Related Experiment Video
Updated: Aug 14, 2026

In Vitro and In Vivo Models to Study Corneal Endothelial-mesenchymal Transition
Published on: August 20, 2016
Conversion of potent MMP inhibitors into selective TACE inhibitors
Robert J Cherney1, Bryan W King, John L Gilmore
1Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. robert.cherney@bms.com
Abstract:
Novel sultam hydroxamates with potent MMP activity were transformed into potent TACE inhibitors, lacking MMP activity. To accomplish this we relied on structural differences between the MMP and TACE S1' pockets and the known advantageous fit of a 2-methyl-4-quinolinylmethoxyphenyl group into this region. From this approach, compound 7d was identified as a potent TACE inhibitor (IC50 = 3.7 nM) that lacked MMP-1, -2, -9, and -13 activity.
Related Concept Videos
Targeted Cancer Therapies
There are several types of targeted therapies against specific...
Role of Matrix Metalloproteases in Degradation of ECM
A...
