کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1377821 | 981989 | 2006 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Crystal structure of human ERK2 complexed with a pyrazolo[3,4-c]pyridazine derivative
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A series of pyrazolopyridazine compounds were briefly investigated as ERK2 inhibitors. The crystal structure of ERK2 complexed with an allyl derivative was determined. The compound induces structural change including movement of the glycine-rich loop and peptide flip between Met108-Glu109. As a result, the newly formed subsite can recognize small hydrophobic substituents but not hydrophilic ones.
A series of pyrazolopyridazine compounds were briefly investigated as ERK2 inhibitors. The crystal structure of ERK2 complexed with the allyl derivative provides structural insight which could be used in the design of more potent ERK2 inhibitors.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 1, 1 January 2006, Pages 55–58
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 1, 1 January 2006, Pages 55–58
نویسندگان
Takayoshi Kinoshita, Masaichi Warizaya, Makoto Ohori, Kentaro Sato, Masahiro Neya, Takashi Fujii,