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Structure-guided discovery of a novel,potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor |
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| Authors: | David Sperandio Vangelis Aktoudianakis Kerim Babaoglu Xiaowu Chen Kristyna Elbel Gregory Chin Britton Corkey Jinfa Du Bob Jiang Tetsuya Kobayashi Richard Mackman Ruben Martinez Hai Yang Jeff Zablocki Saritha Kusam Kim Jordan Heather Webb Jamie G Bates David G Breckenridge |
| Institution: | 1. Department of Medicinal Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA;2. Department of Biology, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA;3. Department of Drug Metabolism, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA;4. Department of Structural Chemistry, Gilead Sciences, Inc., 333 Lakeside Drive, Foster City, CA 94404, USA |
| Abstract: | |
| Keywords: | Antitumor BET proteins Bromodomain inhibitor Epigenetic readers |
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