Maurocalcine and domain A of the II-III loop of the dihydropyridine receptor Cav 1.1 subunit share common binding sites on the skeletal ryanodine receptor

J Biol Chem. 2005 Feb 11;280(6):4013-6. doi: 10.1074/jbc.C400433200. Epub 2004 Dec 9.

Abstract

Maurocalcine is a scorpion venom toxin of 33 residues that bears a striking resemblance to the domain A of the dihydropyridine voltage-dependent calcium channel type 1.1 (Cav1.1) subunit. This domain belongs to the II-III loop of Cav1.1, which is implicated in excitation-contraction coupling. Besides the structural homology, maurocalcine also modulates RyR1 channel activity in a manner akin to a synthetic peptide of domain A. Because of these similarities, we hypothesized that maurocalcine and domain A may bind onto an identical region(s) of RyR1. Using a set of RyR1 fragments, we demonstrate that peptide A and maurocalcine bind onto two discrete RyR1 regions: fragments 3 and 7 encompassing residues 1021-1631 and 3201-3661, respectively. The binding onto fragment 7 is of greater importance and was thus further investigated. We found that the amino acid region 3351-3507 of RyR1 (fragment 7.2) is sufficient for these interactions. Proof that peptide A and maurocalcine bind onto the same site is provided by competition experiments in which binding of fragment 7.2 to peptide A is inhibited by preincubation with maurocalcine. Moreover, when expressed in COS-7 cells, RyR1 carrying a deletion of fragment 7 shows a loss of interaction with both peptide A and maurocalcine. At the functional level, this deletion abolishes the maurocalcine induced stimulation of [3H]ryanodine binding onto microsomes of transfected COS-7 cells without affecting the caffeine and ATP responses.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Triphosphate / chemistry
  • Animals
  • Binding Sites
  • Binding, Competitive
  • COS Cells
  • Calcium Channels, L-Type / chemistry*
  • Caveolin 1
  • Caveolins / chemistry*
  • Chromatography
  • Cloning, Molecular
  • Cryoelectron Microscopy
  • Microscopy, Fluorescence
  • Muscle, Skeletal / metabolism
  • Peptides / chemistry
  • Plasmids / metabolism
  • Protein Binding
  • Protein Structure, Tertiary
  • Recombinant Fusion Proteins / chemistry
  • Ryanodine / chemistry
  • Ryanodine Receptor Calcium Release Channel / chemistry
  • Scorpion Venoms / chemistry
  • Scorpion Venoms / pharmacology*
  • Transfection

Substances

  • Calcium Channels, L-Type
  • Caveolin 1
  • Caveolins
  • Peptides
  • Recombinant Fusion Proteins
  • Ryanodine Receptor Calcium Release Channel
  • Scorpion Venoms
  • maurocalcine
  • Ryanodine
  • Adenosine Triphosphate