Bromodomains: A New Target Class for Drug Development
A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".
Deadline for manuscript submissions: closed (15 November 2022) | Viewed by 10728
Special Issue Editors
Interests: bromodomain; epigenetics; drug discovery
Special Issue Information
Dear Colleagues,
Epigenetic proteins, including histone writers, readers and erasers, modulate the epigenetic landscape of cells which impacts upon gene expression and cell state. Increasing evidence suggests that epigenetic protein function can be dysregulated in neoplastic cell states. Intensive studies by many groups have focused on the bromodomain, an epigenetic reader domain that recognizes acetylated protein and is broadly dysregulated in distinct cancer and disease states. Thus, bromodomains have enormous potential as targets for novel therapeutic development in cancer. An explosion of interest in these proteins was facilitated by the establishment of small molecule inhibitors with great selectivity and potency both in vitro and in vivo. Widespread use of these molecules, especially JQ1 and I-BET762 (Filippakopoulos et al., 2010; Nicodeme et al., 2010), to probe cell responses has led to widely applicable insights into the mechanisms of how inhibition of epigenetic readers impacts transcriptional programs in cancer cells, resulting in differentiation and apoptosis. On the basis of these promising early results, BET inhibitors have entered human clinical investigations for the treatment of different cancers and other diseases (Alqahtani et al., 2019). Next-generation compounds targeting BET bromodomains have been generated using proteolysis-targeted chimera (PROTAC) chemistry, in order to induce targeted degradation of BET proteins (Winter et al., 2015). In parallel, further non-BET bromodomains have been identified as targets for novel therapy in cancers and other diseases. This Special Issue will focus on recent advancements in understanding bromodomain function, ranging from structure to function, and identifying opportunities for drug development for this intriguing class of proteins.
Dr. Jun Qi
Dr. Adam David Durbin
Guest Editors
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Keywords
- epigenetic targets
- inhibitor
- degrader
- transcription factor
- drug development
