857078-06-9Relevant academic research and scientific papers
Identification of potent and selective MMP-13 inhibitors
Wu, Junjun,Rush III, Thomas S.,Hotchandani, Rajeev,Du, Xuemei,Geck, Mary,Collins, Elisabeth,Xu, Zhang-Bao,Skotnicki, Jerry,Levin, Jeremy I.,Lovering, Frank E.
, p. 4105 - 4109 (2005)
A potent, selective series of MMP-13 inhibitors has been derived from a weak (3.2 μM) 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.
