Target intelligence / Profile preview

E2F transcription factor consensus promoter DNA sequence (E2F consensus sequence)

Target
E2F consensus sequence
Molecular classification
DNA sequence, Transcription factor binding site, Cis-regulatory element
01

Overview

The E2F consensus promoter DNA sequence is a specific nucleotide motif, typically represented as TTTSSCGC (where S is C or G), that serves as the primary recognition site for the E2F family of transcription factors (NIH, 2003). These sequences are predominantly located within the promoter regions of genes essential for the G1 to S phase transition of the cell cycle, DNA synthesis, and apoptosis (Wikipedia, 2024). In healthy cells, the binding of E2F factors to these sites is tightly regulated by the retinoblastoma (Rb) protein family; however, in many pathological states such as cancer and vascular proliferative diseases, this regulation is lost, leading to aberrant gene expression and uncontrolled cell growth (Frontiers, 2020). As a therapeutic target, this DNA sequence is addressed using decoy oligonucleotides like Edifoligide, which are synthetic double-stranded DNA fragments containing the consensus motif (PubMed, 2005). These decoys act by competitively binding to E2F transcription factors, thereby preventing them from interacting with endogenous genomic sites and effectively suppressing the proliferative gene program (PNAS, 2002).

Other names
E2F binding siteE2F response elementE2F motifE2F-binding elementE2F-dODN target
02

Mechanism of action

Transcription factor decoy (competitive inhibition of E2F transcription factor binding to endogenous promoter sequences)

03

Biological functions

Cell cycle regulationDNA synthesisApoptosisDNA repairMitosis
04

Disease associations

CancerIntimal hyperplasiaRestenosisCardiovascular disease
05

Safety considerations

Off-target binding to other transcription factorsDelivery to target tissuesSystemic cell cycle inhibitionStability of oligonucleotides in vivo
06

Interacting drugs

Edifoligide
07

Biomarkers

E2F1 expressionRetinoblastoma protein (Rb) phosphorylation statusKi-67 proliferation index

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