Target intelligence / Profile preview

Proto-oncogene c-Fos (c-Fos) (c-Fos)

Target
c-Fos
Molecular classification
Transcription factor, Proto-oncogene, Immediate early gene
01

Overview

Proto-oncogene c-Fos is a nuclear protein that functions as a critical component of the dimeric Activator Protein-1 (AP-1) transcription factor complex (Wikipedia, UniProt). It is classified as an "immediate early gene" because its expression is rapidly and transiently induced within minutes of exposure to extracellular stimuli such as growth factors, cytokines, and neurotransmitters (PubMed, Wikipedia). By heterodimerizing with Jun family proteins via a basic leucine zipper domain, c-Fos binds to specific DNA sequences to regulate genes involved in cell proliferation, differentiation, and survival (UniProt, NCBI). Dysregulation of c-Fos is a hallmark of various pathological conditions; its overexpression is strongly associated with the progression of numerous cancers, including breast, lung, and bone tumors (PubMed, NCBI). In the central nervous system, c-Fos expression serves as a widely used biomarker for neuronal activation and is implicated in the pathophysiology of epilepsy and chronic pain (PubMed). While traditionally difficult to target directly, research efforts focus on small-molecule inhibitors such as T-5224, which aim to disrupt the c-Fos/AP-1 DNA-binding interface to treat inflammatory and malignant diseases (PubMed).

Other names
FOSCellular oncogene fosG0/G1 switch regulatory protein 7AP-1 transcription factor subunit c-FosG0S7Proto-oncogene c-Fos
02

Mechanism of action

Inhibition of the AP-1 transcription factor complex by preventing c-Fos from binding to DNA or dimerizing with Jun family proteins, as well as the modulation of upstream signaling pathways like the MAPK/ERK cascade that regulate its expression.

03

Biological functions

Gene expression regulationSignal transductionCell proliferationCell differentiationApoptosisNeuronal plasticityPhospholipid synthesis
04

Disease associations

CancerInflammationEpilepsyNeurodegenerative diseaseCardiovascular diseaseOsteosarcoma
05

Safety considerations

Potential for broad off-target effects due to its essential role in multiple tissuesInterference with normal cellular homeostasisDifficulty in achieving therapeutic selectivity with transcription factor targetsRapid transient expression dynamics complicating the timing of therapeutic intervention
06

Interacting drugs

T-5224

2 more in the full profile.

07

Biomarkers

Neuronal activation markerTumor aggressiveness markerc-Fos protein expression levelc-Fos mRNA level

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