Peptidic alpha-ketocarboxylic acids and sulfonamides as inhibitors of protein tyrosine phosphatases |
| |
Authors: | Chen Yen Ting Xie Jian Seto Christopher T |
| |
Affiliation: | Department of Chemistry, Brown University, 324 Brook St. Box H, Providence, Rhode Island 02912, USA. |
| |
Abstract: | One common approach for designing protein tyrosine phosphatase (PTPase) inhibitors is to incorporate a nonhydrolyzable phosphotyrosine (pTyr) mimic into a peptide substrate for PTPases. This report describes the synthesis of three such nonhydrolyzable pTyr mimics that contain alpha-ketoacid, alpha-hydroxyacid, and methylenesulfonamide functional groups in place of the phosphate. These pTyr mimics were incorporated into the peptide sequence Ac-Asp-Ala-Asp-Glu-X-Leu-NH(2), where X is the pTyr mimic, and analyzed for activity against the Yersinia PTPase and PTP1B. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|