کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1377618 981982 2007 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Discovery and structure–activity relationship studies of indole derivatives as liver X receptor (LXR) agonists
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Discovery and structure–activity relationship studies of indole derivatives as liver X receptor (LXR) agonists
چکیده انگلیسی

A structurally novel liver X receptor (LXR) agonist (1) was identified from internal compound collection utilizing the combination of structure-based virtual screening and high-throughput gene profiling. Compound 1 increased ABCA1 gene expression by eightfold and SREBP1c by threefold in differentiated THP-1 macrophage cell lines. Confirmation of its agonistic activity against LXR was obtained in the co-factor recruitment and reporter transactivation assays. Structure–activity relationship studies on compound 1 are described.

A structurally novel LXR agonist (1) was identified utilizing the combination of virtual screening and high-throughput gene profiling. Structure–activity relationship studies on 1 are described.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 12, 15 June 2007, Pages 3473–3479
نویسندگان
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