BRPFs (bromodomain and PHD finger-containing proteins) are multidomain  proteins of the Trithorax group (TrxG): regulatory proteins composed of diverse, evolutionary conserved units that form chromatin-associated complexes accounting for epigenetic transcriptional memory. Three BRPFs are known to date, sharing >65% homology in their ~100 amino acid counting sequences, all sharing an acetylated lysine (KAc) recognition site that closely resembles other bromodomains, including those of the BETs[1]. BRPF1 (also known as Br140 and Peregrin) is a component of complexes containing the MOZ/MORF transcriptional coactivators, that links the catalytic HATs to the other subunits ING5 and hEAF6. Furthermore, BRPF1 contains PHD fingers, a bromodomain and a PWWP domain[2]. It has been shown that BRPF1 has a central role during development, since mutations have shown to display anterior transformations of pharyngeal arches due to progressive loss of anterior Hox gene expression. What’s more, translocations of MOZ are associated with aggressive subtypes of leukemia, and make BRPF1 an interesting target in oncology related research[3].

[1] E.H. Demont et al. 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. ACS Med Chem Lett. 2014 Sep 10;5(11):1190-5.
[2] K. Laue et al. The multidomain protein Brpf1 binds histones and is required for Hox gene expression and segmental identity. Development. 2008 Jun;135(11):1935-46.
[3] L. You et al. The chromatin regulator brpf1 regulates embryo development and cell proliferation. J Biol Chem. 2015 May 1;290(18):11349-64.

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Axon ID Name Description From price
2410 GSK 5959 Potent, cell permeable inhibitor of BRPF1 bromodomain €135.00
3186 NVS-BPTF-1 Potent, selective and cell active chemical probe for BPTF €180.00
2442 OF-1 Potent bromodomain inhibitor (BRPF1 and BRPF2 selective) €80.00

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