title: Development of small molecule inhibitors of BRPF1 and TRIM24 bromodomains.
abstract: The entry of small molecule inhibitors of the bromodomain and extra C-terminal domain (BET) family of bromodomains into the clinic has demonstrated the therapeutic potential for this class of epigenetic acetyl-lysine reader proteins. Within the past two years, the development of potent inhibitors for the bromodomain and PHD finger containing protein (BRPF) family and the tripartite motif containing protein 24 (TRIM24) have been reported and are the subject of this review. Both proteins contain other domains with diverse functions and can also be part of a complex of proteins which have implications in epigenetic signaling and disease. These new small molecule tools will be useful for unraveling the biological contribution of the bromodomain and enable pharmacological validation of these proteins.
authors: Institute for Applied Cancer Science, The University of Texas MD Anderson Cancer Center, Houston, TX 77054, USA. Electronic address: wpalmer@mdanderson.org.
authors: Wylie S
authors: WS
authors: Palmer
mesh_terms: D048868:Adaptor Proteins, Signal Transducing / Q000037:antagonists & inhibitors* / Q000737:chemistry; D000818:Animals; D002352:Carrier Proteins / Q000037:antagonists & inhibitors* / Q000737:chemistry; D004268:DNA-Binding Proteins; D006801:Humans; D009687:Nuclear Proteins / Q000037:antagonists & inhibitors* / Q000737:chemistry; D000072417:Protein Domains; D000092468:Bromodomain Containing Proteins
chemical_list: D048868:Adaptor Proteins, Signal Transducing; D002352:Carrier Proteins; D004268:DNA-Binding Proteins; D009687:Nuclear Proteins; C086011:BRPF1 protein, human; D000092468:Bromodomain Containing Proteins; C555317:TRIM24 protein, human