Allosteric mechanisms of G protein-Coupled Receptor signaling: a structural perspective

Methods Mol Biol. 2012:796:133-74. doi: 10.1007/978-1-61779-334-9_8.

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 (G(t)) 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.

MeSH terms

  • Allosteric Regulation / physiology
  • Heterotrimeric GTP-Binding Proteins / chemistry
  • Heterotrimeric GTP-Binding Proteins / metabolism
  • Humans
  • Protein Structure, Secondary
  • Receptors, G-Protein-Coupled / chemistry*
  • Receptors, G-Protein-Coupled / metabolism*
  • Rhodopsin / chemistry
  • Rhodopsin / metabolism
  • Signal Transduction / physiology
  • Transducin / chemistry
  • Transducin / metabolism

Substances

  • Receptors, G-Protein-Coupled
  • Rhodopsin
  • Heterotrimeric GTP-Binding Proteins
  • Transducin