کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1358556 | 981349 | 2016 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
A phenotypic drug discovery study on thienodiazepine derivatives as inhibitors of T cell proliferation induced by CD28 co-stimulation leads to the discovery of a first bromodomain inhibitor
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A phenotypic screening of thienodiazepines derived from a hit compound found through a binding assay targeting co-stimulatory molecules on T cells and antigen presenting cells successfully led to the discovery of a thienotriazolodiazepine compound (7f) possessing potent immunosuppressive activity. A chemical biology approach has succeeded in revealing that 7f is a first inhibitor of epigenetic bromodomain-containing proteins. 7f is expected to become an anti-cancer agent as well as an immunosuppressive agent.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 5, 1 March 2016, Pages 1365–1370
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 5, 1 March 2016, Pages 1365–1370
نویسندگان
Junichi Endo, Hidemasa Hikawa, Maiko Hamada, Seigo Ishibuchi, Naoto Fujie, Naoki Sugiyama, Minoru Tanaka, Haruhito Kobayashi, Kunio Sugahara, Koichi Oshita, Kazunori Iwata, Shinsuke Ooike, Meguru Murata, Hiroshi Sumichika, Kenji Chiba, Kunitomo Adachi,