Cited 22 time in
- Title
- Synthesis of tripeptides as potent Yersinia protein tyrosine phosphatase inhibitors = 여시니아 프로틴포스포타제 저해기능을 갖는 트리펩타이드 합성
- Author(s)
- Kyeong Lee; S K Boovanahalli; K Y Nam; S U Kang; MiJeoung Lee; J Phan; L Wu; D S Waugh; Z Y Zhang; K T No; Jung Joon Lee; T R Burke
- Bibliographic Citation
- Bioorganic & Medicinal Chemistry Letters, vol. 15, no. 18, pp. 4037-4042
- Publication Year
- 2005
- 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.
- Keyword
- bioterrorismPTP1BpTyr mimeticstripeptidesYopH
- ISSN
- 0960-894X
- Publisher
- Elsevier
- DOI
- http://dx.doi.org/10.1016/j.bmcl.2005.06.027
- Type
- Article
- Appears in Collections:
- 1. Journal Articles > Journal Articles
- Files in This Item:
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