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.[1][2][3] 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.[2][3] Known or proposed mARs include ZIP9 and GPRC6A.[2][4]

GPRC6A has been found to be involved in testicular function and prostate cancer.[2][3] mARs have also been found to be expressed in breast cancer cells.[5] Activation of mARs by testosterone has been found to increase skeletal muscle strength, indicating potential anabolic effects.[6] mARs have also been implicated in the antigonadotropic effects of androgens.[7] 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.[7]

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  1. ^ 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.
  2. ^ a b c d 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.
  3. ^ a b c 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.
  4. ^ 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.
  5. ^ 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.
  6. ^ 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.
  7. ^ a b 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.