Potent inhibition of protein-tyrosine phosphatase-1B using the phosphotyrosyl mimetic fluoro-O-malonyl tyrosine (FOMT)

被引：31

作者：

Roller, PP

Wu, L

Zhang, ZY

Burke, TR

机构：

[1] NCI, Med Chem Lab, Div Basic Sci, NIH, Bethesda, MD 20892 USA

[2] Yeshiva Univ Albert Einstein Coll Med, Dept Mol Pharmacol, Bronx, NY 10461 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(98)00376-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

To enhance PTP binding interactions, both inside and outside the pTyr binding pocket, a thioether-cyclized peptide has been designed based on the EGF receptor autophosphorylation sequence (EGFR(988-993)) "Asp-Ala-Asp-GlU-pTyr-Leu", in which the pTyr residue has been replaced by the nonphosphorus-containing pTyr mimetic fluoro-O-malonyltyrosine (FOMT, 2). The resulting peptide 4 exhibits a K-i value of 170 nM, making it one of the most potent inhibitors of PTP1B yet reported. (C) 1998 Elsevier Science Ltd. All rights reserved.

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页码：2149 / 2150

页数：2

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