Nov 30, 2018

Heteromerization Modulates mu Opioid Receptor Functional Properties in vivo

Frontiers in Pharmacology
Muzeyyen UgurDominique Massotte


Mu opioid receptors modulate a large number of physiological functions. They are in particular involved in the control of pain perception and reward properties. They are also the primary molecular target of opioid drugs and mediate their beneficial analgesic effects, euphoric properties as well as negative side effects such as tolerance and physical dependence. Importantly, mu opioid receptors can physically associate with another receptor to form a novel entity called heteromer that exhibits specific ligand binding, signaling, and trafficking properties. As reviewed here, in vivo physical proximity has now been evidenced for several receptor pairs, subsequent impact of heteromerization on native mu opioid receptor signaling and trafficking identified and a link to behavioral changes established. Selective targeting of heteromers as a tool to modulate mu opioid receptor activity is therefore attracting growing interest and raises hopes for innovative therapeutic strategies.

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Mentioned in this Paper

In Vivo
Ligand Binding
Analgesic brand of acetaminophen-phenyltoloxamine
Receptors, Opioid, mu
Molecular Target
Binding (Molecular Function)
OPRM1 gene

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