Bromodomain proteins are involved in a diverse range of functions, such as acetylating histones, remodeling chromatin, and recruiting other factors necessary for transcription. These proteins thus play a critical role in the regulation of transcription.
How many Bromodomains are there?
The 61 different bromodomains found in the human proteome are located in 46 proteins and several of them represent interesting pharmaceutical targets for the treatment of inflammatory diseases, viral infections and cancer [62].
How many Bromo domains could a protein have?
three domains
The group of proteins containing these three domains is termed the Bromodomain and Extra-Terminal Domain (BET) family. Based on the structural and functional similarities among the four paralogous genes, mammalian Ring3, Orfx, Mcap, and Brdt are simply named as Brd2, Brd3, Brd4, and Brdt, respectively.
How do bet inhibitors work?
BET inhibitors are a class of drugs that reversibly bind the bromodomains of Bromodomain and Extra-Terminal motif (BET) proteins BRD2, BRD3, BRD4, and BRDT, and prevent protein-protein interaction between BET proteins and acetylated histones and transcription factors.
What is acetylation in drug metabolism?
Acetylation is a very common metabolic reaction which occurs with amino, hydroxyl or sulfhydryl groups. The acetyl group is transferred from acetyl-coenzyme A and the reaction is catalysed by acetyltransferases. In a few cases, the conjugates are further metabolized to toxic compounds, as is seen with isoniazid.
What bet drugs?
From Wikipedia, the free encyclopedia. BET inhibitors are a class of drugs that reversibly bind the bromodomains of Bromodomain and Extra-Terminal motif (BET) proteins BRD2, BRD3, BRD4, and BRDT, and prevent protein-protein interaction between BET proteins and acetylated histones and transcription factors.
