Complexes of the neurotensin receptor 1 with small-molecule …
2021年1月27日 · Neurotensin receptor 1 (NTSR1) and related G protein–coupled receptors of the ghrelin family are clinically unexploited, and several mechanistic aspects of their activation and …
Conformational transitions of a neurotensin receptor 1–G
2019年6月26日 · Neurotensin receptor 1 (NTSR1) is a G-protein-coupled receptor (GPCR) that engages multiple subtypes of G protein, and is involved in the regulation of blood pressure, …
β-Arrestin-Biased Allosteric Modulator of NTSR1 ... - Cell Press
2020年5月28日 · NTSR1, a G protein-coupled receptor (GPCR), signals through the canonical activation of G proteins and engages β-arrestins to mediate distinct cellular signaling events. …
GPCR activation and GRK2 assembly by a biased intracellular agonist
2023年8月2日 · NTSR1 is a class A GPCR that is regulated by an endogenous peptide ligand, neurotensin 27 (NTS). Upon activation, NTSR1 couples to various signal effectors, including …
Structural Dynamics and Thermostabilization of Neurotensin Receptor 1
The neurotensin receptor NTSR1 binds the peptide agonist neurotensin (NTS) and signals preferentially via the Gq protein. Recently, Grisshammer and co-workers reported the crystal …
Neurotensin Receptor Allosterism Revealed in Complex with a …
2023年3月14日 · Recent studies indicate that biasing NTSR1 toward β-arrestin signaling can attenuate the actions of psychostimulants and other drugs of abuse. Here, we provide the …
具有偏向变构调节剂的复合物揭示了神经降压素受体变 …
2023年3月14日 · 最近的研究表明，将 NTSR1 偏向 β-arrestin 信号传导可以减弱精神兴奋剂和其他滥用药物的作用。 在这里，我们提供了 NTSR1 三元复合物与异三聚体 Gq 和 GoA 的冷冻电 …
Structural prerequisites for G-protein activation by the ... - Nature
2015年7月24日 · Our research focuses on understanding the structural and functional requirements for the activation of the neurotensin receptor 1 (NTSR1, ref. 8). Its agonist ligand …
8JPB: cryo-EM structure of NTSR1-GRK2-Galpha(q) complexes 1
2023年8月9日 · Here we report the complex structure of neurotensin receptor 1 (NTSR1) bound to GRK2, Gα q and the arrestin-biased ligand SBI-553 7 . The density map reveals the …
Structure of the Neurotensin Receptor 1 in complex with β-arrestin 1
While there are three neurotensin receptor subtypes, most of the physiologic responses of NTS are mediated by NTSR1. NTSR1 is a promiscuous GPCR, coupling to Gs, Gq/11, Gi/o and …