ArticleScientific reports2016
Structure and dynamics of a constitutively active neurotensin receptor.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 34 papers.
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Who cites it
34 citing papers in PubMed, 69 citations in OpenAlex.
- Advances in neurotensin receptor 1-targeted molecular probes for tumor molecular imaging and therapy.Frontiers in oncology · 2026Review
- Design and Synthesis ofChemMedChem · 2025Article
- Dually Labeled Neurotensin NTSJournal of medicinal chemistry · 2024Article
- G Protein-Coupled Receptor-Ligand Pose and Functional Class Prediction.International journal of molecular sciences · 2024Article
- Bayesian network models identify cooperative GPCR:G protein interactions that contribute to G protein coupling.The Journal of biological chemistry · 2024Article
- Insights on the G protein-coupled receptor helix 8 solution structure and orientation using a neurotensin receptor 1 peptide.Protein science : a publication of the Protein Society · 2024Article
- Single-molecule visualization of human ACommunications biology · 2023Article
- Bayesian network models identify co-operative GPCR:G protein interactions that contribute to G protein coupling.bioRxiv : the preprint server for biology · 2023Article
- NMR sample optimization and backbone assignment of a stabilized neurotensin receptor.Journal of structural biology · 2023Article
- Screening of Membrane Protein Production by Comparison of Transient Expression in Insect and Mammalian Cells.Biomolecules · 2023Article
- A peroxidase-derived ligand that inducesFrontiers in cellular and infection microbiology · 2023Article
- Effect of Ligands and Transducers on the Neurotensin Receptor 1 Conformational Ensemble.Journal of the American Chemical Society · 2022Article
- Sequence coevolution and structure stabilization modulate olfactory receptor expression.Biophysical journal · 2022Article
- Article
- Allosteric communication regulates ligand-specific GPCR activity.The FEBS journal · 2021Review
- Engineering of Challenging G Protein-Coupled Receptors for Structure Determination and Biophysical Studies.Molecules (Basel, Switzerland) · 2021Review
- Complexes of the neurotensin receptor 1 with small-molecule ligands reveal structural determinants of full, partial, and inverse agonism.Science advances · 2021Article
- Conformational Changes in Tyrosine 11 of Neurotensin Are Required to Activate the Neurotensin Receptor 1.ACS pharmacology & translational science · 2020Article
- Conformational dynamics of a G protein-coupled receptor helix 8 in lipid membranes.Science advances · 2020Article
- A Structural Study on theToxins · 2020Article
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Authors and funding
8 authors at 4 institutions in 1 country.
Funding
Abstract
Many G protein-coupled receptors show constitutive activity, resulting in the production of a second messenger in the absence of an agonist; and naturally occurring constitutively active mutations in receptors have been implicated in diseases. To gain insight into mechanistic aspects of constitutive activity, we report here the 3.3 Å crystal structure of a constitutively active, agonist-bound neurotensin receptor (NTSR1) and molecular dynamics simulations of agonist-occupied and ligand-free receptor. Comparison with the structure of a NTSR1 variant that has little constitutive activity reveals uncoupling of the ligand-binding domain from conserved connector residues, that effect conformational changes during GPCR activation. Furthermore, molecular dynamics simulations show strong contacts between connector residue side chains and increased flexibility at the intracellular receptor face as features that coincide with robust signalling in cells. The loss of correlation between the binding pocket and conserved connector residues, combined with altered receptor dynamics, possibly explains the reduced neurotensin efficacy in the constitutively active NTSR1 and a facilitated initial engagement with G protein in the absence of agonist.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.