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Target intelligence / Profile preview
Androgen Receptor Ligand Binding Domain (AR-LBD)
- Target
- AR-LBD
- Molecular classification
- Nuclear Receptor Domain, Transcription Factor Domain
01
Overview
The androgen receptor ligand binding domain (AR-LBD) is a critical region of the androgen receptor (AR), responsible for binding androgens such as testosterone and dihydrotestosterone (DHT). This binding triggers conformational changes that activate the receptor's function as a transcription factor, regulating gene expression related to male development and reproduction. Abnormalities or mutations within this domain can lead to diseases including prostate cancer, Kennedy’s disease, complete androgen insensitivity syndrome (CAIS), and male infertility.
02
Mechanism of action
Ligand binding induces conformational changes, leading to dimerization, DNA binding, and recruitment of co-regulators to modulate gene transcription.
03
Biological functions
Ligand bindingReceptor dimerizationDNA interactionTranscriptional regulation
04
Disease associations
Prostate cancerKennedy's disease/Spinal bulbar muscular atrophyComplete Androgen Insensitivity Syndrome (CAIS)Male infertility
05
Safety considerations
Mutations can alter ligand specificity or disrupt normal signaling pathways.Dysregulation can lead to various diseases including prostate cancer and androgen insensitivity syndromes.
06
Interacting drugs
Testosterone
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