Heteromer Induction: An Approach to Unique Pharmacology? | Zendy

Philip S. Portoghese | Zendy; Eyüp Akgün | Zendy; Mary M. Lunzer | Zendy

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Heteromer Induction: An Approach to Unique Pharmacology?

Author(s) -

Philip S. Portoghese,

Eyüp Akgün,

Mary M. Lunzer

Publication year - 2017

Publication title -

acs chemical neuroscience

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.158

H-Index - 69

ISSN - 1948-7193

DOI - 10.1021/acschemneuro.7b00002

Subject(s) - pharmacophore , chemistry , pharmacology , antagonist , opioid , stereochemistry , receptor , biochemistry , biology

It is proposed that two types of opioid receptor heteromers exist: a) those that are constitutive and b) those that are induced by bivalent ligands. Mu opioid agonists interact with constitutive MOR-DOR heteromer to mediate tolerance and dependence. Bivalent ligand, MDAN21, is devoid of these adverse effects by virtue of its DOR antagonist pharmacophore. We propose that bivalent ligands MMG22 and MCC22 induce colocalized receptors to form heteromers (MOR-mGluR5 and MOR-CCR5, respectively) that do not occur naturally, thereby promoting unique pharmacology. Heteromer induction with bivalent ligands offers a general approach to unique pharmacology that complements traditional SAR.

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