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Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
Bromodomain (BRD)-containing kinases initiate acetylation-dependent assembly of transcriptional regulator complexes by binding to (or 'reading') acetyl-lysine marks on histone tails. The regulator complexes thus formed, control expression of sets of proteins which alter the cellular phenotype in specific ways. (BRD)-containing proteins are exciting targets for the development of novel small molecule therapeutics in the areas of cancer, inflammation and viral infection .
1. Filippakopoulos P, Knapp S. (2014) Targeting bromodomains: epigenetic readers of lysine acetylation. Nat Rev Drug Discov, 13 (5): 337-56. [PMID:24751816]
2. Picaud S, Wells C, Felletar I, Brotherton D, Martin S, Savitsky P, Diez-Dacal B, Philpott M, Bountra C, Lingard H et al.. (2013) RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc. Natl. Acad. Sci. U.S.A., 110 (49): 19754-9. [PMID:24248379]
3. Theodoulou NH, Bamborough P, Bannister AJ, Becher I, Bit RA, Che KH, Chung CW, Dittmann A, Drewes G, Drewry DH et al.. (2015) Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition. J. Med. Chem., [Epub ahead of print]. [PMID:25856009]
Database page citation:
Bromodomain kinase (BRDK) family. Accessed on 29/03/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=558.
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Fabbro D, Kelly E, Marrion N, Peters JA, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Southan C, Davies JA and CGTP Collaborators (2015) The Concise Guide to PHARMACOLOGY 2015/16: Enzymes. Br J Pharmacol. 172: 6024-6109.