A proposed structure for transmembrane segment 7 of G protein-coupled receptors incorporating an asn-Pro/Asp-Pro motif

Biophys J. 1998 Aug;75(2):601-11. doi: 10.1016/S0006-3495(98)77551-4.

Abstract

Transmembrane segment (TMS) 7 has been shown to play an important role in the signal transduction function of G-protein-coupled receptors (GPCRs). Although transmembrane segments are most likely to adopt a helical structure, results from a variety of experimental studies involving TMS 7 are inconsistent with it being an ideal alpha-helix. Using results from a search of the structure database and extensive simulated annealing Monte Carlo runs with the new Conformational Memories method, we have identified the conserved (N/D)PxxY region of TMS 7 as the major determinant for deviation of TMS 7 from ideal helicity. The perturbation consists of an Asx turn and a flexible "hinge" region. The Conformational Memories procedure yielded a model structure of TMS 7 which, unlike an ideal alpha-helix, is capable of accommodating all of the experimentally derived geometrical criteria for the interactions of TMS 7 in the transmembrane bundle of GPCRs. In the context of the entire structure of a transmembrane bundle model for the 5HT2a receptor, the specific perturbation of TMS 7 by the NP sequence suggests a structural hypothesis for the pattern of amino acid conservation observed in TMS 1, 2, and 7 of GPCRs. The structure resulting from the incorporation of the (N/D)P motif satisfies fully the H-bonding capabilities of the 100% conserved polar residues in these TMSs, in agreement with results from mutagenesis experiments. The flexibility introduced by the specific structural perturbation produced by the (NP/DP) motif in TMS 7 is proposed to have a significant role in receptor activation.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amino Acid Sequence
  • Cell Membrane / physiology
  • Conserved Sequence
  • Databases as Topic
  • Dipeptides
  • GTP-Binding Proteins / metabolism*
  • Hydrogen Bonding
  • Models, Molecular
  • Molecular Sequence Data
  • Peptide Fragments / chemistry
  • Protein Structure, Secondary*
  • Receptor, Serotonin, 5-HT2A
  • Receptors, Cell Surface / chemistry*
  • Receptors, Cell Surface / physiology
  • Receptors, Serotonin / chemistry*
  • Receptors, Serotonin / physiology*
  • Recombinant Proteins / chemistry
  • Sequence Alignment
  • Signal Transduction

Substances

  • Dipeptides
  • Peptide Fragments
  • Receptor, Serotonin, 5-HT2A
  • Receptors, Cell Surface
  • Receptors, Serotonin
  • Recombinant Proteins
  • asparaginyl-proline
  • aspartyl-proline
  • GTP-Binding Proteins