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Overview
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Background
SGC-CBP 30 is a selective inhibitor of CREBBP and EP300 with IC50 value of 21 nM and 38 nM, respectively [1]. EP300 (E1A binding protein p300) is encoded by EP300 gene and plays an important role in regulating cell growth and division, prompting cells mature and assume specialized functions, and preventing tumor cells growth. CREBBP (CREB-binding protein) is encoded by CREBBP gene and involves in the transcriptional coactivation of many different transcription factors [2].
[1]. Duncan A. Hay, Oleg Fedorov, Sarah Martin, et al. Discovery and Optimization of Small-Molecule Ligands for the CBP/p300 Bromodomains [J]. J. Am. Chem. Soc., 2014, 136 (26), pp 9308–9319.
[2]. van Belzen M, Bartsch O, Lacombe D, et al. Rubinstein-Taybi syndrome (CREBBP, EP300) [J]. Eur J Hum Genet. 2011 Jan; 19(1):preceeding 118-20.
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Overview