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• W2607118599 abstract "Bromodomains (BD) are readers of lysine acetylation marks present in numerous proteins associated with chromatin. Here we describe a dual inhibitor of the bromodomain and PHD finger (BRPF) family member BRPF2 and the TATA box binding protein-associated factors TAF1 and TAF1L. These proteins are found in large chromatin complexes and play important roles in transcription regulation. The substituted benzoisoquinolinedione series was identified by high-throughput screening, and subsequent structure–activity relationship optimization allowed generation of low nanomolar BRPF2 BD inhibitors with strong selectivity against BRPF1 and BRPF3 BDs. In addition, a strong inhibition of TAF1/TAF1L BD2 was measured for most derivatives. The best compound of the series was BAY-299, which is a very potent, dual inhibitor with an IC50 of 67 nM for BRPF2 BD, 8 nM for TAF1 BD2, and 106 nM for TAF1L BD2. Importantly, no activity was measured for BRD4 BDs. Furthermore, cellular activity was evidenced using a BRPF2– or TAF1–histone H3.3 or H4 interaction assay." @default.
• W2607118599 created "2017-04-28" @default.
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• W2607118599 date "2017-05-01" @default.
• W2607118599 modified "2023-10-10" @default.
• W2607118599 title "Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains" @default.
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• W2607118599 cites W1835221221 @default.
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• W2607118599 cites W1969672293 @default.
• W2607118599 cites W1978867804 @default.
• W2607118599 cites W1994563738 @default.
• W2607118599 cites W2001641653 @default.
• W2607118599 cites W2003872705 @default.
• W2607118599 cites W2008022683 @default.
• W2607118599 cites W2015681476 @default.
• W2607118599 cites W2022694548 @default.
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• W2607118599 cites W2043620462 @default.
• W2607118599 cites W2043816982 @default.
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• W2607118599 cites W2057460011 @default.
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• W2607118599 cites W2088947549 @default.
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• W2607118599 cites W2144081223 @default.
• W2607118599 cites W2154714625 @default.
• W2607118599 cites W2163341755 @default.
• W2607118599 cites W2184580009 @default.
• W2607118599 cites W2202769927 @default.
• W2607118599 cites W2210685190 @default.
• W2607118599 cites W2222589778 @default.
• W2607118599 cites W2261819980 @default.
• W2607118599 cites W2262681364 @default.
• W2607118599 cites W2274338038 @default.
• W2607118599 cites W2286533764 @default.
• W2607118599 cites W2286718346 @default.
• W2607118599 cites W2308896320 @default.
• W2607118599 cites W2331846333 @default.
• W2607118599 cites W2335442430 @default.
• W2607118599 cites W2337020460 @default.
• W2607118599 cites W2346149257 @default.
• W2607118599 cites W2346501107 @default.
• W2607118599 cites W2399229449 @default.
• W2607118599 cites W2404861930 @default.
• W2607118599 cites W2411462408 @default.
• W2607118599 cites W2414011796 @default.
• W2607118599 cites W2417500499 @default.
• W2607118599 cites W2510334948 @default.
• W2607118599 cites W2519263923 @default.
• W2607118599 cites W2523675873 @default.
• W2607118599 cites W2524202321 @default.
• W2607118599 cites W2570397282 @default.
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• W2607118599 doi "https://doi.org/10.1021/acs.jmedchem.7b00306" @default.
• W2607118599 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/5443610" @default.

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