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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.(reference enhancement jujunem) (Reference dopamine) Due to the vast array of functions that these proteins serve and their high abundance within the body, these proteins have become a major site of drug targets in medicine making a deeper, more in depth understanding of these proteins very important. (drug discovery)

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

A major player in the transduction of the extracellular signal to the intracellular G protein is the hydrogen bonding network that links the bound hormone with the hydrophobic core of the neurotensin receptor. The carboxylate of L13 forms a hydrogen bond network with R327, R328, and Y324. The Y324 in turn then forms a network with F358, W321, A157, and F317 to traduce the signal through the transmembrane helices of the receptor. (Reference structural prereq)

Sodium Binding Pocket

Allosteric Effects

This is a sample scene created with SAT to by Group, and another to make of the protein. You can make your own scenes on SAT starting from scratch or loading and editing one of these sample scenes.