[Covalent drug discovery targeting G protein-coupled receptors]

Autor: Moe Kondo, Kazuhiro Nishiyama, Akiyuki Nishimura, Yuri Kato, Motohiro Nishida
Rok vydání: 2022
Předmět:
Zdroj: Nihon yakurigaku zasshi. Folia pharmacologica Japonica. 157(5)
ISSN: 0015-5691
Popis: G protein-coupled receptors (GPCRs) play pivotal roles in converting physicochemical stimuli due to environmental changes to intracellular responses. After ligand stimulation, many GPCRs are desensitized and then recycled or degraded through phosphorylation and β-arrestin-dependent internalization, an important process to maintain protein quality control of GPCRs. However, it is unknown how GPCRs with low β-arrestin sensitivity are controlled. Here we unmasked a β-arrestin-independent GPCR internalization, named Redox-dependent Alternative Internalization (REDAI), focusing on β-arrestin-resistant purinergic P2Y
Databáze: OpenAIRE