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Title 

Synthesis of tripeptides as potent Yersinia protein tyrosine phosphatase inhibitors

 

여시니아 프로틴포스포타제 저해기능을 갖는 트리펩타이드 합성

Authors 

Kyeong LeeS K BoovanahalliK Y NamS U KangMiJeoung LeeJ PhanL WuD S WaughZ Y ZhangK T NoJung Joon LeeT R Burke

Publisher 

Elsevier

Issue Date 

2005

Citation 

Bioorganic & Medicinal Chemistry Letters, vol. 15, no. 18, pp. 4037-4042

Keywords 

bioterrorismPTP1BpTyr mimeticstripeptidesYopHprotein tyrosine phosphatase 1Bprotein tyrosine phosphatase inhibitordrug synthesisyersiniabacterial outer membrane proteins

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.

ISSN 

0960-894X

Link 

http://dx.doi.org/10.1016/j.bmcl.2005.06.027

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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