Discovery and Characterization of a Novel Inhibitor of Matrix Metalloprotease-13 (mmp13) That Reduces Cartilage Damage in Vivo without Joint Fibroplasia Side Effects
نویسندگان
چکیده
DISCOVERY AND CHARACTERIZATION OF A NOVEL INHIBITOR OF MATRIX METALLOPROTEASE-13 (MMP13) THAT REDUCES CARTILAGE DAMAGE IN VIVO WITHOUT JOINT FIBROPLASIA SIDE EFFECTS Adam R. Johnson, # Alexander G. Pavlovsky, Daniel F. Ortwine, Faith Prior, Chiu-Fai Man, Dirk A. Bornemeier, Craig A. Banotai, W. Thomas Mueller, Patrick McConnell, Chunhong Yan, Vijay Baragi, Charles Lesch, W. Howard Roark, Michael Wilson, Kaushik Datta, Roberto Guzman, Hyo-Kyung Han, and Richard D. Dyer From the Departments of Inflammation Molecular Sciences, Discovery Technologies, Inflammation Pharmacology, Inflammation Chemistry, World Wide Safety Sciences, and Pharmacokinetics and Drug Metabolism, Pfizer Global Research & Development, Ann Arbor, Michigan 48105 USA. Running head: Noncompetitive non-chelating MMP13 inhibitors
منابع مشابه
Discovery and characterization of a novel inhibitor of matrix metalloprotease-13 that reduces cartilage damage in vivo without joint fibroplasia side effects.
Matrix metalloproteinase-13 (MMP13) is a Zn(2+)-dependent protease that catalyzes the cleavage of type II collagen, the main structural protein in articular cartilage. Excess MMP13 activity causes cartilage degradation in osteoarthritis, making this protease an attractive therapeutic target. However, clinically tested MMP inhibitors have been associated with a painful, joint-stiffening musculos...
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