Title of article
Synthesis of tripeptides as potent Yersinia protein tyrosine phosphatase inhibitors
Author/Authors
Kyeong Lee، نويسنده , , Shanthaveerappa K. Boovanahalli، نويسنده , , Ky-Youb Nam، نويسنده , , Sang Uk Kang، نويسنده , , Mijeoung Lee، نويسنده , , Jason Phan، نويسنده , , Li Wu، نويسنده , , David S. Waugh، نويسنده , , Zhong-Yin Zhang، نويسنده , , Kyoung Tai No، نويسنده , , Jung Jun Lee، نويسنده , , Terrence R. Burke Jr.، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
6
From page
4037
To page
4042
Abstract
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.
Keywords
Tripeptides , Bioterrorism , YopH , pTyr mimetics , PTP1B
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795929
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