Skip to main content
Advertisement

Main menu

  • Home
  • Articles
    • Current Issue
    • Fast Forward
    • Latest Articles
    • Archive
  • Information
    • Instructions to Authors
    • Submit a Manuscript
    • FAQs
    • For Subscribers
    • Terms & Conditions of Use
    • Permissions
  • Editorial Board
  • Alerts
    • Alerts
    • RSS Feeds
  • Virtual Issues
  • Feedback
  • Other Publications
    • Drug Metabolism and Disposition
    • Journal of Pharmacology and Experimental Therapeutics
    • Molecular Pharmacology
    • Pharmacological Reviews
    • Pharmacology Research & Perspectives
    • ASPET

User menu

  • My alerts
  • Log in
  • My Cart

Search

  • Advanced search
Molecular Pharmacology
  • Other Publications
    • Drug Metabolism and Disposition
    • Journal of Pharmacology and Experimental Therapeutics
    • Molecular Pharmacology
    • Pharmacological Reviews
    • Pharmacology Research & Perspectives
    • ASPET
  • My alerts
  • Log in
  • My Cart
Molecular Pharmacology

Advanced Search

  • Home
  • Articles
    • Current Issue
    • Fast Forward
    • Latest Articles
    • Archive
  • Information
    • Instructions to Authors
    • Submit a Manuscript
    • FAQs
    • For Subscribers
    • Terms & Conditions of Use
    • Permissions
  • Editorial Board
  • Alerts
    • Alerts
    • RSS Feeds
  • Virtual Issues
  • Feedback
  • Visit molpharm on Facebook
  • Follow molpharm on Twitter
  • Follow molpharm on LinkedIn
Research ArticleArticle

Segregation of Family A G Protein–Coupled Receptor Protomers in the Plasma Membrane

Anthony Gavalas, Tien-Hung Lan, Qiuju Liu, Ivan R. Corrêa Jr., Jonathan A. Javitch and Nevin A. Lambert
Molecular Pharmacology September 2013, 84 (3) 346-352; DOI: https://doi.org/10.1124/mol.113.086868
Anthony Gavalas
Department of Pharmacology and Toxicology, Medical College of Georgia, Georgia Regents University, Augusta, Georgia (A.G., T.-H.L., Q.L., N.A.L.); New England Biolabs, Inc., Ipswich, Massachusetts (I.R.C.); Departments of Psychiatry and Pharmacology, College of Physicians and Surgeons, Columbia University, New York, New York (J.A.J.); and Division of Molecular Therapeutics, New York State Psychiatric Institute, New York, New York (J.A.J.)
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Tien-Hung Lan
Department of Pharmacology and Toxicology, Medical College of Georgia, Georgia Regents University, Augusta, Georgia (A.G., T.-H.L., Q.L., N.A.L.); New England Biolabs, Inc., Ipswich, Massachusetts (I.R.C.); Departments of Psychiatry and Pharmacology, College of Physicians and Surgeons, Columbia University, New York, New York (J.A.J.); and Division of Molecular Therapeutics, New York State Psychiatric Institute, New York, New York (J.A.J.)
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Qiuju Liu
Department of Pharmacology and Toxicology, Medical College of Georgia, Georgia Regents University, Augusta, Georgia (A.G., T.-H.L., Q.L., N.A.L.); New England Biolabs, Inc., Ipswich, Massachusetts (I.R.C.); Departments of Psychiatry and Pharmacology, College of Physicians and Surgeons, Columbia University, New York, New York (J.A.J.); and Division of Molecular Therapeutics, New York State Psychiatric Institute, New York, New York (J.A.J.)
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Ivan R. Corrêa Jr.
Department of Pharmacology and Toxicology, Medical College of Georgia, Georgia Regents University, Augusta, Georgia (A.G., T.-H.L., Q.L., N.A.L.); New England Biolabs, Inc., Ipswich, Massachusetts (I.R.C.); Departments of Psychiatry and Pharmacology, College of Physicians and Surgeons, Columbia University, New York, New York (J.A.J.); and Division of Molecular Therapeutics, New York State Psychiatric Institute, New York, New York (J.A.J.)
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Jonathan A. Javitch
Department of Pharmacology and Toxicology, Medical College of Georgia, Georgia Regents University, Augusta, Georgia (A.G., T.-H.L., Q.L., N.A.L.); New England Biolabs, Inc., Ipswich, Massachusetts (I.R.C.); Departments of Psychiatry and Pharmacology, College of Physicians and Surgeons, Columbia University, New York, New York (J.A.J.); and Division of Molecular Therapeutics, New York State Psychiatric Institute, New York, New York (J.A.J.)
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Nevin A. Lambert
Department of Pharmacology and Toxicology, Medical College of Georgia, Georgia Regents University, Augusta, Georgia (A.G., T.-H.L., Q.L., N.A.L.); New England Biolabs, Inc., Ipswich, Massachusetts (I.R.C.); Departments of Psychiatry and Pharmacology, College of Physicians and Surgeons, Columbia University, New York, New York (J.A.J.); and Division of Molecular Therapeutics, New York State Psychiatric Institute, New York, New York (J.A.J.)
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
  • Article
  • Figures & Data
  • Info & Metrics
  • eLetters
  • PDF + SI
  • PDF
Loading

