Figures & data
Figure 1. Overview of bromodomain inhibition. Bromodomains recognize acetylation marks in histone tails and recruit transcriptional machinery promoting target gene transcription, such as in the case of c-MYC. Bromodomain inhibitors prevent interaction between the bromodomain and the acetyl group, causing the downregulation of certain genes. Bromodomains play a key role in gene transcription regulation.
Figure 2. Structure-based phylogeny of the human bromodomains and their inhibitors. There are 61 bromodomains in 46 bromodomain-containing proteins. Roman numerals indicate the eight major structural classes. The phylogenetic tree is derived from data obtained Filipakoupoulos at al. (ref 17). The specific inhibitors described in this review are indicated next to the corresponding bromodomain.
Figure 3. BET bromodomain inhibitor molecules. (+)-JQ1, I-BET762, OTX015, I-BET151, CPI203, PFI-1, MS436, CPI-0610 chemical structures are shown. RVX2135, FT-1101, BAY1238097, INCB054329, TEN-010, GSK2820151, ZEN003694, BAY-299, BMS-986158, ABBV-075, GS-5829, and PLX51107 are BET bromodomain inhibitors that are under clinical trial and whose structure has not been disclosed.
Table 1. BET inhibitors
Table 2. Non-BET inhibitors
Figure 4. Non-BET bromodomain inhibitor molecules. Chemical structures of non-BET inhibitors, clustered according to the specific bromodomains in which they act. Bromosporine is a multibromodomain inhibitor.
