期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 60, 期 2, 页码 695-709出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.6b01566
关键词
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p300/CREB binding pi-otein associated factor (PCAF/KAT2B) and general control nonderepressible 5 (GCNS/KAT2A) are multidomain proteins that have been implicated in retroviral infection, inflammation pathways, and cancer development. However, outside of viral replication, little is known about the dependence of these effects on the C-terminal bromodomain. Herein, we report GSK4027 as a chemical probe for the PCAF/GCN5 bromodomain, together with GSK4028 as an enantiomeric negative control. The probe was optimized from a weakly potent, nonselective p-yridazinone hit to deliver high potency for the PCAF/GCNS bromodomain, high solubility, cellular target engagement, and >= 18000-fold selectivity over the BET family, together with >= 70-fold selectivity over the wider bromodomain families.
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