Target intelligence / Profile preview

Transcription factor E2F3 (E2F3) mRNA (E2F3)

Target
E2F3
Molecular classification
Transcription factor, mRNA
01

Overview

Transcription factor E2F3 mRNA encodes a protein that is a key regulator of the mammalian cell cycle. It specifically controls the G1/S phase transition by activating genes required for DNA replication (UniProt O00716). The gene produces two isoforms, E2F3a and E2F3b, with E2F3a being a major driver of cell proliferation (NCBI Gene 1871). Overexpression or amplification of E2F3 is a common feature in several human cancers, including bladder, prostate, and lung carcinomas (PMID: 22431511). This overexpression correlates with high tumor grade and poor clinical prognosis, making it a significant biomarker and therapeutic target. Therapeutic approaches targeting E2F3 mRNA include the use of small interfering RNAs (siRNAs) and antisense oligonucleotides to silence its expression. By reducing E2F3 levels, these strategies aim to arrest the cell cycle and induce apoptosis in malignant cells. Although no E2F3-targeted therapies are currently approved for clinical use, preclinical studies demonstrate significant anti-tumor activity. A major challenge in targeting E2F3 is its essential role in the proliferation of normal cells, which may lead to systemic toxicity. Future developments focus on improving the delivery and specificity of RNA-based inhibitors to minimize these off-target effects.

Other names
E2F transcription factor 3KIAA0075E2F-3E2F3aE2F3b
02

Mechanism of action

RNA interference-mediated degradation of mRNA or antisense-mediated translational inhibition

03

Biological functions

Cell cycle regulationG1/S transitionDNA replicationCell proliferationApoptosis regulation
04

Disease associations

Bladder cancerProstate cancerLung cancerBreast cancerHepatocellular carcinomaRetinoblastoma
05

Safety considerations

Potential systemic toxicity due to essential role in normal cell proliferationOff-target effects of RNA-based therapiesPotential for compensatory upregulation of other E2F family members
06

Interacting drugs

siRNA (experimental)

1 more in the full profile.

07

Biomarkers

E2F3 mRNA expression levelE2F3 protein expressionRB1 mutation status

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