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.
- ↑ He L, Zhang Q, You Y, Sun P, Xu Z, Li R, Wang F, Zhang S, He J, Shen J, Zhao L, Hong Y, Li Y, Liu M, Sun JP, Wang N, Sun Y, Yang H, Luo J. Exogenous activation of the adhesion GPCR ADGRD1/GPR133 protects against bone loss by negatively regulating osteoclastogenesis. Sci Adv. 2025 Jul 11;11(28):eads3829. doi:10.1126/sciadv.ads3829 PMID 40644539
- ↑ Lehmann J, Lin H, Zhang Z, Wiermann M, Ricken AM, Brinkmann F, Brendler J, Ullmann C, Bayer L, Berndt S, Penk A, Winkler N, Hirsch FW, Fuhs T, Käs J, Xiao P, Schöneberg T, Rauner M, Sun JP, Liebscher I. The mechanosensitive adhesion G protein-coupled receptor 133 (GPR133/ADGRD1) enhances bone formation. Signal Transduct Target Ther. 2025 Jun 30;10(1):199. 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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