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Constitutive Activity and Inverse Agonists of G Protein-Coupled Receptors: a Current Perspective

Graeme Milligan
Molecular Pharmacology December 2003, 64 (6) 1271-1276; DOI: https://doi.org/10.1124/mol.64.6.1271
Graeme Milligan
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Abstract

Over the last decade, the ability to detect agonist-independent signal transduction by G protein-coupled receptors has in turn resulted in the detection and study of ligands able to block this activity. Such ligands are generically described as inverse agonists. Considerable attention has recently been devoted to the presence and roles of endogenous antagonist/inverse agonists and the concept that inverse agonists may have specific therapeutic benefits compared with neutral antagonists.

  • Received June 20, 2003.
  • Accepted August 29, 2003.
  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 64 (6)
Molecular Pharmacology
Vol. 64, Issue 6
1 Dec 2003
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Constitutive Activity and Inverse Agonists of G Protein-Coupled Receptors: a Current Perspective

Graeme Milligan
Molecular Pharmacology December 1, 2003, 64 (6) 1271-1276; DOI: https://doi.org/10.1124/mol.64.6.1271

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Constitutive Activity and Inverse Agonists of G Protein-Coupled Receptors: a Current Perspective

Graeme Milligan
Molecular Pharmacology December 1, 2003, 64 (6) 1271-1276; DOI: https://doi.org/10.1124/mol.64.6.1271
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    • GPCRs Display Varying Levels of Constitutive Activity
    • Virally Encoded GPCRs
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