Heteromer Induction: An Approach to Unique Pharmacology?

Research output: Contribution to journalArticlepeer-review

17 Scopus citations

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

Bibliographical note

Funding Information:
This research was supported by NIH Grant R01 DA030316.

Publisher Copyright:
© 2017 American Chemical Society.

Keywords

  • DOR
  • MOR
  • heterodimer
  • opiod receptor

Fingerprint

Dive into the research topics of 'Heteromer Induction: An Approach to Unique Pharmacology?'. Together they form a unique fingerprint.

Cite this