Bromodomains bind proteins with acetylated lysine residues, such as histones, to regulate gene transcription. Listed herein are examples of bromodomain-containing proteins for which sufficient pharmacology exists.

* Key recommended reading is highlighted with an asterisk

Brand M, Measures AR, Measures AM, Wilson BG, Cortopassi WA, Alexander R, Höss M, Hewings DS, Rooney TP, Paton RS et al.. (2015) Small molecule inhibitors of bromodomain-acetyl-lysine interactions. ACS Chem Biol, 10 (1): 22-39. [PMID:25549280]

Filippakopoulos P, Knapp S. (2014) Targeting bromodomains: epigenetic readers of lysine acetylation. Nat Rev Drug Discov, 13 (5): 337-56. [PMID:24751816]

* Fujisawa T, Filippakopoulos P. (2017) Functions of bromodomain-containing proteins and their roles in homeostasis and cancer. Nat Rev Mol Cell Biol, 18 (4): 246-262. [PMID:28053347]

Gallenkamp D, Gelato KA, Haendler B, Weinmann H. (2014) Bromodomains and their pharmacological inhibitors. ChemMedChem, 9 (3): 438-64. [PMID:24497428]

* Myrianthopoulos V, Mikros E. (2019) From bench to bedside, via desktop. Recent advances in the application of cutting-edge in silico tools in the research of drugs targeting bromodomain modules. Biochem Pharmacol, 159: 40-51. [PMID:30414936]

* Nicholas DA, Andrieu G, Strissel KJ, Nikolajczyk BS, Denis GV. (2017) BET bromodomain proteins and epigenetic regulation of inflammation: implications for type 2 diabetes and breast cancer. Cell Mol Life Sci, 74 (2): 231-243. [PMID:27491296]

* Ramadoss M, Mahadevan V. (2018) Targeting the cancer epigenome: synergistic therapy with bromodomain inhibitors. Drug Discov Today, 23 (1): 76-89. [PMID:28943305]

Sanchez R, Meslamani J, Zhou MM. (2014) The bromodomain: from epigenome reader to druggable target. Biochim Biophys Acta, 1839 (8): 676-85. [PMID:24686119]

* Spriano F, Stathis A, Bertoni F. (2020) Targeting BET bromodomain proteins in cancer: The example of lymphomas. Pharmacol Ther, 215: 107631. [PMID:32693114]

* Tang P, Zhang J, Liu J, Chiang CM, Ouyang L. (2021) Targeting Bromodomain and Extraterminal Proteins for Drug Discovery: From Current Progress to Technological Development. J Med Chem, 64 (5): 2419-2435. [PMID:33616410]

Theodoulou NH, Tomkinson NC, Prinjha RK, Humphreys PG. (2016) Clinical progress and pharmacology of small molecule bromodomain inhibitors. Curr Opin Chem Biol, 33: 58-66. [PMID:27295577]

Theodoulou NH, Tomkinson NC, Prinjha RK, Humphreys PG. (2016) Progress in the Development of non-BET Bromodomain Chemical Probes. ChemMedChem, 11 (5): 477-87. [PMID:26749027]

1. Fedorov O, Lingard H, Wells C, Monteiro OP, Picaud S, Keates T, Yapp C, Philpott M, Martin SJ, Felletar I et al.. (2014) [1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains. J Med Chem, 57 (2): 462-76. [PMID:24313754]

2. SGC. GSK2801: A Selective Chemical Probe for BAZ2B/A bromodomains. Accessed on 03/03/2015. Modified on 04/08/2023. thesgc.org, https://www.thesgc.org/chemical-probes/GSK2801

3. SGC. I-CBP112 A CREBBP/EP300-selective chemical probe. Accessed on 04/08/2023. Modified on 04/08/2023. thesgc.org, https://www.thesgc.org/chemical-probes/I-CBP112

4. SGC. PFI-3 A Selective chemical probe for SMARCA bromodomains. Accessed on 10/11/2014. Modified on 04/08/2023. thesgc.org, https://www.thesgc.org/chemical-probes/PFI-3

5. Taylor AM, Bailey C, Belmont LD, Campbell R, Cantone N, Côté A, Crawford TD, Cummings R, DeMent K, Duplessis M et al.. (2022) GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1. J Med Chem, 65 (16): 11177-11186. [PMID:35930799]

6. Welti J, Sharp A, Brooks N, Yuan W, McNair C, Chand SN, Pal A, Figueiredo I, Riisnaes R, Gurel B et al.. (2021) Targeting the p300/CBP Axis in Lethal Prostate Cancer. Cancer Discov, 11 (5): 1118-1137. [PMID:33431496]