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Target intelligence / Profile preview
Androgen Receptor Variant 7 (AR-V7)
- Target
- AR-V7
- Molecular classification
- Receptor, Transcription factor, Steroid hormone receptor
01
Overview
AR-V7 (Androgen Receptor Variant 7) is a splice variant of the androgen receptor (AR) that lacks the C-terminal ligand-binding domain (LBD), but retains the N-terminal transactivation domain and DNA-binding domain, along with a unique C-terminal sequence. This structural alteration renders AR-V7 constitutively active, functioning as a transcription factor in the absence of androgens. Its expression is associated with castration-resistant prostate cancer (CRPC), predicting resistance to anti-androgen therapies and poorer prognosis. AR-V7 drives expression of genes related to cell cycle progression and represses some tumor suppressor genes.
02
Mechanism of action
Inhibition of AR-V7 transcriptional activity
03
Biological functions
Transcription regulationCell cycleCell proliferationOncogenesis
04
Disease associations
CancerCastration-resistant prostate cancer
05
Safety considerations
Potential for off-target effects due to shared DNA-binding domain with full-length ARResistance mechanisms may emerge
06
Interacting drugs
Niclosamide
07
Biomarkers
AR-V7 expression (predictive of resistance to anti-androgen therapies)
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