Effects of the selective protein kinase C inhibitor Ro 31-7549 on human angiotensin II receptor desensitisation and intracellular calcium release

FEBS Lett. 1995 Aug 7;369(2-3):263-6. doi: 10.1016/0014-5793(95)00725-o.

Abstract

The mechanism underlying type I angiotensin II (Ang II) receptor (AT1 receptor) desensitisation is unknown. Structural features suggest it may be a substrate for protein kinase C (PKC). The effects of a selective PKC inhibitor, Ro 31-7549, on receptor desensitisation were investigated in CHO cells expressing the human AT1 receptor. Desensitisation was demonstrated with respect to the calcium response to Ang II in Fura-2-loaded cells. Ro 31-7549 had no effect on desensitisation. However, pretreatment with Ro 31-7549 caused a dose-dependent reduction in calcium release from intracellular stores. PKC may therefore act at a locus distal from the receptor itself.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiotensin II / metabolism
  • Angiotensin II / pharmacology
  • Animals
  • CHO Cells
  • Calcium / metabolism*
  • Cricetinae
  • Humans
  • Indoles / pharmacology*
  • Ion Transport / drug effects
  • Maleimides / pharmacology*
  • Protein Kinase C / antagonists & inhibitors*
  • Protein Kinase C / physiology
  • Receptors, Angiotensin / genetics
  • Receptors, Angiotensin / physiology*
  • Transfection

Substances

  • Indoles
  • Maleimides
  • Receptors, Angiotensin
  • Angiotensin II
  • Protein Kinase C
  • Calcium
  • Ro 31-7549