Abstract

G protein–coupled receptors (GPCRs) transduce many important physiological signals and are targets for a large fraction of therapeutic drugs. Members of the largest family of GPCRs (family A) are thought to self-associate as dimers and higher-order oligomers, although the significance of such quaternary structures for signaling or receptor trafficking is known for only a few examples. One outstanding question is the physical stability of family A oligomers in cell membranes. Stable oligomers would be expected to move through cellular compartments and membrane domains as intact groups of protomers. Here, we test this prediction by recruiting subsets of affinity-tagged family A protomers into artificial microdomains on the surface of living cells and asking if untagged protomers move into these domains (are corecruited) at the same time. We find that tagged β2 adrenergic and μ-opioid protomers are unable to corecruit untagged protomers into microdomains. In contrast, tagged metabotropic glutamate receptor protomers do corecruit untagged protomers into such microdomains, which is consistent with the known covalent mechanism whereby these family C receptors dimerize. These observations suggest that interactions between these family A protomers are too weak to directly influence subcellular location, and that mechanisms that move these receptors between subcellular compartments and domains must operate on individual protomers.

Footnotes

    • Received April 16, 2013.
    • Accepted June 13, 2013.
  • This work was supported by the National Institutes of Health National Institute of General Medical Sciences [Grants GM078319 and GM096762]; the National Institutes of Health National Institute on Drug Abuse [Grant DA022413]; and the National Institutes of Health National Institute of Mental Health [Grant MH54137].

  • dx.doi.org/10.1124/mol.113.086868.

  • ↵Embedded ImageThis article has supplemental material available at molpharm.aspetjournals.org.

  • Copyright © 2013 by The American Society for Pharmacology and Experimental Therapeutics
View Full Text

MolPharm articles become freely available 12 months after publication, and remain freely available for 5 years. 

Non-open access articles that fall outside this five year window are available only to institutional subscribers and current ASPET members, or through the article purchase feature at the bottom of the page. 

 

  • Click here for information on institutional subscriptions.
  • Click here for information on individual ASPET membership.

 

Log in using your username and password

Forgot your user name or password?

Purchase access

You may purchase access to this article. This will require you to create an account if you don't already have one.
PreviousNext
Back to top

In this issue

Molecular Pharmacology: 84 (3)
Molecular Pharmacology
Vol. 84, Issue 3
1 Sep 2013
  • Table of Contents
  • Table of Contents (PDF)
  • About the Cover
  • Index by author
  • Editorial Board (PDF)
  • Front Matter (PDF)
Download PDF
Article Alerts
Sign In to Email Alerts with your Email Address
Email Article

Thank you for sharing this Molecular Pharmacology article.

NOTE: We request your email address only to inform the recipient that it was you who recommended this article, and that it is not junk mail. We do not retain these email addresses.

Enter multiple addresses on separate lines or separate them with commas.
Segregation of Family A G Protein–Coupled Receptor Protomers in the Plasma Membrane
(Your Name) has forwarded a page to you from Molecular Pharmacology
(Your Name) thought you would be interested in this article in Molecular Pharmacology.
CAPTCHA
This question is for testing whether or not you are a human visitor and to prevent automated spam submissions.
Citation Tools
Research ArticleArticle

Segregation of Family A GPCR Protomers

Anthony Gavalas, Tien-Hung Lan, Qiuju Liu, Ivan R. Corrêa, Jonathan A. Javitch and Nevin A. Lambert
Molecular Pharmacology September 1, 2013, 84 (3) 346-352; DOI: https://doi.org/10.1124/mol.113.086868

Citation Manager Formats

  • BibTeX
  • Bookends
  • EasyBib
  • EndNote (tagged)
  • EndNote 8 (xml)
  • Medlars
  • Mendeley
  • Papers
  • RefWorks Tagged
  • Ref Manager
  • RIS
  • Zotero
Share
Research ArticleArticle

Segregation of Family A GPCR Protomers

Anthony Gavalas, Tien-Hung Lan, Qiuju Liu, Ivan R. Corrêa, Jonathan A. Javitch and Nevin A. Lambert
Molecular Pharmacology September 1, 2013, 84 (3) 346-352; DOI: https://doi.org/10.1124/mol.113.086868
del.icio.us logo Digg logo Reddit logo Twitter logo CiteULike logo Facebook logo Google logo Mendeley logo
  • Tweet Widget
  • Facebook Like
  • Google Plus One

Jump to section

  • Article
    • Abstract
    • Introduction
    • Materials and Methods
    • Results
    • Discussion
    • Acknowledgments
    • Authorship Contributions
    • Footnotes
    • Abbreviations
    • References
  • Figures & Data
  • Info & Metrics
  • eLetters
  • PDF + SI
  • PDF

Related Articles

Cited By...

More in this TOC Section

  • Identification of Celecoxib targets by label-free TPP
  • Editing TOP2α Intron 19 5′ SS Circumvents Drug Resistance
  • CTS Bias
Show more Articles

Similar Articles

  • Home
  • Alerts
Facebook   Twitter   LinkedIn   RSS

Navigate

  • Current Issue
  • Fast Forward by date
  • Fast Forward by section
  • Latest Articles
  • Archive
  • Search for Articles
  • Feedback
  • ASPET

More Information

  • About Molecular Pharmacology
  • Editorial Board
  • Instructions to Authors
  • Submit a Manuscript
  • Customized Alerts
  • RSS Feeds
  • Subscriptions
  • Permissions
  • Terms & Conditions of Use

ASPET's Other Journals

  • Drug Metabolism and Disposition
  • Journal of Pharmacology and Experimental Therapeutics
  • Pharmacological Reviews
  • Pharmacology Research & Perspectives
ISSN 1521-0111 (Online)

Copyright © 2021 by the American Society for Pharmacology and Experimental Therapeutics