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Item No. 11509

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Bromodomain-containing protein 9 (BRD9) is a member of family IV bromodomains.1 It is composed of an N-terminal bromodomain that recognizes acetyl-, propionyl- and butyryllysine modifications on histones and a C-terminal DUF3512 domain, and is a component of the SWI/SNF chromatin remodeling complex.2,3 BRD9 is involved in transcriptional regulation, androgen receptor signaling, inflammation, viral defense, and homologous recombination.4,5,6,7 Inhibition of BRD9 by the small molecule I-BRD9 (Item No. 17749) or PROTAC dBRD9 (Item No. 45720) inhibits the proliferation of prostate cancer cells in vitro, and knockdown of BRD9 reduces tumor growth in an LNCaP prostate cancer mouse xenograft model.4 BRD9 mutations have been found in patients with Sézary syndrome, an aggressive form of cutaneous T cell lymphoma (CTCL).8
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1. Biological function and histone recognition of family IV bromodomain-
2. A subset of human bromodomains recognizes butyryllysine and crotonyllysine histone peptide modifications. Structure 23(10), 1801-1814 (2015).
3. Mammalian SWI/SNF complexes in cancer: Emerging therapeutic opportunities. Curr. Opin. Genet. Dev. 42, 56-67 (2017).
4. BRD9 is a critical regulator of androgen receptor signaling and prostate cancer progression. Cancer Res. 81(4), 820-833 (2021).
5. Bromodomain containing 9 (BRD9) regulates macrophage inflammatory responses by potentiating glucocorticoid receptor activity. Proc. Natl. Acad. Sci. USA 118(35), e2109517118 (2021).
6. BRD9 is a druggable component of interferon-
7. The bromodomain containing protein BRD-
8. The mutational landscape of cutaneous T cell lymphoma and Sézary syndrome. Nat. Genet. 47(12), 1465-1470 (2015).