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 ,
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
