کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1370139 | 981809 | 2011 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery, optimisation and in vivo evaluation of novel GPR119 agonists
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
GPR119 is increasingly seen as an attractive target for the treatment of type II diabetes and other elements of the metabolic syndrome. During a programme aimed at developing agonists of the GPR119 receptor, we identified compounds that were potent with reduced hERG liabilities, that had good pharmacokinetic properties and that displayed excellent glucose-lowering effects in vivo. However, further profiling in a GPR119 knock-out (KO) mouse model revealed that the biological effects were not exclusively due to GPR119 agonism, highlighting the value of transgenic animals in drug discovery programs.
Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 24, 15 December 2011, Pages 7310–7316
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 24, 15 December 2011, Pages 7310–7316
نویسندگان
Katy J. Brocklehurst, Anders Broo, Roger J. Butlin, Hayley S. Brown, David S. Clarke, Öjvind Davidsson, Kristin Goldberg, Sam D. Groombridge, Elizabeth E. Kelly, Andrew Leach, Darren McKerrecher, Charles O’Donnell, Simon Poucher, Paul Schofield,