کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1379580 | 982032 | 2005 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Boro-norleucine as a P1 residue for the design of selective and potent DPP7 inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Dipeptide-based inhibitors with C-substituted (alkyl or aminoalkyl) α-amino acids in the P2 position and boro-norleucine (boro-Nle) in the P1 position were synthesized. Relative to boro-proline, boro-Nle as a P1 residue was shown able to significantly dial out DPP4, FAP, DPP8, and DPP9 activity. Dab-boro-Nle (4g) proved to be the most selective and potent DPP7 inhibitor with a DPP7 IC50 value of 480 pM.
Dipeptide-based dipeptidyl peptidase inhibitors with C-substituted (alkyl or aminoalkyl) α-amino acids in the P2 position and boro-norleucine (boro-Nle) in the P1 position were synthesized. Dab-boro-Nle (4g) proved to be the most selective and potent DPP7 inhibitor with a DPP7 IC50 value of 480 pM.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 19, 1 October 2005, Pages 4256–4260
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 19, 1 October 2005, Pages 4256–4260
نویسندگان
Kevin R. Shreder, Melissa S. Wong, Sergio Corral, Zhizhou Yu, David T. Winn, Min Wu, Yi Hu, Tyzoon Nomanbhoy, Senaiet Alemayehu, Stacy R. Fuller, Jonathan S. Rosenblum, John W. Kozarich,