From Proteopedia
proteopedia linkproteopedia link Neurotensin Receptor (Rattus norvegicus)
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Introduction
The neurotensin receptor (NTSR1) belongs to the superfamily of proteins known as G protein-coupled receptors (GPCRs) and responds to the 13 amino acid hormone nuerotensin (NT). There are currently around 800 G protein-coupled receptors that have been identified and are thought to be responsible for roughly 80% of signal transduction across the cell membrane.(reference year in g protein) These receptors are involved in a vast array of physiological processes within the body that range from interactions with dopamine to effects on secretion of bile in the intestines and are a major site of drug targets in medicine. (reference 5 main families) (reference enhancement jujunem) (Reference dopamine)
Neurotensin
Structure
Overall Structure
Like other G protein-coupled receptors, the neurotensin receptor is composed of 3 distinct regions. An extracellular binding site where neurotensin binds and causes a conformational change of the protein, a region containing that transduce the signal from the extracellular side of the cell membrane to the intracellular side, and an intracellular region that, when activated by a conformational change in the protein, activates a G protein associated with this receptor.
Neurotensin Binding Site
Hydrophobic Stacking
Sodium Binding Pocket
Allosteric Effects
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References
Millar, Robert P., and Claire L. Newton. "The year in G protein-coupled receptor research." Molecular endocrinology 24.1 (2010): 261-274.
Fredriksson, Robert, et al. "The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints." Molecular pharmacology 63.6 (2003): 1256-1272.
Gui, Xianyong, and Robert E. Carraway. "Enhancement of jejunal absorption of conjugated bile acid by neurotensin in rats." Gastroenterology 120.1 (2001): 151-160.
Binder, Elisabeth B., et al. "Neurotensin and dopamine interactions."Pharmacological reviews 53.4 (2001): 453-486.