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Identification of Potent and Selective MMP-13 Inhibitors
- Source :
- ChemInform. 36
- Publication Year :
- 2005
- Publisher :
- Wiley, 2005.
-
Abstract
- A potent, selective series of MMP-13 inhibitors has been derived from a weak (3.2 microM) inhibitor that did not bear a zinc chelator. Structure-based drug design strategies were employed to append a Zn-chelating group to one end of the molecule and functionality to enhance selectivity to the other. A compound from this series demonstrated rat oral bioavailability and efficacy in a bovine articular cartilage explant model.
- Subjects :
- Models, Molecular
Matrix metalloproteinase inhibitor
Clinical Biochemistry
Administration, Oral
Pharmaceutical Science
Articular cartilage
Pharmacology
Matrix metalloproteinase
Crystallography, X-Ray
Biochemistry
Substrate Specificity
Drug Discovery
Amino Acids
Chelating Agents
media_common
chemistry.chemical_classification
biology
Chemistry
General Medicine
Zinc
Enzyme inhibitor
Molecular Medicine
Selectivity
Drug
media_common.quotation_subject
In Vitro Techniques
Matrix Metalloproteinase Inhibitors
Sensitivity and Specificity
Inhibitory Concentration 50
Structure-Activity Relationship
Pharmacokinetics
Matrix Metalloproteinase 13
Animals
Structure–activity relationship
Protease Inhibitors
Chelation
Collagenases
Molecular Biology
Benzofurans
Organic Chemistry
In vitro
Protein Structure, Tertiary
Rats
Bioavailability
Cartilage
Enzyme
Drug Design
biology.protein
Cattle
Explant culture
Subjects
Details
- ISSN :
- 15222667 and 09317597
- Volume :
- 36
- Database :
- OpenAIRE
- Journal :
- ChemInform
- Accession number :
- edsair.doi.dedup.....23b84593b836a26fe32ec51c336a0614