کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1375466 | 981939 | 2005 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Preparation of human Melanocortin-4 receptor agonist libraries: Linear peptides X-Y-DPhe7-Arg8-Trp(or 2-Nal)9-Z-NH2
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Two libraries of hMC4R agonists, X-Y-DPhe7-Arg8-2-Nal9-Z-NH2 and X-Y-DPhe7-Arg8-Trp9-Z-NH2, totaling 185 peptides were prepared using Irori tagging technology and Argonaut Quest 210 Synthesizer, where X stands for N-caps, Y for His6 surrogates, and Z for Gly10 surrogates. As a result of this study, pentapeptides with Trp were found to be more hMC4R potent than the corresponding 2-Nal analogs, novel N-caps and Gly surrogates were identified, and 19 new peptides which are potent hMC4R agonists (EC50 1-15Â nM) and selective against hMC1R were discovered.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 24, 15 December 2005, Pages 5504-5508
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 24, 15 December 2005, Pages 5504-5508
نویسندگان
Adrian Wai-Hing Cheung, Lida Qi, Vijay Gore, Xin-Jie Chu, David Bartkovitz, Grazyna Kurylko, Joseph Swistok, Waleed Danho, Li Chen, Keith Yagaloff,