4.5 Article

Identification of potent and selective TACE inhibitors via the S1 pocket

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 17, Issue 1, Pages 34-39

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.10.004

Keywords

inflammation; TACE; rheumatoid arthritis

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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. (c) 2006 Elsevier Ltd. All rights reserved.

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