Oxytocin receptor

UniProt P30559 Organism Homo sapiens Gene OXTR

Also known as: OXTR

Function

G protein-coupled receptor for oxytocin (OXT), a neuropeptide hormone released by the posterior pituitary gland that plays a key role in social behavior and other biological processes, such as milk ejection. 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 phospholipase C. OXTR is mainly coupled to G(q) G proteins and mediates production of diacylglycerol (DAG) and inositol 1,4,5-trisphosphate (IP3) second messengers that modulate the activity of phosphatidylinositol 3-kinase and promote the release of Ca(2+) ions from intracellular stores, respectively. In presence of high levels of oxytocin, also coupled to G(i) G proteins, mediating inhibition of adenylate cyclase activity. Central release of oxytocin plays essential roles in social behavior, such as maternal care, social cognition and affiliative behaviors, triggering signaling that modulates neural circuits by altering ion channel activity, changing intrinsic neuronal properties and modifying synaptic transmission (both excitatory and inhibitory). Peripheral release of oxytocin (secretion into the bloodstream) promotes various processes, such as parturition, lactation or osteoblast differentiation. OXTR-mediated signaling promotes milk ejection by triggering and strengthening contraction of the smooth muscle of mammary gland (By similarity).

Classification

Family (Pfam): PF00001 7tm_1
InterPro: GPCR_Rhodpsn, GPCR_Rhodpsn_7TM, Oxytocn_rcpt, Vasoprsn_rcpt
Functional cluster: Membrane Transporters & GPCRs

Experimental structures · PDB · 3

6TPK X-ray 3.20A
7QVM EM 3.25A
7RYC EM 2.90A

A predicted model is available from AlphaFold.

Gene Ontology · 13

Drugs targeting this protein · 9

NOLASIBAN antagonist
EPELSIBAN antagonist
BARUSIBAN antagonist
CARBETOCIN agonist
ATOSIBAN antagonist
OXYTOCIN agonist
RELCOVAPTAN antagonist
RETOSIBAN antagonist
ATOSIBAN ACETATE antagonist

Related proteins · sequence + function similarity

Co-cited proteins · studied together in the literature

Oxytocin-neurophysin 1 proprotein 3 shared papers
G protein-coupled receptor kinase 6 1 shared papers
G protein-coupled receptor kinase 2 2 shared papers
Oxytocin receptor 1 shared papers
Beta-arrestin-2 2 shared papers
Serine/threonine-protein kinase D1 1 shared papers
Serine/threonine-protein kinase D1 1 shared papers

Literature · 18 cited papers

Structural basis for the activation and ligand recognition of the human oxytocin receptor. Nat. Commun. · 2022
The oxytocin signaling complex reveals a molecular switch for cation dependence. Nat. Struct. Mol. Biol. · 2022
Phosphorylation-dependent positive feedback on the oxytocin receptor through the kinase PKD1 contributes to long-term social memory. Sci. Signal. · 2022
Crystal structure of the human oxytocin receptor. Sci. Adv. · 2020
Common polymorphism in the oxytocin receptor gene (OXTR) is associated with human social recognition skills. Proc. Natl. Acad. Sci. U.S.A. · 2014
Common oxytocin receptor gene (OXTR) polymorphism and social support interact to reduce stress in humans. Proc. Natl. Acad. Sci. U.S.A. · 2011
Functional selective oxytocin-derived agonists discriminate between individual G protein family subtypes. J. Biol. Chem. · 2012
Oxytocin receptor gene (OXTR) is related to psychological resources. Proc. Natl. Acad. Sci. U.S.A. · 2011
A common allele in the oxytocin receptor gene (OXTR) impacts prosocial temperament and human hypothalamic-limbic structure and function. Proc. Natl. Acad. Sci. U.S.A. · 2010
Oxytocin receptor genetic variation relates to empathy and stress reactivity in humans. Proc. Natl. Acad. Sci. U.S.A. · 2009
Regulation of oxytocin receptor responsiveness by G protein-coupled receptor kinase 6 in human myometrial smooth muscle. Mol. Endocrinol. · 2009
Internalization and desensitization of the oxytocin receptor is inhibited by Dynamin and clathrin mutants in human embryonic kidney 293 cells. Mol. Endocrinol. · 2006
… and 6 more in the literature graph

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