Functionally selective activation of the dopamine receptor D₂ is mirrored by the protein expression profiles.

ABSTRACT: The development of functionally selective or biased ligands is a promising approach towards drugs with less side effects. Biased ligands for G protein-coupled receptors can selectively induce G protein activation or β-arrestin recruitment. The consequences of this selective action on cellular functions, however, are not fully understood. Here, we investigated the impact of five biased and balanced dopamine D₂ receptor agonists and antagonists on the global protein expression in HEK293T cells by untargeted nanoscale liquid chromatography-tandem mass spectrometry. The proteome analysis detected 5290 protein groups. Hierarchical clustering and principal component analysis based on the expression levels of 1462 differential proteins led to a separation of antagonists and balanced ag

SUBMITTER: Wenk D 

PROVIDER: S-EPMC7875989 | biostudies-literature | 2021 Feb

REPOSITORIES: biostudies-literature