8fyt

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LSD-bound serotonin 1A (5-HT1A) receptor-Gi1 protein complex

Structural highlights

8fyt is a 4 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:Electron Microscopy, Resolution 2.64Å
Ligands:7LD, J40, Y01
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Disease

5HT1A_HUMAN Menstrual cycle-dependent periodic fever. The disease is caused by variants affecting the gene represented in this entry.

Function

5HT1A_HUMAN G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling inhibits adenylate cyclase activity and activates a phosphatidylinositol-calcium second messenger system that regulates the release of Ca(2+) ions from intracellular stores. Plays a role in the regulation of 5-hydroxytryptamine release and in the regulation of dopamine and 5-hydroxytryptamine metabolism. Plays a role in the regulation of dopamine and 5-hydroxytryptamine levels in the brain, and thereby affects neural activity, mood and behavior. Plays a role in the response to anxiogenic stimuli.[1] [2] [3] [4]

References

  1. ↑ Singh P, Paila YD, Chattopadhyay A. Role of glycosphingolipids in the function of human serotonin₁A receptors. J Neurochem. 2012 Dec;123(5):716-24. PMID:22957663 doi:10.1111/jnc.12008
  2. ↑ Fargin A, Raymond JR, Lohse MJ, Kobilka BK, Caron MG, Lefkowitz RJ. The genomic clone G-21 which resembles a beta-adrenergic receptor sequence encodes the 5-HT1A receptor. Nature. 1988 Sep 22;335(6188):358-60. PMID:3138543 doi:10.1038/335358a0
  3. ↑ Harrington MA, Shaw K, Zhong P, Ciaranello RD. Agonist-induced desensitization and loss of high-affinity binding sites of stably expressed human 5-HT1A receptors. J Pharmacol Exp Ther. 1994 Mar;268(3):1098-106 PMID:8138923
  4. ↑ Aune TM, McGrath KM, Sarr T, Bombara MP, Kelley KA. Expression of 5HT1a receptors on activated human T cells. Regulation of cyclic AMP levels and T cell proliferation by 5-hydroxytryptamine. J Immunol. 1993 Aug 1;151(3):1175-83 PMID:8393041

Contents


PDB ID 8fyt

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