کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1378887 | 982012 | 2006 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design and synthesis of selective, high-affinity inhibitors of human cytochrome P450 2J2
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
The active site topology, substrate specificity, and biological roles of the human cytochrome P450 CYP2J2, which is mainly expressed in the cardiovascular system, are poorly known even though recent data suggest that it could be a novel biomarker and potential target for therapy of human cancer. This paper reports a first series of high-affinity, selective CYP2J2 inhibitors that are related to terfenadine, with Ki values as low as 160 nM, that should be useful tools to determine the biological roles of CYP2J2.
A series of terfenadine analogs were synthetized and evaluated as human CYP2J2 inhibitors. Some of these compounds are high-affinity, selective inhibitors of this enzyme (R = Pr, Ki = 160 nM).Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 10, 15 May 2006, Pages 2777–2780
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 10, 15 May 2006, Pages 2777–2780
نویسندگان
Pierre Lafite, Sylvie Dijols, Didier Buisson, Anne-Christine Macherey, Darryl C. Zeldin, Patrick M. Dansette, Daniel Mansuy,