Author/Authors :
Junjun Wu، نويسنده , , Thomas S. Rush III، نويسنده , , Rajeev Hotchandani، نويسنده , , Xuemei Du، نويسنده , , Mary Geck، نويسنده , , Elisabeth Collins، نويسنده , , Zhang-Bao Xu، نويسنده , , Jerry Skotnicki، نويسنده , , Jeremy I. Levin، نويسنده , , Frank E. Lovering، نويسنده ,
Abstract :
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.
