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Identification of potent and selective TACE inhibitors via the S1 pocket |
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| Authors: | Condon Jeffrey S Joseph-McCarthy Diane Levin Jeremy I Lombart Henry-Georges Lovering Frank E Sun Linhong Wang Weiheng Xu Weixin Zhang Yuhua |
| Affiliation: | Chemical and Screening Sciences, Wyeth Research, 200 Cambridge Park Drive, Cambridge, MA 02140, USA. |
| Abstract: | By focusing on the P1 portion of the piperidine beta-sulfone ligands we identified a motif that induces selectivity and resulted in a series of TACE inhibitors that demonstrated excellent in vitro potency against isolated TACE enzyme and excellent selectivity over MMPs 1, 2, 9, 13, and 14. |
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