کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1369428 | 1379505 | 2016 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design and evaluation of 1,7-naphthyridones as novel KDM5 inhibitors
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Features from a high throughput screening (HTS) hit and a previously reported scaffold were combined to generate 1,7-naphthyridones as novel KDM5 enzyme inhibitors with nanomolar potencies. These molecules exhibited high selectivity over the related KDM4C and KDM2B isoforms. An X-ray co-crystal structure of a representative molecule bound to KDM5A showed that these inhibitors are competitive with the co-substrate (2-oxoglutarate or 2-OG).
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 18, 15 September 2016, Pages 4492–4496
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 18, 15 September 2016, Pages 4492–4496
نویسندگان
Sharada S. Labadie, Peter S. Dragovich, Richard T. Cummings, Gauri Deshmukh, Amy Gustafson, Ning Han, Jean-Christophe Harmange, James R. Kiefer, Yue Li, Jun Liang, Bianca M. Liederer, Yichin Liu, Wanda Manieri, Wiefeng Mao, Lesley Murray,