The accessible surface of the nicotinic acetylcholine receptor. Identification by chemical modification and cross-linking with 14C-dimethyl suberimidate

Eur J Biochem. 1998 Mar 1;252(2):222-8. doi: 10.1046/j.1432-1327.1998.2520222.x.

Abstract

To obtain structural information on the nicotinic acetylcholine receptor from Torpedo electric tissue we modified and cross-linked lysine residues with the agonistic bifunctional reagent [14C]dimethyl suberimidate. This reagent labels exposed lysine residues, especially those located near the ligand-binding site, and cross-links lysine residues located not more than 11 A, the length of the cross-linker, apart. Using this method, we identified a cross-link located between betaLys177 and betaLys191 showing that the 13 amino acids in between form a loop with these two residues located at the surface. Cross-linking also occurred between the vicinal lysine residues alphaLys76 and alphaLys77, indicating that these neighbouring lysine residues are not involved in a beta-sheet structure. A total of 21 out of 97 lysine residues present in the receptor were modified by [14C]dimethyl suberimidate. Thus these residues are located on the accessible extramembrane surface. The two lysine residues alphaLys76 and alphaLys179 were predominantly labelled. Because of the agonistic property of [14C]dimethyl suberimidate [Watty, A., Methfessel, C. & Hucho, F. (1997) Proc. Natl Acad. Sci. USA 94, 8202-8209] this might be due to their close proximity to the ligand binding site.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Binding Sites / physiology
  • Carbon Radioisotopes / metabolism
  • Cross-Linking Reagents / metabolism
  • Dimethyl Suberimidate / metabolism*
  • Lysine / metabolism
  • Molecular Sequence Data
  • Organophosphorus Compounds / metabolism
  • Protein Structure, Secondary
  • Receptors, Nicotinic / chemistry*
  • Sequence Analysis
  • Torpedo / physiology

Substances

  • 2-(4-isothiocyanatophenoxy)-1,3,2-dioxaphosphinene 2-oxide
  • Carbon Radioisotopes
  • Cross-Linking Reagents
  • Organophosphorus Compounds
  • Receptors, Nicotinic
  • Dimethyl Suberimidate
  • Lysine