Androgen receptor Recombinant Rabbit Monoclonal Antibody [ST0453]

Function

Androgens exhibit a wide range of effects on the development, maintenance and regulation of male phenotype and male reproductive physiology. The androgen receptor (AR) is a member of the steroid superfamily of ligand-dependent transcription factors. ARs bind the two biologically active androgens, testosterone (T) and dihydrotestosterone (DHT), with high and nearly identical affinities; however, the rates of association and dissociation of T are about three times more rapid than those of DHT. This difference has resulted in speculation as to whether these differences in binding kinetics could account for the different physiological effects of T and DHT. A striking feature of AR is its rapid degradation in the absence of ligand. It is now well established that androgen binding results in an at least six-fold increase in androgen stability and that ligand-induced stabilization of AR is highly androgen- specific.

Background References

1. Ma Q et al. A Novel Missense Mutation in USP26 Gene Is Associated With Nonobstructive Azoospermia. Reprod Sci 23:1434-41 (2016).

2. Venant H et al. The Sphingosine Kinase 2 Inhibitor ABC294640 Reduces the Growth of Prostate Cancer Cells and Results in Accumulation of Dihydroceramides In Vitro and In Vivo. Mol Cancer Ther 14:2744-52 (2015).

Sequence Similarity

Belongs to the nuclear hormone receptor family. NR3 subfamily.

Tissue Specificity

Isoform 2 is mainly expressed in heart and skeletal muscle. Isoform 3 is expressed by basal and stromal cells of prostate (at protein level).

Post-translational Modification

Sumoylated on Lys-388 (major) and Lys-521. Ubiquitinated. Deubiquitinated by USP26. 'Lys-6' and 'Lys-27'-linked polyubiquitination by RNF6 modulates AR transcriptional activity and specificity.; Phosphorylated in prostate cancer cells in response to several growth factors including EGF. Phosphorylation is induced by c-Src kinase (CSK). Tyr-535 is one of the major phosphorylation sites and an increase in phosphorylation and Src kinase activity is associated with prostate cancer progression. Phosphorylation by TNK2 enhances the DNA-binding and transcriptional activity and may be responsible for androgen-independent progression of prostate cancer. Phosphorylation at Ser-83 by CDK9 regulates AR promoter selectivity and cell growth. Phosphorylation by PAK6 leads to AR-mediated transcription inhibition.; Palmitoylated by ZDHHC7 and ZDHHC21. Palmitoylation is required for plasma membrane targeting and for rapid intracellular signaling via ERK and AKT kinases and cAMP generation.

Subcellular Location

Nucleus, Cytoplasm.

UNIPROT

SwissProt: P10275 Human

Synonyms