Membrane androgen receptor
Membrane androgen receptors (mARs) are a group of G protein-coupled receptors (GPCRs) which bind and are activated by testosterone and/or other androgens. Unlike the androgen receptor (AR), a nuclear receptor which mediates its effects via genomic mechanisms, mARs are cell surface receptors which rapidly alter cell signaling via modulation of intracellular signaling cascades. Known or proposed mARs include ZIP9 and GPRC6A.
GPRC6A has been found to be involved in testicular function and prostate cancer. mARs have also been found to be expressed in breast cancer cells. Activation of mARs by testosterone has been found to increase skeletal muscle strength, indicating potential anabolic effects. mARs have also been implicated in the antigonadotropic effects of androgens. 3α-Androstanediol, an active metabolite of dihydrotestosterone (DHT) and a weak androgen as well as a neurosteroid via acting as a positive allosteric modulator of the GABAA receptor, rapidly influences sexual receptivity and behavior in animals, an effect that is GABAA receptor-dependent.
- Bennett NC, Gardiner RA, Hooper JD, Johnson DW, Gobe GC (2010). "Molecular cell biology of androgen receptor signalling". Int. J. Biochem. Cell Biol. 42 (6): 813–27. doi:10.1016/j.biocel.2009.11.013. PMID 19931639.
- Wang C, Liu Y, Cao JM (2014). "G protein-coupled receptors: extranuclear mediators for the non-genomic actions of steroids". Int J Mol Sci. 15 (9): 15412–25. doi:10.3390/ijms150915412. PMC 4200746. PMID 25257522.
- Lang F, Alevizopoulos K, Stournaras C (2013). "Targeting membrane androgen receptors in tumors". Expert Opin. Ther. Targets. 17 (8): 951–63. doi:10.1517/14728222.2013.806491. PMID 23746222.
- Pi M, Quarles LD (June 2011). "GPRC6A regulates prostate cancer progression". Prostate. 72 (4): 399–409. doi:10.1002/pros.21442. PMC 3183291. PMID 21681779.
- Papadopoulou N, Papakonstanti EA, Kallergi G, Alevizopoulos K, Stournaras C (2009). "Membrane androgen receptor activation in prostate and breast tumor cells: molecular signaling and clinical impact". IUBMB Life. 61 (1): 56–61. doi:10.1002/iub.150. PMID 19109827.
- Dent JR, Fletcher DK, McGuigan MR (2012). "Evidence for a Non-Genomic Action of Testosterone in Skeletal Muscle Which may Improve Athletic Performance: Implications for the Female Athlete". J Sports Sci Med. 11 (3): 363–70. PMC 3737931. PMID 24149341.
- Foradori CD, Weiser MJ, Handa RJ (2008). "Non-genomic actions of androgens". Front Neuroendocrinol. 29 (2): 169–81. doi:10.1016/j.yfrne.2007.10.005. PMC 2386261. PMID 18093638.
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