Target intelligence / Profile preview

Androgen Receptor Splice Variant 7 (AR-v7)

Target
AR-v7
Molecular classification
Transcription factor, Receptor
01

Overview

Androgen receptor splice variant 7 (AR-v7) is a splice variant of the androgen receptor (AR) that lacks the C-terminal ligand-binding domain (LBD). AR-v7 is constitutively active and drives gene transcription independently of ligand binding. It is frequently detected in castration-resistant prostate cancer (CRPC) and associated with resistance to therapies targeting the androgen receptor pathway, particularly those inhibiting the LBD such as enzalutamide and abiraterone. Detection of AR-V7 is important for guiding therapy selection in metastatic CRPC.

02

Mechanism of action

AR-v7 is constitutively active and drives transcription independently of ligand binding, bypassing the mechanism of action of drugs targeting the ligand-binding domain of the full-length androgen receptor.

03

Biological functions

Transcriptional regulationCell proliferationCell survivalGene expression regulation
04

Disease associations

CancerCastration-resistant prostate cancer (CRPC)Drug resistance
05

Safety considerations

Resistance to androgen receptor-targeted therapies (enzalutamide, abiraterone)Poor prognosis in CRPC patientsTherapeutic challenges in targeting the constitutively active variant.
06

Interacting drugs

Enzalutamide

1 more in the full profile.

07

Biomarkers

AR-V7 mRNA or protein levels (detection methods include immunohistochemistry and molecular assays)

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