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E2F transcription factor 1 (E2F1) is a key member of the E2F family of transcription factors. It plays a central role in regulating cell cycle progression, DNA repair, differentiation, and apoptosis. E2F1 functions as a transcription activator by binding to specific DNA sequences in promoter regions of target genes. Its activity is tightly regulated by retinoblastoma protein pRB; when pRB is phosphorylated or absent, free E2F1 activates its target genes promoting S-phase entry. E2F1 has strong pro-apoptotic activity and is uniquely phosphorylated by ATM/CHK upon genotoxic stress. Overexpression or dysregulation contributes to oncogenesis making it a target for anticancer drug development.
Inhibition of E2F1 transcriptional activity
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