7xtb

Structural highlights

Function

C562_ECOLX Electron-transport protein of unknown function.5HT6R_HUMAN G-protein coupled receptor for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone and a mitogen (PubMed:35714614, PubMed:36989299, PubMed:37327704, PubMed:8522988). Also has a high affinity for tricyclic psychotropic drugs (By similarity). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors (PubMed:35714614). HTR6 is coupled to G(s) G alpha proteins and mediates activation of adenylate cyclase activity (PubMed:35714614, PubMed:37327704). Controls pyramidal neurons migration during corticogenesis, through the regulation of CDK5 activity (By similarity). Is an activator of mTOR signaling (PubMed:23027611).[UniProtKB:P31388][UniProtKB:Q9R1C8]^{[1] [2] [3] [4] [5]}

See Also

• Transducin 3D structures
• 5-hydroxytryptamine receptor 3D structures

References

1. ↑ Meffre J, Chaumont-Dubel S, Mannoury la Cour C, Loiseau F, Watson DJ, Dekeyne A, Séveno M, Rivet JM, Gaven F, Déléris P, Hervé D, Fone KC, Bockaert J, Millan MJ, Marin P. 5-HT(6) receptor recruitment of mTOR as a mechanism for perturbed cognition in schizophrenia. EMBO Mol Med. 2012 Oct;4(10):1043-56. PMID:23027611 doi:10.1002/emmm.201201410
2. ↑ Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE. GPCRs steer Gi and Gs selectivity via TM5-TM6 switches as revealed by structures of serotonin receptors. Mol Cell. 2022 Jul 21;82(14):2681-2695.e6. doi: 10.1016/j.molcel.2022.05.031., Epub 2022 Jun 16. PMID:35714614 doi:http://dx.doi.org/10.1016/j.molcel.2022.05.031
3. ↑ He L, Zhao Q, Qi J, Wang Y, Han W, Chen Z, Cong Y, Wang S. Structural insights into constitutive activity of 5-HT(6) receptor. Proc Natl Acad Sci U S A. 2023 Apr 4;120(14):e2209917120. PMID:36989299 doi:10.1073/pnas.2209917120
4. ↑ Pei Y, Wen X, Guo SC, Yang ZS, Zhang R, Xiao P, Sun JP. Structural insight into the selective agonist ST1936 binding of serotonin receptor 5-HT6. Biochem Biophys Res Commun. 2023 Jun 5;671:327-334. PMID:37327704 doi:10.1016/j.bbrc.2023.05.126
5. ↑ Kohen R, Metcalf MA, Khan N, Druck T, Huebner K, Lachowicz JE, Meltzer HY, Sibley DR, Roth BL, Hamblin MW. Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor. J Neurochem. 1996 Jan;66(1):47-56. PMID:8522988 doi:10.1046/j.1471-4159.1996.66010047.x
6. ↑ Huang S, Xu P, Shen DD, Simon IA, Mao C, Tan Y, Zhang H, Harpsoe K, Li H, Zhang Y, You C, Yu X, Jiang Y, Zhang Y, Gloriam DE, Xu HE. GPCRs steer Gi and Gs selectivity via TM5-TM6 switches as revealed by structures of serotonin receptors. Mol Cell. 2022 Jul 21;82(14):2681-2695.e6. doi: 10.1016/j.molcel.2022.05.031., Epub 2022 Jun 16. PMID:35714614 doi:http://dx.doi.org/10.1016/j.molcel.2022.05.031