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BD2-specific BET inhibitor
- Development stage
- Preclinical
- Lead developer
- AbbVie
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
A BD2-specific BET inhibitor is a class of small molecule epigenetic modulators designed to selectively target the second bromodomain (BD2) of the Bromodomain and Extra-Terminal (BET) family proteins, which include BRD2, BRD3, BRD4, and BRDT. This selectivity is intended to provide therapeutic benefits while minimizing the toxicities associated with pan-BET inhibition, such as thrombocytopenia. In glioblastoma (GBM), these inhibitors have been shown to displace BRD2 from the promoters of mesenchymal (MES) genes, thereby inhibiting the transition of GBM cells to a more aggressive and therapy-resistant mesenchymal state. Research indicates that brain-penetrant BD2 inhibitors can effectively reduce tumor cell invasion and modulate the tumor microenvironment by decreasing the abundance of tumor-associated microglia and macrophages (TAMs), potentially enhancing the sensitivity of GBM to ionizing radiation.
- Other names
- BD2-specific BET inhibitorBD-2-specific BET inhibitorBD 2-specific BET inhibitorBD2-selective BET inhibitorBD-2-selective BET inhibitorBD 2-selective BET inhibitorBD2 inhibitorBD-2 inhibitorBD 2 inhibitorbromodomain-specific BET inhibitor
02
Targets
BRD3 BD2 (Bromodomain-containing protein 3 (BRD3) bromodomain 2 (BD2))BRD2 BD2 (Bromodomain-containing protein 2, bromodomain 2)BRDT BD2 (Bromodomain testis-specific protein (BRDT), bromodomain 2)Bromodomain-containing protein 4, Bromodomain 2
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