5-hydroxytryptamine receptor 4

UniProt Q13639 Organism Homo sapiens Gene HTR4

Also known as: HTR4

Function

G protein-coupled receptor for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone and a mitogen. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of downstream effectors. HTR4 is coupled to G(s) G alpha proteins and mediates activation of adenylate cyclase activity.

Classification

Family (Pfam): PF00001 7tm_1
InterPro: 5HT4_rcpt, GPCR_Rhodpsn, GPCR_Rhodpsn_7TM
Functional cluster: G Protein-Coupled Receptors

Experimental structures · PDB · 4

5EM9 X-ray 1.60A
7XT8 EM 3.10A
7XT9 EM 3.20A
7XTA EM 3.20A

A predicted model is available from AlphaFold.

Gene Ontology · 23

Drugs targeting this protein · 20

PRUCALOPRIDE agonist
CISAPRIDE MONOHYDRATE agonist
METOCLOPRAMIDE HYDROCHLORIDE agonist
TEGASEROD MALEATE partial agonist
DEXFENFLURAMINE HYDROCHLORIDE agonist
CAPESEROD partial agonist
VELUSETRAG agonist
NARONAPRIDE agonist
PRUCALOPRIDE SUCCINATE agonist
ZIMELDINE HYDROCHLORIDE antagonist
FELCISETRAG agonist
AMISULPRIDE antagonist
LEVOSULPIRIDE agonist
RENZAPRIDE agonist
CLEBOPRIDE agonist
PRX-03140 partial agonist
RELENOPRIDE agonist
REVEXEPRIDE agonist
PIBOSEROD antagonist
MOSAPRIDE agonist

Related proteins · sequence + function similarity

Co-cited proteins · studied together in the literature

5-hydroxytryptamine receptor 4 2 shared papers
5-hydroxytryptamine receptor 4 1 shared papers
Macrophage colony-stimulating factor 1 receptor 1 shared papers
G protein-coupled receptor kinase 5 1 shared papers
5-hydroxytryptamine receptor 4 1 shared papers
5-hydroxytryptamine receptor 1E 1 shared papers
5-hydroxytryptamine receptor 2B 1 shared papers
5-hydroxytryptamine receptor 6 2 shared papers
5-hydroxytryptamine receptor 7 1 shared papers
5-hydroxytryptamine receptor 2A 1 shared papers
Beta-arrestin-1 1 shared papers
Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2 1 shared papers

Literature · 14 cited papers

GPCRs steer Gi and Gs selectivity via TM5-TM6 switches as revealed by structures of serotonin receptors. Mol. Cell · 2022
Mutations in the colony stimulating factor 1 receptor (CSF1R) gene cause hereditary diffuse leukoencephalopathy with spheroids. Nat. Genet. · 2012
Beta-arrestin1 phosphorylation by GRK5 regulates G protein-independent 5-HT4 receptor signalling. EMBO J. · 2009
A high-affinity monoclonal antibody with functional activity against the 5-hydroxytryptaminergic (5-HT4) receptor. Biochem. Pharmacol. · 2005
The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. · 2004
The DNA sequence and comparative analysis of human chromosome 5. Nature · 2004
Cloning, pharmacological characterisation and tissue distribution of a novel 5-HT4 receptor splice variant, 5-HT4(i). Naunyn Schmiedebergs Arch. Pharmacol. · 2004
Cloning and characterization of a novel human 5-HT4 receptor variant that lacks the alternatively spliced carboxy terminal exon. RT-PCR distribution in human brain and periphery of multiple 5-HT4 receptor variants. Neuropharmacology · 2002
Exploration of the ligand binding site of the human 5-HT(4) receptor by site-directed mutagenesis and molecular modeling. Br. J. Pharmacol. · 2000
Structure of the human serotonin 5-HT4 receptor gene and cloning of a novel 5-HT4 splice variant. J. Neurochem. · 2000
Novel brain-specific 5-HT4 receptor splice variants show marked constitutive activity: role of the C-terminal intracellular domain. Mol. Pharmacol. · 1999
Cloning, expression, and pharmacology of four human 5-hydroxytryptamine 4 receptor isoforms produced by alternative splicing in the carboxyl terminus. J. Neurochem. · 1998
… and 2 more in the literature graph

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