Design and development of stapled transmembrane peptides that disrupt the activity of G-protein-coupled receptor oligomers.

ABSTRACT: Membrane proteins can associate into larger complexes. Examples include receptor tyrosine complexes, ion channels, transporters, and G protein-coupled receptors (GPCRs). For the latter, there is abundant evidence indicating that GPCRs assemble into complexes, through both homo- and heterodimerization. However, the tools for studying and disrupting these complexes, GPCR or otherwise, are limited. Here, we have developed stabilized interference peptides for this purpose. We have previously reported that tetrahydrocannabinol-mediated cognitive impairment arises from homo- or heterooligomerization between the GPCRs cannabinoid receptor type 1 (CB₁R) and 5-hydroxytryptamine 2A (5-HT_2AR) receptors. Here, to disrupt this interaction through targeting CB₁-5-HT

SUBMITTER: Botta J 

PROVIDER: S-EPMC6851324 | biostudies-literature | 2019 Nov

REPOSITORIES: biostudies-literature