5-hydroxytryptamine receptor 1E

Function

G protein-coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various alkaloids and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors, such as adenylate cyclase. HTR1E is coupled to G(i)/G(o) G alpha proteins and mediates inhibitory neurotransmission by inhibiting adenylate cyclase activity.

Classification

Family (Pfam)

PF00001 7tm_1

InterPro

5HT_rcpt, GPCR_Rhodpsn, GPCR_Rhodpsn_7TM

Functional cluster

G Protein-Coupled Receptors

Experimental structures · PDB · 3

• 7E33 EM 2.90A
• 8UGY EM 3.31A
• 8UH3 EM 3.31A

A predicted model is available from AlphaFold.

Gene Ontology · 14

• GO:0030425 dendrite
• GO:0005886 plasma membrane
• GO:0045202 synapse
• GO:0004930 G protein-coupled receptor activity
• GO:0004993 G protein-coupled serotonin receptor activity
• GO:0001586 Gi/o-coupled serotonin receptor activity
• GO:0030594 neurotransmitter receptor activity
• GO:0051378 serotonin binding
• GO:0099589 serotonin receptor activity
• GO:0007193 adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway
• GO:0007198 adenylate cyclase-inhibiting serotonin receptor signaling pathway
• GO:0007268 chemical synaptic transmission
• GO:0007186 G protein-coupled receptor signaling pathway
• GO:0007187 G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger

Drugs targeting this protein · 3

• DEXFENFLURAMINE HYDROCHLORIDE agonist
• ZIMELDINE HYDROCHLORIDE antagonist
• AMISULPRIDE antagonist

Related proteins · sequence + function similarity

• 5-hydroxytryptamine receptor 1E 1.00
• 5-hydroxytryptamine receptor 1E 1.00
• 5-hydroxytryptamine receptor 1F 0.96
• 5-hydroxytryptamine receptor 1F 0.96
• 5-hydroxytryptamine receptor 1F 0.96
• 5-hydroxytryptamine receptor 1F 0.96
• 5-hydroxytryptamine receptor 1F 0.96
• 5-hydroxytryptamine receptor 1D 0.94
• 5-hydroxytryptamine receptor 1D 0.94
• 5-hydroxytryptamine receptor 1D 0.94
• 5-hydroxytryptamine receptor 1D 0.93
• 5-hydroxytryptamine receptor 1A-beta 0.93

Co-cited proteins · studied together in the literature

• 5-hydroxytryptamine receptor 1E 1 shared papers
• 5-hydroxytryptamine receptor 1F 4 shared papers
• 5-hydroxytryptamine receptor 1D 3 shared papers
• 5-hydroxytryptamine receptor 1A 4 shared papers
• 5-hydroxytryptamine receptor 1B 3 shared papers
• 5-hydroxytryptamine receptor 5A 1 shared papers
• 5-hydroxytryptamine receptor 2B 2 shared papers
• 5-hydroxytryptamine receptor 2A 2 shared papers
• Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2 2 shared papers
• Guanine nucleotide-binding protein G(i) subunit alpha-1 2 shared papers
• Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1 2 shared papers
• 5-hydroxytryptamine receptor 2C 1 shared papers

Literature · 13 cited papers

• Structural insights into the ligand binding and Gi coupling of serotonin receptor 5-HT5A. Cell Discov. · 2022
• Structural insights into the lipid and ligand regulation of serotonin receptors. Nature · 2021
• Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: a comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationships. J. Pharmacol. Exp. Ther. · 2011
• Serotonin receptors - from molecular biology to clinical applications. Physiol. Res. · 2011
• Serotonin receptors. Chem. Rev. · 2008
• The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. · 2004
• Human-specific amino acid changes found in 103 protein-coding genes. Mol. Biol. Evol. · 2004
• Molecular cloning and pharmacological characterization of the guinea pig 5-HT1E receptor. Eur. J. Pharmacol. · 2004
• The DNA sequence and analysis of human chromosome 6. Nature · 2003
• Characterization of single-nucleotide polymorphisms in coding regions of human genes. Nat. Genet. · 1999
• Molecular cloning of a human gene (S31) encoding a novel serotonin receptor mediating inhibition of adenylyl cyclase. FEBS Lett. · 1992
• Molecular cloning of a serotonin receptor from human brain (5HT1E): a fifth 5HT1-like subtype. Proc. Natl. Acad. Sci. U.S.A. · 1992
• … and 1 more in the literature graph