| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1378118 | Bioorganic & Medicinal Chemistry Letters | 2005 | 6 Pages |
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Kyeong Lee, Shanthaveerappa K. Boovanahalli, Ky-Youb Nam, Sang-Uk Kang, Mijeoung Lee, Jason Phan, Li Wu, David S. Waugh, Zhong-Yin Zhang, Kyoung Tai No, Jung Jun Lee, Terrence R. Burke Jr.,