RyR2 regulates Cx43 hemichannel intracellular Ca2+-dependent activation in cardiomyocytes

Cardiovasc Res. 2021 Jan 1;117(1):123-136. doi: 10.1093/cvr/cvz340.

Abstract

Aims: Connexin-based gap junctions are crucial for electrical communication in the heart; they are each composed of two docked hemichannels (HCs), supplied as unpaired channels via the sarcolemma. When open, an unpaired HC forms a large pore, high-conductance and Ca2+-permeable membrane shunt pathway that may disturb cardiomyocyte function. HCs composed of connexin 43 (Cx43), a major cardiac connexin, can be opened by electrical stimulation but only by very positive membrane potentials. Here, we investigated the activation of Cx43 HCs in murine ventricular cardiomyocytes voltage-clamped at -70 mV.

Methods and results: Using whole-cell patch-clamp, co-immunoprecipitation, western blot analysis, immunocytochemistry, proximity ligation assays, and protein docking studies, we found that stimulation of ryanodine receptors (RyRs) triggered unitary currents with a single-channel conductance of ∼220 pS, which were strongly reduced by Cx43 knockdown. Recordings under Ca2+-clamp conditions showed that both RyR activation and intracellular Ca2+ elevation were necessary for HC opening. Proximity ligation studies indicated close Cx43-RyR2 apposition (<40 nm), and both proteins co-immunoprecipitated indicating physical interaction. Molecular modelling suggested a strongly conserved RyR-mimicking peptide sequence (RyRHCIp), which inhibited RyR/Ca2+ HC activation but not voltage-triggered activation. The peptide also slowed down action potential repolarization. Interestingly, alterations in the concerned RyR sequence are known to be associated with primary familial hypertrophic cardiomyopathy.

Conclusion: Our results demonstrate that Cx43 HCs are intimately linked to RyRs, allowing them to open at negative diastolic membrane potential in response to RyR activation.

Keywords: Calcium; Cardiac; Connexin; Hemichannel; RyR2.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Action Potentials
  • Animals
  • Calcium / metabolism*
  • Calcium Channel Agonists / pharmacology
  • Calcium Signaling* / drug effects
  • Connexin 43 / genetics
  • Connexin 43 / metabolism*
  • Gap Junctions / drug effects
  • Gap Junctions / metabolism*
  • HeLa Cells
  • Humans
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Molecular Docking Simulation
  • Myocytes, Cardiac / drug effects
  • Myocytes, Cardiac / metabolism*
  • Protein Binding
  • Ryanodine Receptor Calcium Release Channel / drug effects
  • Ryanodine Receptor Calcium Release Channel / metabolism*

Substances

  • Calcium Channel Agonists
  • Connexin 43
  • GJA1 protein, mouse
  • Ryanodine Receptor Calcium Release Channel
  • ryanodine receptor 2. mouse
  • Calcium