BRD9 explained

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

Notes and References

1. Web site: Entrez Gene: Bromodomain containing 9.
2. 23644491. 3667980. 2013. Kadoch. C. Proteomic and bioinformatic analysis of mammalian SWI/SNF complexes identifies extensive roles in human malignancy. Nature Genetics. 45. 6. 592–601. Hargreaves. D. C.. Hodges. C. Elias. L. Ho. L. Ranish. J. Crabtree. G. R.. 10.1038/ng.2628.
3. 18328944. 2008. Kang. J. U.. 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. Koo. S. H.. Kwon. K. C.. Park. J. W.. Kim. J. M.. 10.1016/j.cancergencyto.2007.12.004.
4. 24313754. 3906316. 2014. Fedorov. O. 1,2,4triazolo4,3-aphthalazines: Inhibitors of diverse bromodomains. Journal of Medicinal Chemistry. 57. 2. 462–76. 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.. 10.1021/jm401568s.
5. 25864491. 2015. Clark. P. G.. LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor. Angewandte Chemie International Edition. 6217–6221. 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.. 10.1002/anie.201501394 . 54 . 21. 4449114.
6. 25856009. 2015. Theodoulou. N. H.. The Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition. Journal of Medicinal Chemistry. 59. 4. 1425–1439. 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.. 10.1021/acs.jmedchem.5b00256. 7354103. free.