Emerging Paradigm of Intracellular Targeting of G Protein-Coupled Receptors.

ABSTRACT: G protein-coupled receptors (GPCRs) recognize a diverse array of extracellular stimuli, and they mediate a broad repertoire of signaling events involved in human physiology. Although the major effort on targeting GPCRs has typically been focused on their extracellular surface, a series of recent developments now unfold the possibility of targeting them from the intracellular side as well. Allosteric modulators binding to the cytoplasmic surface of GPCRs have now been described, and their structural mechanisms are elucidated by high-resolution crystal structures. Furthermore, pepducins, aptamers, and intrabodies targeting the intracellular face of GPCRs have also been successfully utilized to modulate receptor signaling. Moreover, small molecule compounds, aptamers, and synthetic intrabodie

SUBMITTER: Chaturvedi M 

PROVIDER: S-EPMC7258685 | biostudies-literature | 2018 Jul

REPOSITORIES: biostudies-literature