Structure of the membrane reconstituted transmembrane-juxtamembrane peptide EGFR(622-660) and its interaction with Ca2+/calmodulin

Biochemistry. 2006 Oct 24;45(42):12704-14. doi: 10.1021/bi061264m.

Abstract

The transmembrane (TM) and juxtamembrane (JM) regions of the epidermal growth factor receptor (EGFR) couple ligand binding in the extracellular domain to activation of the kinase domain. Solid-state NMR and polarized FTIR measurements of peptides corresponding to the TM plus JM regions of EGFR (residues 622-660) reconstituted in model phospholipid membranes are presented to address the role of the short cytoplasmic JM sequence (residues 645-660) in regulating EGFR activity. We show that the TM domain is helical with a transition to non-helical structure at the TM-JM boundary. Fluorescence measurements indicate that the JM region of EGFR(622-660) binds to the membrane surface and that binding can be reversed by the addition of the complex of Ca2+ and calmodulin. Together these data support models suggesting the cytoplasmic JM region of EGFR plays an active role in regulating receptor activity.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Amino Acid Sequence
  • Binding Sites
  • Calcium / metabolism*
  • Calmodulin / chemistry
  • Calmodulin / metabolism*
  • Carbon Isotopes
  • Circular Dichroism
  • Deuterium
  • Dimerization
  • ErbB Receptors / chemistry
  • ErbB Receptors / metabolism*
  • Ligands
  • Magnetic Resonance Spectroscopy
  • Peptide Fragments / chemical synthesis
  • Peptide Fragments / chemistry
  • Peptide Fragments / metabolism*
  • Protein Structure, Secondary
  • Spectrophotometry, Infrared

Substances

  • Calmodulin
  • Carbon Isotopes
  • Ligands
  • Peptide Fragments
  • Deuterium
  • ErbB Receptors
  • Calcium