as potent MMP-13 inhibitors that spare MMP-1.
Pfizer
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
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
The development of new carboxylic acid-based MMP inhibitors derived from a cyclohexylglycine scaffold.
Procter and Gamble Pharmaceuticals
2-(2-Oxo-1,4-dihydro-2H-quinazolin-3-yl)- and 2-(2,2-dioxo-1,4-dihydro-2H-2lambda6-benzo[1,2,6]thiadiazin-3-yl)-N-hydroxy-acetamides as potent and selective peptide deformylase inhibitors.
F. Hoffmann-La Roche
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
Development of new carboxylic acid-based MMP inhibitors derived from functionalized propargylglycines.
Procter and Gamble Pharmaceuticals
Chemoenzymatic synthesis of functionalized cyclohexylglycines and alpha-methylcyclohexylglycines via Kazmaier-Claisen rearrangement.
University of Florida
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
General synthesis of alpha-substituted 3-bisaryloxy propionic acid derivatives as specific MMP inhibitors.
Institut De Recherches Servier
Development of new hydroxamate matrix metalloproteinase inhibitors derived from functionalized 4-aminoprolines.
Procter and Gamble Pharmaceuticals
Validating the 1,2-Difluoro Motif As a Hybrid Bioisostere of CF
Westf£Lische Wilhelms-Universit£T M£Nster
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
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 biological evaluation of matrix metalloproteinase inhibitors derived from a modified proline scaffold.
University of Florida
The synthesis and biological evaluation of non-peptidic matrix metalloproteinase inhibitors.
British Biotech Pharmaceuticals
Proline-based hydroxamates targeting the zinc-dependent deacetylase LpxC: Synthesis, antibacterial properties, and docking studies.
University of Hamburg
Synthesis and identification of conformationally constrained selective MMP inhibitors.
Searle Discovery Research
Discovery of a novel series of selective MMP inhibitors: identification of the gamma-sulfone-thiols.
Searle Discovery Research
Inhibition of MMP-1 and MMP-13 with phosphinic acids that exploit binding in the S2 pocket.
Pfizer
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
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
Discovery and process development of a novel TACE inhibitor for the topical treatment of psoriasis.
Nestl�
Synthesis of radioiodinated probes targeted toward matrix metalloproteinase-12.
Kobe Pharmaceutical University
Development of matrix metalloproteinase-13 inhibitors - A structure-activity/structure-property relationship study.
Graz University of Technology
Exploitation of Conformational Dynamics in Imparting Selective Inhibition for Related Matrix Metalloproteinases.
University of Notre Dame
Zinc-Metalloproteinase Inhibitors: Evaluation of the Complex Role Played by the Zinc-Binding Group on Potency and Selectivity.
Universit£
Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry.
St. John'S University
Targeted Polypharmacology: Discovery of a Highly Potent Non-Hydroxamate Dual Matrix Metalloproteinase (MMP)-10/-13 Inhibitor.
Zhaw Zurich University of Applied Sciences
First insight into structure-activity relationships of selective meprin? inhibitors.
Fraunhofer Institute For Cell Therapy and Immunology Izi
Structure-Based Design and Synthesis of Potent and Selective Matrix Metalloproteinase 13 Inhibitors.
Scripps Florida
Insights from selective non-phosphinic inhibitors of MMP-12 tailored to fit with an S1' loop canonical conformation.
Commissariat À
Simple Pseudo-dipeptides with a P2' Glutamate: A NOVEL INHIBITOR FAMILY OF MATRIX METALLOPROTEASES AND OTHER METZINCINS.
Commissariat Á
Heteroarylimino-4-thiazolidinones as inhibitors of cartilage degradation.
University of Catania
Improving potency and selectivity of a new class of non-Zn-chelating MMP-13 inhibitors.
Boehringer Ingelheim Pharmaceuticals
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.
Novartis
Synthesis and activity of quinolinylmethyl P1' alpha-sulfone piperidine hydroxamate inhibitors of TACE.
Wyeth Research
Synthesis of bicyclic molecular scaffolds (BTAa): an investigation towards new selective MMP-12 inhibitors.
University of Florence
A selective matrix metalloprotease 12 inhibitor for potential treatment of chronic obstructive pulmonary disease (COPD): discovery of (S)-2-(8-(methoxycarbonylamino)dibenzo[b,d]furan-3-sulfonamido)-3-methylbutanoic acid (MMP408).
Wyeth Research
Extra Binding Region Induced by Non-Zinc Chelating Inhibitors into the S(1)' Subsite of Matrix Metalloproteinase 8 (MMP-8) (dagger).
Universita Degli Studi
Potent, exceptionally selective, orally bioavailable inhibitors of TNF-alpha Converting Enzyme (TACE): novel 2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamide P1' substituents.
Bristol-Myers Squibb
Novel thiol-based TACE inhibitors. Part 2: Rational design, synthesis, and SAR of thiol-containing aryl sulfones.
Vertex Pharmaceuticals
Novel thiol-based TACE inhibitors: rational design, synthesis, and SAR of thiol-containing aryl sulfonamides.
Vertex Pharmaceuticals
Synthesis and biological evaluation of biphenylsulfonamide carboxylate aggrecanase-1 inhibitors.
Wyeth Research
5'-Phenyl-3'H-spiro[indoline-3,2'-[1,3,4]thiadiazol]-2-one inhibitors of ADAMTS-5 (aggrecanase-2).
Wyeth Research
Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket.
Wyeth Research
Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-alpha-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheumatoid arthritis.
Wyeth Research
Structural basis for the highly selective inhibition of MMP-13.
Aventis Pharma Deutschland
Synthesis and structure-activity relationships of beta- and alpha-piperidine sulfone hydroxamic acid matrix metalloproteinase inhibitors with oral antitumor efficacy.
Pfizer