کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1365198 | 981554 | 2008 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Aryl–indolyl maleimides as inhibitors of CaMKIIδ. Part 3: Importance of the indole orientation
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A family of aryl-substituted maleimides was prepared and studied for their activity against calmodulin dependant kinase. Inhibitory activities against the enzyme ranged from 10 nM to >20 μM and were dependant upon both the nature of the aryl group and the tether joining the basic amine to the indolyl maleimide core of the inhibitors. Key interactions with the kinase ATP site and hinge region, predicted by homology modeling, were confirmed.
Aryl-substituted maleimides were prepared and studied for their activity against CaMKII. Inhibitory activities ranged from 10 nM to >20 μM. Key predicted interactions with the kinase ATP site and hinge region were confirmed.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 7, 1 April 2008, Pages 2399–2403
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 7, 1 April 2008, Pages 2399–2403
نویسندگان
Qing Lu, Zheng Chen, John Perumattam, Dan-Xiong Wang, Weiling Liang, Yong-jin Xu, Steven Do, Llorente Bonaga, Jeffrey Higaki, Hanmin Dong, Albert Liclican, Steve Sideris, Maureen Laney, Sundeep Dugar, Babu Mavunkel, Daniel E. Levy,