Biomolecules & Therapeutics

The Korean Society of Applied Pharmacology (한국응용약물학회)
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Recent Progress in Understanding the Conformational Mechanism of Heterotrimeric G Protein Activation

  • Received : 2016.08.02
  • Accepted : 2016.09.01
  • Published : 2017.01.01
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Abstract

Heterotrimeric G proteins are key intracellular coordinators that receive signals from cells through activation of cognate G protein-coupled receptors (GPCRs). The details of their atomic interactions and structural mechanisms have been described by many biochemical and biophysical studies. Specifically, a framework for understanding conformational changes in the receptor upon ligand binding and associated G protein activation was provided by description of the crystal structure of the ${\beta}2$-adrenoceptor-Gs complex in 2011. This review focused on recent findings in the conformational dynamics of G proteins and GPCRs during activation processes.

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References

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