Mapping the Interface of a GPCR Dimer: A Structural Model of the A_2A Adenosine and D₂ Dopamine Receptor Heteromer.

ABSTRACT: The A_2A adenosine (A_2AR) and D₂ dopamine (D₂R) receptors form oligomers in the cell membrane and allosteric interactions across the A_2AR-D₂R heteromer represent a target for development of drugs against central nervous system disorders. However, understanding of the molecular determinants of A_2AR-D₂R heteromerization and the allosteric antagonistic interactions between the receptor protomers is still limited. In this work, a structural model of the A_2AR-D₂R heterodimer was generated using a combined experimental and computational approach. Regions involved in the heteromer interface were modeled based on the effects of peptides derived from the transmembrane (TM) helices on A₂

SUBMITTER: Borroto-Escuela DO 

PROVIDER: S-EPMC6125358 | biostudies-literature | 2018

REPOSITORIES: biostudies-literature