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
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Design and evaluation of 1,7-naphthyridones as novel KDM5 inhibitors
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).

Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 18, 15 September 2016, Pages 4492–4496
نویسندگان
, , , , , , , , , , , , , , ,