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, …
Structural Dynamics and Thermostabilization of Neurotensin Receptor 1
The neurotensin receptor NTSR1 binds the peptide agonist neurotensin (NTS) and signals preferentially via the G q protein. Recently, Grisshammer and co-workers reported the crystal …
GPCR activation and GRK2 assembly by a biased intracellular
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 …
Complexes of the neurotensin receptor 1 with small-molecule …
The neurotensin receptor 1 (NTSR1) is a peptide-binding G protein–coupled receptor (GPCR) belonging to the ghrelin receptor family (1, 2), which encompasses several physiologically …
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. …
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 …
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 · 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 …
RCSB PDB - 8JPB: cryo-EM structure of NTSR1-GRK2-Galpha (q) …
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
NTSR1 is a promiscuous GPCR, coupling to Gs, Gq/11, Gi/o and G12/13 18. Both active- and inactive-state structures of NTSR1 have been determined by crystallography 19 – 21, and …
Design of allosteric modulators that change GPCR G protein …
2024年11月20日 · Here, using the prototypical class A GPCR neurotensin receptor 1 (NTSR1), we find that small molecules binding the intracellular GPCR-transducer interface change G …