Heteromer Induction

An Approach to Unique Pharmacology?

Research output: Contribution to journalArticle

9 Citations (Scopus)

Abstract

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.

Original languageEnglish (US)
Pages (from-to)426-428
Number of pages3
JournalACS Chemical Neuroscience
Volume8
Issue number3
DOIs
StatePublished - Mar 15 2017

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Pharmacology
Ligands
Opioid Receptors
Opioid Analgesics

Keywords

  • DOR
  • MOR
  • heterodimer
  • opiod receptor

Cite this

Heteromer Induction : An Approach to Unique Pharmacology? / Portoghese, Philip S; Akgun, Eyup; Lunzer, Mary M.

In: ACS Chemical Neuroscience, Vol. 8, No. 3, 15.03.2017, p. 426-428.

Research output: Contribution to journalArticle

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