Unraveling the Structure and Function of G Protein-Coupled Receptors Through NMR Spectroscopy

Irina G. Tikhonova, Stefano Costanzi

Research output: Contribution to journalLiterature reviewpeer-review

27 Citations (Scopus)
355 Downloads (Pure)


G protein-coupled receptors (GPCRs) are a large superfamily of signaling proteins expressed on the plasma membrane. They are involved in a wide range of physiological processes and, therefore, are exploited as drug targets in a multitude of therapeutic areas. In this extent, knowledge of structural and functional properties of GPCRs may greatly facilitate rational design of modulator compounds. Solution and solid-state nuclear magnetic resonance (NMR) spectroscopy represents a powerful method to gather atomistic insights into protein structure and dynamics. In spite of the difficulties inherent the solution of the structure of membrane proteins through NMR, these methods have been successfully applied, sometimes in combination with molecular modeling, to the determination of the structure of GPCR fragments, the mapping of receptor-ligand interactions, and the study of the conformational changes associated with the activation of the receptors. In this review, we provide a summary of the NMR contributions to the study of the structure and function of GPCRs, also in light of the published crystal structures.

Original languageEnglish
Pages (from-to)4003-4016
Number of pages14
JournalCurrent Pharmaceutical Design
Issue number35
Publication statusPublished - Dec 2009

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology


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