Browsing by Author "Qi, Jun"

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Development of Dimethylisoxazole-Attached Imidazo[1,2‑a]pyridines as Potent and Selective CBP/P300 Inhibitors

Muthengi, Alex; Wimalasena, Virangika K.; Yosief, Hailemichael O.; Bikowitz, Melissa J.; Sigua, Logan H.; Wang, Tingjian; Li, Deyao; Zhang, Wei; Qi, Jun; Schönbrunn, Ernst; Amaro, Rommie E.; Erickson, Jon; Liu, Shuai; Dhawan, Gagan; Gaieb, Zied (2021)

The use of epigenetic bromodomain inhibitors as anticancer therapeutics has transitioned from targeting bromodo main extraterminal domain (BET) proteins into targeting non-BET bromodomains. The two most relevant non-BET ...
Structure-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors

Liu, Shuai; Yosief, Hailemichael O.†; Dai, Lingling; Huang, He; Dhawan, Gagan; Zhang, Xiaofeng; Muthengi, Alex; Roberts, Justin; Buckley, Dennis L.; Perry, Jennifer A.; Wu, Lei; Bradner, James E.; Qi, Jun; Zhang, Wei (2018)

The simultaneous inhibition of polo-like kinase 1 (PLK1) and BRD4 bromodomain by a single molecule could lead to the development of an effective therapeutic strategy for a variety of diseases in which PLK1 and BRD4 are ...