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
  • Submit
  • 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
Pharmacological Reviews
  • 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
Pharmacological Reviews

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
  • Submit
  • Visit Pharm Rev on Facebook
  • Follow Pharm Rev on Twitter
  • Follow ASPET on LinkedIn
Review ArticleReview Article

Seven Transmembrane Receptors as Shapeshifting Proteins: The Impact of Allosteric Modulation and Functional Selectivity on New Drug Discovery

Terry Kenakin and Laurence J. Miller
Pharmacological Reviews June 2010, 62 (2) 265-304; DOI: https://doi.org/10.1124/pr.108.000992
Terry Kenakin
Molecular Discovery Research, GlaxoSmithKline Research and Development, Research Triangle Park, North Carolina (T.P.K.); and Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona (L.J.M.)
  • Find this author on Google Scholar
  • Find this author on PubMed
  • Search for this author on this site
Laurence J. Miller
Molecular Discovery Research, GlaxoSmithKline Research and Development, Research Triangle Park, North Carolina (T.P.K.); and Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona (L.J.M.)
  • 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
Loading

Article Information

vol. 62 no. 2 265-304
DOI 
https://doi.org/10.1124/pr.108.000992
PubMed 
20392808

Published By 
American Society for Pharmacology and Experimental Therapeutics
Print ISSN 
0031-6997
Online ISSN 
1521-0081
History 
  • Published online May 14, 2010.

Article Versions

  • Earlier version (April 14, 2010 - 05:14).
  • You are viewing the most recent version of this article.
Copyright & Usage 
Copyright © 2010 by The American Society for Pharmacology and Experimental Therapeutics

Author Information

  1. Terry Kenakin and
  2. Laurence J. Miller
  1. Molecular Discovery Research, GlaxoSmithKline Research and Development, Research Triangle Park, North Carolina (T.P.K.); and Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, Arizona (L.J.M.)
  1. Address correspondence to: Terry P. Kenakin, GlaxoSmithKline, 5 Moore Drive, Mailtstop V-287, Research Triangle Park, NC 27709. E-mail: terry.p.kenakin{at}gsk.com
View Full Text

Funding

  • National Institutes of Health

    DK32878; DK46577

Statistics from Altmetric.com

Article usage

Article usage: January 2018 to February 2023

AbstractFullPdf
Jan 2018295921
Feb 2018167335
Mar 2018216633
Apr 2018208326
May 2018207426
Jun 201846124
Jul 2018730323
Aug 2018123620
Sep 20181013233
Oct 2018114134
Nov 2018176324
Dec 201870148
Jan 201973377
Feb 2019623610
Mar 2019725211
Apr 2019694916
May 20192235614
Jun 201948259
Jul 201961159
Aug 2019732411
Oct 201957217
Nov 201975165
Dec 201944177
Jan 202042416
Feb 2020179443
Mar 2020123477
May 202097516
Jun 20201304611
Jul 202094477
Aug 20203453
Sep 202068166
Oct 202091169
Nov 20206282
Dec 202083185
Jan 2021705211
Feb 20211095516
Mar 202155226
Apr 2021126122
May 202190235
Jun 202170242
Jul 20216985
Aug 202155337
Sep 202174238
Oct 202172109
Nov 20215593
Dec 202156233
Jan 20224988
Feb 202281118
Mar 20225384
Apr 202268156
May 202254127
Jun 202254105
Jul 2022811710
Aug 202261137
Sep 202260415
Oct 2022382324
Nov 2022639616
Dec 202264169
Jan 202392154
Feb 20231653

PreviousNext
Back to top

In this issue

Pharmacological Reviews: 62 (2)
Pharmacological Reviews
Vol. 62, Issue 2
1 Jun 2010
  • Table of Contents
  • Table of Contents (PDF)
  • About the Cover
  • Index by author
  • Back Matter (PDF)
  • 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 Pharmacological Reviews 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.
Seven Transmembrane Receptors as Shapeshifting Proteins: The Impact of Allosteric Modulation and Functional Selectivity on New Drug Discovery
(Your Name) has forwarded a page to you from Pharmacological Reviews
(Your Name) thought you would be interested in this article in Pharmacological Reviews.
CAPTCHA
This question is for testing whether or not you are a human visitor and to prevent automated spam submissions.
Citation Tools
Review ArticleReview Article

Seven Transmembrane Receptors as Shapeshifting Proteins: The Impact of Allosteric Modulation and Functional Selectivity on New Drug Discovery

Terry Kenakin and Laurence J. Miller
Pharmacological Reviews June 1, 2010, 62 (2) 265-304; DOI: https://doi.org/10.1124/pr.108.000992

Citation Manager Formats

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

Share
Review ArticleReview Article

Seven Transmembrane Receptors as Shapeshifting Proteins: The Impact of Allosteric Modulation and Functional Selectivity on New Drug Discovery

Terry Kenakin and Laurence J. Miller
Pharmacological Reviews June 1, 2010, 62 (2) 265-304; DOI: https://doi.org/10.1124/pr.108.000992
del.icio.us logo Digg logo Reddit logo Twitter logo Facebook logo Google logo Mendeley logo
  • Tweet Widget
  • Facebook Like
  • Google Plus One

Jump to section

  • Article
    • Abstract
    • I. Receptors as Allosteric Proteins
    • II. The Structural Organization of Seven Transmembrane Receptors
    • III. Receptor Conformation as Protein Ensembles
    • IV. Allosteric Transitions within Receptor Ensembles
    • V. The Vectorial Nature of Allostery
    • VI. Conclusions
    • Acknowledgments.
    • Footnotes
    • References
  • Figures & Data
  • Info & Metrics
  • eLetters
  • PDF

Related Articles

Cited By...

More in this TOC Section

  • The Quest to Define and Target Cellular Senescence
  • Nanozymes for viral diagnosis and therapy
  • Structure and Inhibition of NLRP3 Inflammasome
Show more Review Articles

Similar Articles

Advertisement
  • Home
  • Alerts
Facebook   Twitter   LinkedIn   RSS

Navigate

  • Current Issue
  • Latest Articles
  • Archive
  • Search for Articles
  • Feedback
  • ASPET

More Information

  • About Pharmacological Reviews
  • 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
  • Molecular Pharmacology
  • Pharmacology Research & Perspectives
ISSN 1521-0081 (Online)

Copyright © 2023 by the American Society for Pharmacology and Experimental Therapeutics