Biology:GPR133
 Generic protein structure example |
Probable G-protein coupled receptor 133 is a protein that in humans is encoded by the GPR133 gene.[1][2]
This gene encodes a member of the adhesion-GPCR family of receptors. Family members are characterized by an extended extracellular region with a variable number of protein domains coupled to a TM7 domain via a domain known as the GPCR-Autoproteolysis INducing (GAIN) domain.[3][4]
GPR133 binds androgens, specifically the androgen 5α-dihydrotestosterone (5α-DHT).[5] GPR133 is an adhesion G protein-coupled receptor that functions as a membrane receptor for androgens. When activated by 5α-DHT, GPR133 increases intracellular cyclic AMP (cAMP) levels in muscle cells, leading to enhanced muscle strength.[5]
Agonists of GPR133 such as GL64 and AP503 have potential applications in the treatment of osteoporosis.[6][7]
References
- ↑ "Entrez Gene: GPR133 G protein-coupled receptor 133". https://www.ncbi.nlm.nih.gov/gene/283383.
- ↑ "Novel human G protein-coupled receptors with long N-terminals containing GPS domains and Ser/Thr-rich regions". FEBS Letters 531 (3): 407–414. November 2002. doi:10.1016/S0014-5793(02)03574-3. PMID 12435584.
- ↑ AdhesionGPCRs: Structure to Function (Advances in Experimental Medicine and Biology). Berlin: Springer. 2011. ISBN 978-1-4419-7912-4.
- ↑ "A novel evolutionarily conserved domain of cell-adhesion GPCRs mediates autoproteolysis". The EMBO Journal 31 (6): 1364–1378. March 2012. doi:10.1038/emboj.2012.26. PMID 22333914.
- ↑ 5.0 5.1 "Identification, structure, and agonist design of an androgen membrane receptor". Cell. January 2025. doi:10.1016/j.cell.2025.01.006. PMID 39884271.
- ↑ "Exogenous activation of the adhesion GPCR ADGRD1/GPR133 protects against bone loss by negatively regulating osteoclastogenesis". Science Advances 11 (28). July 2025. doi:10.1126/sciadv.ads3829. PMID 40644539.
- ↑ "The mechanosensitive adhesion G protein-coupled receptor 133 (GPR133/ADGRD1) enhances bone formation". Signal Transduction and Targeted Therapy 10 (1). 30 June 2025. doi:10.1038/s41392-025-02291-y. PMID 40583059.
Further reading
- "Novel human G-protein-coupled receptors". Biochemical and Biophysical Research Communications 305 (1): 67–71. May 2003. doi:10.1016/S0006-291X(03)00709-5. PMID 12732197.
- "The human and mouse repertoire of the adhesion family of G-protein-coupled receptors". Genomics 84 (1): 23–33. July 2004. doi:10.1016/j.ygeno.2003.12.004. PMID 15203201.
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