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Allostery

Volume 796 of the series Methods in Molecular Biology pp 133-174

Date:

Allosteric Mechanisms of G Protein-Coupled Receptor Signaling: A Structural Perspective

  • Tarjani M. ThakerAffiliated withDepartment of Biochemistry, Vanderbilt University Medical Center
  • , Ali I. KayaAffiliated withDepartment of Pharmacology, Vanderbilt University Medical Center
  • , Anita M. PreiningerAffiliated withDepartment of Pharmacology, Vanderbilt University Medical Center
  • , Heidi E. HammAffiliated withDepartment of Pharmacology, Vanderbilt University Medical Center
  • , T. M. IversonAffiliated withDepartments of Biochemistry and Pharmacology, Vanderbilt University Medical Center Email author 

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Abstract

G protein-Coupled Receptors (GPCRs) use a complex series of intramolecular conformational changes to couple agonist binding to the binding and activation of cognate heterotrimeric G protein (Gαβγ). The mechanisms underlying this long-range activation have been identified using a variety of biochemical and structural approaches and have primarily used visual signal transduction via the GPCR rhodopsin and cognate heterotrimeric G protein transducin (Gt) as a model system. In this chapter, we review the methods that have revealed allosteric signaling through rhodopsin and transducin. These methods can be applied to a variety of GPCR-mediated signaling pathways.

Key words

G protein-coupled receptor Heterotrimeric G proteins Rhodopsin Transducin Receptor-mediated nucleotide exchange