PKC-θ is a drug target for prevention of T cell-mediated autoimmunity and allograft rejection

Endocr Metab Immune Disord Drug Targets. 2010 Dec;10(4):367-72. doi: 10.2174/1871530311006040367.


Protein kinase C theta (PKC-θ) is a key kinase in mediating T cell receptor (TCR) signals. PKC-θ activated by T cell receptor (TCR) engagement translocates to immunological synapses and regulates the activation of transcriptional factors NFκB, AP-1, and NFAT. These transcription factors then activate target genes such as IL-2. T cells deficient in PKC-θ display defects in T cell activation, survival, activation-induced cell death, and the differentiation into inflammatory T cells, such as Th2 and Th17 cells both in vitro and in vivo. Since these effector T helper cells are responsible for mediating autoimmunity, selective inhibition of PKC-θ is considered a treatment for prevention of autoimmune diseases and allograft rejection.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Autoimmune Diseases / enzymology
  • Autoimmune Diseases / immunology
  • Autoimmune Diseases / prevention & control*
  • Autoimmunity / drug effects*
  • Graft Rejection / enzymology
  • Graft Rejection / immunology
  • Graft Rejection / prevention & control*
  • Humans
  • Immunosuppressive Agents / pharmacology*
  • Isoenzymes
  • Protein Kinase C / antagonists & inhibitors*
  • Protein Kinase C / metabolism
  • Protein Kinase Inhibitors / pharmacology*
  • Protein Transport
  • Signal Transduction / drug effects
  • T-Lymphocytes / drug effects*
  • T-Lymphocytes / enzymology
  • T-Lymphocytes / immunology
  • Transplantation, Homologous


  • Immunosuppressive Agents
  • Isoenzymes
  • Protein Kinase Inhibitors
  • Protein Kinase C