Structural characterization of receptor–receptor interactions in the allosteric modulation of G protein-coupled receptor (Gpcr) dimers

Raudah Lazim, Donghyuk Suh, Jai Woo Lee, Thi Ngoc Lan Vu, Sanghee Yoon, Sun Choi

Research output: Contribution to journalReview articlepeer-review

5 Scopus citations


G protein-coupled receptor (GPCR) oligomerization, while contentious, continues to at-tract the attention of researchers. Numerous experimental investigations have validated the presence of GPCR dimers, and the relevance of dimerization in the effectuation of physiological functions intensifies the attractiveness of this concept as a potential therapeutic target. GPCRs, as a single entity, have been the main source of scrutiny for drug design objectives for multiple diseases such as cancer, inflammation, cardiac, and respiratory diseases. The existence of dimers broadens the research scope of GPCR functions, revealing new signaling pathways that can be targeted for disease pathogenesis that have not previously been reported when GPCRs were only viewed in their monomeric form. This review will highlight several aspects of GPCR dimerization, which include a summary of the structural elucidation of the allosteric modulation of class C GPCR activation offered through recent solutions to the three-dimensional, full-length structures of metabotropic glutamate receptor and γ-aminobutyric acid B receptor as well as the role of dimerization in the modification of GPCR function and allostery. With the growing influence of computational methods in the study of GPCRs, we will also be reviewing recent computational tools that have been utilized to map protein–protein interactions (PPI).

Original languageEnglish
Article number3241
Pages (from-to)1-20
Number of pages20
JournalInternational Journal of Molecular Sciences
Issue number6
StatePublished - 2 Mar 2021

Bibliographical note

Publisher Copyright:
© 2021 by the authors. Licensee MDPI, Basel, Switzerland.


  • Allosteric modulation
  • Dimerization
  • G protein-coupled receptor (GPCR)
  • PPI prediction
  • Peptide design
  • Protein dy-namics
  • Protein dynamics
  • Receptor–receptor interaction


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