Synthesis of tripeptides as potent Yersinia protein tyrosine phosphatase inhibitors

K Lee, SK Boovanahalli, KY Nam, SU Kang…

文献索引：Lee, Kyeong; Boovanahalli, Shanthaveerappa K.; Nam, Ky-Youb; Kang, Sang-Uk; Lee, Mijeoung; Phan, Jason; Wu, Li; Waugh, David S.; Zhang, Zhong-Yin; Kyoung, Tai No; Jung, Jun Lee; Burke Jr., Terrence R. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 18 p. 4037 - 4042

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被引用次数: 21

摘要

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- ...