کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1254061 | 971335 | 2015 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Structure-based design of conformationally constrained cyclic peptidomimetics to target the MLL1-WDR5 protein–protein interaction as inhibitors of the MLL1 methyltransferase activity
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی (عمومی)
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
We described herein structure-based design, synthesis and evaluation of conformationally constrained, cyclic peptidomimetics to block the MLL1-WDR5 protein–protein interaction as inhibitors of the MLL1 histone methyltransferase activity. Our study has yielded cyclic peptidomimetics with very high binding affinities to WDR5 (Ki values <1 nmol/L) and function as antagonists of the MLL1 histone methyltransferase activity.
Structure-based design, synthesis and evaluation of high-affinity, conformationally constrained peptidomimetics as inhibitors of the WDR5-MLL1 protein–protein interaction and MLL1 methyltransferase activity are described.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Chinese Chemical Letters - Volume 26, Issue 4, April 2015, Pages 455–458
Journal: Chinese Chemical Letters - Volume 26, Issue 4, April 2015, Pages 455–458
نویسندگان
Hacer Karatas, Shirley Y. Lee, Elizabeth C. Townsend, Fang Cao, Jing Xu, Denzil Bernard, Liu Liu, Yali Dou, Shaomeng Wang,