Target intelligence / Profile preview

Androgen Receptor Splice Variant (AR-V)

Target
AR-V
Molecular classification
Receptor, Transcription factor, Nuclear receptor
01

Overview

Androgen receptor splice variants (AR-Vs) are alternative forms of the androgen receptor (AR) protein generated through alternative splicing of AR mRNA. These variants often lack the ligand-binding domain (LBD) and can have distinct structural and functional properties compared to canonical AR. Many clinically relevant AR-Vs retain the NTD and DBD but lack all or part of the LBD. Expression of certain splice variants is associated with resistance to androgen deprivation therapy (ADT) and next-generation antiandrogens used in prostate cancer treatment. The presence of constitutively active forms such as AR-V7 enables continued signaling even under low-androgen conditions typical after ADT.

Other names
AR splice variantAR-V7AR45AR23
02

Mechanism of action

Ligand-independent transcriptional activation

03

Biological functions

Transcription regulationGene expressionSignal transductionCell proliferation
04

Disease associations

CancerProstate cancerCastration-resistant prostate cancerDrug resistance
05

Safety considerations

Resistance to antiandrogen therapiesConstitutive activation leading to uncontrolled cell growth
06

Interacting drugs

Enzalutamide

1 more in the full profile.

07

Biomarkers

AR-V7

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