Role of the GRK2/3 N-terminus in discriminating the endocytic
We identify the N-terminal domain (NTD) of GRK2, which is identical in GRK3, as a discrete element required for the full agonist-selectivity of MOR-GRK2 interaction and show that the …
Key phosphorylation sites for robust β-arrestin2 binding at the MOR ...
2024年8月2日 · We show that both GRK2/3 and GRK5/6 subfamilies promote phosphorylation of 370 Thr and 375 Ser. Importantly, only GRK2/3 induce phosphorylation of 376 Thr and 379 …
Role of the G protein-coupled receptor kinase 2/3 N terminus in ...
2025年1月1日 · Focusing on GRK2 as a prototype, we show that this single GRK subtype can distinguish the endocytic activities of different MOR agonists in cells lacking other GRKs and …
GRK2 Dictates A Functional Switch of Peripheral Mu-Opioid …
2020年12月12日 · Here we identify that G protein-coupled receptor kinase 2 (GRK2) constitutively interacts with MOR in peripheral sensory neurons to suppress peripheral MOR activity. Brief …
Monoclonal antibody targeting mu-opioid receptor attenuates …
2023年10月1日 · 3A5C7 facilitates morphine-induced MOR endocytosis via GRK2/β-arrestin2 pathway. Morphine is a frequently used analgesic that activates the mu-opioid receptor …
要影响。许多实验表明GRK2 可以调节MOR的功能发挥,在长期注射吗啡的大鼠的蓝斑区和皮质中,GRK2 表达水平� 所上升。β-arrestin的募集需要激活GRK2 和MOR 磷酸化,而GRK募集也依赖 …
Signal profiles and spatial regulation of β-arrestin recruitment ...
2025年1月15日 · We co-expressed mStayGold-tagged MOR (MOR-mSG), Halo-tagged Gβ subunit (Halo-Gβ 1 or Halo-Gβ 5), and SNAP-tagged GRK3 (GRK3-SNAP) in the …
Involvement of PKC alpha and G-protein-coupled receptor kinase …
In mature mammalian neurons, different MOR agonists can induce MOR desensitization by different mechanisms, morphine by a PKCalpha-mediated, heterologous mechanism and …
Agonist-selective recruitment of engineered protein probes and of GRK2 …
We focused on GRK2 because this kinase is known to be important for generating agonist-selective patterns of multi-site phosphorylation in the MOR cytoplasmic tail, which convey …
Multisite phosphorylation is required for sustained interaction with ...
We identified two components of high-efficacy agonist desensitization of MOR: a sustained component, which required GRK2-mediated phosphorylation and a potential soluble factor, …