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GSK778
- Development stage
- Preclinical
- Lead developer
- GSK
- Modality
- Small Molecules
- Administration
- Oral, Intraperitoneal
01
Overview
GSK778 (also known as iBET-BD1) is a potent and selective small molecule inhibitor of the first bromodomain (BD1) of the Bromodomain and Extra-Terminal (BET) family of epigenetic reader proteins. Developed by GSK, it is designed to distinguish the biological functions of the two tandem bromodomains (BD1 and BD2) found in BET proteins such as BRD2, BRD3, and BRD4. In the context of triple-mutant (IDH1R132H/p53mut/ATRXloss) astrocytomas, GSK778 has demonstrated the ability to impair tumor cell growth and neurosphere self-renewal, while also suppressing the induction of PD-L1 and disrupting YAP1/TAZ transcriptional signaling. This selectivity for BD1 over BD2 allows for targeted modulation of specific transcriptional networks, potentially offering a more refined therapeutic approach compared to pan-BET inhibitors.
- Other names
- iBET-BD1iBET-BD-1iBET-BD 1
02
Targets
BRDT BD2 (Bromodomain testis-specific protein (BRDT), bromodomain 2)BRD2 BD2 (Bromodomain-containing protein 2, bromodomain 2)BRDT (Bromodomain testis-specific protein)NAT (Arylamine N-acetyltransferase 2)BRD3 BD1 (Bromodomain-containing protein 3, bromodomain 1)BRD3 BD2 (Bromodomain-containing protein 3 (BRD3) bromodomain 2 (BD2))BRD4 (Bromodomain-containing protein 4)Bromodomain-containing protein 4, Bromodomain 2
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