Modification of the N-terminus of peptidomimetic protein tyrosine phosphatase 1B (PTP1B) inhibitors: Identification of analogues with cellular activity

被引：29

作者：

Larsen, SD

Stevens, FC

Lindberg, TJ

Bodnar, PM

O'Sullivan, TJ

Schostarez, HJ

Palazuk, BJ

Bleasdale, JE

机构：

[1] Pharmacia Corp, Med Chem Res, Kalamazoo, MI 49007 USA

[2] Pharmacia Corp, Cell & Mol Biol, Kalamazoo, MI 49007 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 05期

关键词：

D O I：

10.1016/S0960-894X(02)01065-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Low molecular weight peptidomimetic compounds based on 0-malonyl tyrosine and 0-carboxymethyl salicylic acid are potent inhibitors of PTP1B. Modifications of the N-terminal Boc-Phe moiety were undertaken in an effort to improve physical chemical properties and to achieve cellular activity. Although Phe ultimately proved to be the optimal N-terminal amino acid, several viable replacements for the Boc group were identified, two of which afforded analogues that were effective at enhancing the insulin-stimulated uptake of 2-deoxyglucose by L6 myocytes. (C) 2003 Elsevier Science Ltd. All rights reserved.

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页码：971 / 975

页数：5

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