Intermolecular interactions between the neurotensin and the third extracellular loop of human neurotensin 1 receptor

J Biomol Struct Dyn. 2013 Dec;31(12):1381-92. doi: 10.1080/07391102.2012.736776. Epub 2012 Nov 12.

Abstract

Neurotensin (NT) is a tridecapeptide hormone in the periphery and neurotransmitter in the brain that principally activates three receptor subtypes, named NTS1, NTS2, and NTS3. Since little is known about its structure in the presence of its principal receptor NTS1, we determined it using the key domain of the receptor, i.e. the third extracellular loop. We conclude the following: (i) for the receptor fragment, NT binding modifies its central part, underlying the great flexibility and adaptability of this region; (ii) for bound NT, the extended conformation of its C-terminus is confirmed for the first time in experimental conditions and in the presence of a part of the receptor; and (iii) despite some substitutions, the human receptor residues that are involved in the interaction with NT could be similar to those of the rat receptor which play an important role in NT binding.

MeSH terms

  • Amino Acid Sequence
  • Binding Sites
  • Humans
  • Magnetic Resonance Spectroscopy
  • Models, Molecular
  • Molecular Sequence Data
  • Neurotensin / chemistry*
  • Neurotensin / metabolism
  • Peptide Fragments / chemistry*
  • Peptide Fragments / metabolism
  • Protein Binding
  • Protein Conformation
  • Protein Isoforms / chemistry
  • Protein Isoforms / metabolism
  • Protein Structure, Tertiary*
  • Receptors, Neurotensin / chemistry*
  • Receptors, Neurotensin / metabolism

Substances

  • Peptide Fragments
  • Protein Isoforms
  • Receptors, Neurotensin
  • Neurotensin