期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 15, 期 18, 页码 4037-4042出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.06.027
关键词
tripeptides; bioterrorism; pTyr mimetics; YopH; PTP1B
资金
- NIAID NIH HHS [1U54 AI57158] Funding Source: Medline
We report the synthesis of a series of monoanionic phosphotyrosyl (pTyr) mimetic-containing tripeptides based on `Fmoc-Glu(OBn)-Xxx-Leu-amide' (where Xxx = pTyr mimetic) and their N-terminally modified derivatives. The inhibitory potencies of compounds were tested against YopH and human PTP1B enzymes. Several compounds exhibited noteworthy activity against both YopH and PTP1B. Among the N-terminally modified analogues, 5-methylindole derivative 30 was found to be the best moiety to replace base-labile Fmoc group. A mode of binding with YopH is proposed for tripeptides 21, 30, and 31. (c) 2005 Elsevier Ltd. All rights reserved.
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