Regulation of cardiac Na+,Ca2+ exchange and KATP potassium channels by PIP2

Science. 1996 Aug 16;273(5277):956-9. doi: 10.1126/science.273.5277.956.

Abstract

Cardiac Na+,Ca2+ exchange is activated by a mechanism that requires hydrolysis of adenosine triphosphate (ATP) but is not mediated by protein kinases. In giant cardiac membrane patches, ATP acted to generate phosphatidylinositol-4,5-bisphosphate (PIP2) from phosphatidylinositol (PI). The action of ATP was abolished by a PI-specific phospholipase C (PLC) and recovered after addition of exogenous PI; it was reversed by a PIP2-specific PLC; and it was mimicked by exogenous PIP2. High concentrations of free Ca2+ (5 to 20 microM) accelerated reversal of the ATP effect, and PLC activity in myocyte membranes was activated with a similar Ca2+ dependence. Aluminum reversed the ATP effect by binding with high affinity to PIP2. ATP-inhibited potassium channels (KATP) were also sensitive to PIP2, whereas Na+,K+ pumps and Na+ channels were not. Thus, PIP2 may be an important regulator of both ion transporters and channels.

Publication types

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

MeSH terms

  • Adenosine Triphosphate / metabolism
  • Adenosine Triphosphate / pharmacology
  • Aluminum / metabolism
  • Aluminum / pharmacology
  • Animals
  • Calcium / metabolism*
  • Calcium / pharmacology
  • Carrier Proteins / metabolism
  • Guinea Pigs
  • Myocardium / cytology
  • Myocardium / metabolism*
  • Patch-Clamp Techniques
  • Phosphatidylinositol 4,5-Diphosphate
  • Phosphatidylinositol Phosphates / metabolism*
  • Phosphatidylinositol Phosphates / pharmacology
  • Phosphatidylinositols / metabolism
  • Potassium Channel Blockers
  • Potassium Channels / metabolism*
  • Sodium / metabolism*
  • Sodium-Calcium Exchanger
  • Type C Phospholipases / metabolism

Substances

  • Carrier Proteins
  • Phosphatidylinositol 4,5-Diphosphate
  • Phosphatidylinositol Phosphates
  • Phosphatidylinositols
  • Potassium Channel Blockers
  • Potassium Channels
  • Sodium-Calcium Exchanger
  • Adenosine Triphosphate
  • Sodium
  • Aluminum
  • Type C Phospholipases
  • Calcium