Heteromer Induction: An Approach to Unique Pharmacology?

Philip S. Portoghese, Eyup Akgün, Mary M. Lunzer

Research output: Contribution to journalArticlepeer-review

20 Scopus citations


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
Issue number3
StatePublished - Mar 15 2017

Bibliographical note

Publisher Copyright:
© 2017 American Chemical Society.


  • DOR
  • MOR
  • heterodimer
  • opiod receptor


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