BRD9

Bromodomain-containing protein 9 is a protein that in humans is encoded by the BRD9 gene. [1]

Structure and interaction

BRD9 contains a bromodomain. It is closely related to BRD7. BRD9 is present in some SWI/SNF ATPase remodeling complexes.[2]

Role in cancer

The BRD9 gene is frequently present in variable copy number in lung cancer.[3]

Small molecule inhibition

Small molecules capable of binding to the bromodomain of BRD9 have been developed.[4][5][6]

See also

Bromodomain

References

  1. ↑ "Entrez Gene: Bromodomain containing 9".
  2. ↑ Kadoch, C; Hargreaves, D. C.; Hodges, C; Elias, L; Ho, L; Ranish, J; Crabtree, G. R. (2013). "Proteomic and bioinformatic analysis of mammalian SWI/SNF complexes identifies extensive roles in human malignancy". Nature Genetics. 45 (6): 592–601. doi:10.1038/ng.2628. PMC 3667980Freely accessible. PMID 23644491.
  3. ↑ Kang, J. U.; Koo, S. H.; Kwon, K. C.; Park, J. W.; Kim, J. M. (2008). "Gain at chromosomal region 5p15.33, containing TERT, is the most frequent genetic event in early stages of non-small cell lung cancer". Cancer Genetics and Cytogenetics. 182 (1): 1–11. doi:10.1016/j.cancergencyto.2007.12.004. PMID 18328944.
  4. ↑ Fedorov, O; Lingard, H; Wells, C; Monteiro, O. P.; Picaud, S; Keates, T; Yapp, C; Philpott, M; Martin, S. J.; Felletar, I; Marsden, B. D.; Filippakopoulos, P; Müller, S; Knapp, S; Brennan, P. E. (2014). "1,2,4triazolo4,3-aphthalazines: Inhibitors of diverse bromodomains". Journal of Medicinal Chemistry. 57 (2): 462–76. doi:10.1021/jm401568s. PMC 3906316Freely accessible. PMID 24313754.
  5. ↑ Clark, P. G.; Vieira, L. C.; Tallant, C; Fedorov, O; Singleton, D. C.; Rogers, C. M.; Monteiro, O. P.; Bennett, J. M.; Baronio, R; Müller, S; Daniels, D. L.; Méndez, J; Knapp, S; Brennan, P. E.; Dixon, D. J. (2015). "LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor". Angewandte Chemie International Edition: n/a. doi:10.1002/anie.201501394. PMID 25864491.
  6. ↑ Theodoulou, N. H.; Bamborough, P; Bannister, A. J.; Becher, I; Bit, R. A.; Che, K. H.; Chung, C. W.; Dittmann, A; Drewes, G; Drewry, D. H.; Gordon, L; Grandi, P; Leveridge, M; Lindon, M; Michon, A. M.; Molnar, J; Robson, S. C.; Tomkinson, N. C.; Kouzarides, T; Prinjha, R. K.; Humphreys, P. G. (2015). "The Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition". Journal of Medicinal Chemistry: 150430080108003. doi:10.1021/acs.jmedchem.5b00256. PMID 25856009.


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