7xt9

Structural highlights

Function

C562_ECOLX Electron-transport protein of unknown function.5HT4R_HUMAN G-protein coupled receptor for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone and a mitogen (PubMed:10821780, PubMed:16102731, PubMed:35714614, PubMed:9603189). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors (PubMed:16102731, PubMed:35714614). HTR4 is coupled to G(s) G alpha proteins and mediates activation of adenylate cyclase activity (PubMed:16102731, PubMed:35714614).^{[1] [2] [3] [4]}

See Also

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

References

1. ↑ Mialet J, Dahmoune Y, Lezoualc'h F, Berque-Bestel I, Eftekhari P, Hoebeke J, Sicsic S, Langlois M, Fischmeister R. Exploration of the ligand binding site of the human 5-HT(4) receptor by site-directed mutagenesis and molecular modeling. Br J Pharmacol. 2000 Jun;130(3):527-38. PMID:10821780 doi:10.1038/sj.bjp.0703356
2. ↑ Kamel R, Eftekhari P, Garcia S, Berthouze M, Berque-Bestel I, Peter JC, Lezoualc'h F, Hoebeke J. A high-affinity monoclonal antibody with functional activity against the 5-hydroxytryptaminergic (5-HT4) receptor. Biochem Pharmacol. 2005 Oct 1;70(7):1009-18. PMID:16102731 doi:10.1016/j.bcp.2005.07.005
3. ↑ 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
4. ↑ Blondel O, Gastineau M, Dahmoune Y, Langlois M, Fischmeister R. Cloning, expression, and pharmacology of four human 5-hydroxytryptamine 4 receptor isoforms produced by alternative splicing in the carboxyl terminus. J Neurochem. 1998 Jun;70(6):2252-61. PMID:9603189 doi:10.1046/j.1471-4159.1998.70062252.x
5. ↑ 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