Effect of K252a, a protein kinase inhibitor, on the proliferation of vascular smooth muscle cells

Biochem Biophys Res Commun. 1990 Dec 31;173(3):976-81. doi: 10.1016/s0006-291x(05)80881-2.

Abstract

In the growth arrested cultures of bovine carotid smooth muscle, K252a (10 - 100 ng/ml), a protein kinase inhibitor with wide spectrum suppressed the cell proliferation induced by TPA and increase of serum. K252a was more potent in the antiproliferative activity than H7, a C-kinase-specific inhibitor, but less than staurosporine, another wide-spectrum protein kinase inhibitor. Since C-kinase plays an important role in the signal transduction leading to the cell proliferation and K252a inhibits C-kinase in vitro, the antiproliferative effect of K252a to carotid smooth muscle cells is likely to be exerted through c-kinase dependent pathway.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Carbazoles / pharmacology*
  • Carotid Arteries / metabolism
  • Cattle
  • Cell Division / drug effects
  • Cells, Cultured
  • DNA / biosynthesis
  • Indole Alkaloids
  • Muscle Contraction / drug effects
  • Muscle, Smooth, Vascular / blood supply
  • Muscle, Smooth, Vascular / drug effects
  • Muscle, Smooth, Vascular / physiology*
  • Protein Kinase C / antagonists & inhibitors*
  • Protein Kinase C / genetics
  • Signal Transduction / drug effects

Substances

  • Carbazoles
  • Indole Alkaloids
  • DNA
  • staurosporine aglycone
  • Protein Kinase C