Protein kinase Calpha: disease regulator and therapeutic target

Trends Pharmacol Sci. 2010 Jan;31(1):8-14. doi: 10.1016/j.tips.2009.10.006. Epub 2009 Dec 5.

Abstract

Protein kinase Calpha (PKCalpha) is a member of the AGC (which includes PKD, PKG and PKC) family of serine/threonine protein kinases that is widely expressed in mammalian tissues. It is closely related in structure, function and regulation to other members of the protein kinase C family, but has specific functions within the tissues in which it is expressed. There is substantial recent evidence, from gene knockout studies in particular, that PKCalpha activity regulates cardiac contractility, atherogenesis, cancer and arterial thrombosis. Selective targeting of PKCalpha therefore has potential therapeutic value in a wide variety of disease states, although will be technically complicated by the ubiquitous expression and multiple functions of the molecule.

Publication types

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

MeSH terms

  • Animals
  • Cardiovascular Diseases / drug therapy
  • Cardiovascular Diseases / physiopathology
  • Disease Models, Animal
  • Drug Delivery Systems*
  • Humans
  • Mice
  • Mice, Knockout
  • Neoplasms / drug therapy
  • Neoplasms / physiopathology
  • Protein Kinase C-alpha / drug effects*
  • Protein Kinase C-alpha / metabolism
  • Thrombosis / drug therapy
  • Thrombosis / physiopathology

Substances

  • Protein Kinase C-alpha