کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1378118 | 981994 | 2005 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis of tripeptides as potent Yersinia protein tyrosine phosphatase inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
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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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 18, 15 September 2005, Pages 4037–4042
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 18, 15 September 2005, Pages 4037–4042
نویسندگان
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.,