Desensitisation of the oxytocin receptor and other G-protein coupled receptors in the human myometrium.
G-protein coupled receptors (GPCRs) are key to maintaining uterine quiescence and inducing phasic contractions at term. However, the biochemical mechanisms whereby uterine GPCRs are desensitised and re-sensitised during these physiological conditions are unknown. For example, the number of oxytocin receptors (OTRs) on uterine myocytes decrease significantly after the addition of oxytocin. Therefore, further understanding of the desensitisation/re-sensitisation of the OTR and other uterine GPCRs during pregnancy may provide a target for more efficient tocolytic drugs and more selective ways to modulate uterine activity. Here, we briefly review some of the mechanisms that may be involved during OTR and other GPCR desensitisation. Experimental Physiology (2001) 86.2, 303-312.
Plested
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CP
Nuffield Department of Obstetrics and Gynaecology, University of Oxford, Oxford OX3 9DU, UK. paul.plested@obs-gyn.ox.ac.uk
Bernal
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D000595:Amino Acid Sequence / Q000235:genetics; D005260:Female; D019204:GTP-Binding Proteins / Q000378:metabolism*; D006801:Humans; D008969:Molecular Sequence Data; D009215:Myometrium / Q000378:metabolism*; D010766:Phosphorylation; D011247:Pregnancy; D011943:Receptors, Adrenergic, beta / Q000235:genetics; D011956:Receptors, Cell Surface / Q000378:metabolism*; D018045:Receptors, Oxytocin / Q000235:genetics / Q000378:metabolism*; D017483:Receptors, Vasopressin / Q000235:genetics
D011943:Receptors, Adrenergic, beta; D011956:Receptors, Cell Surface; D018045:Receptors, Oxytocin; D017483:Receptors, Vasopressin; D019204:GTP-Binding Proteins