Therapeutic potential of tyrosine kinase 2 in autoimmunity

Expert Opin Ther Targets. 2014 May;18(5):571-80. doi: 10.1517/14728222.2014.892925. Epub 2014 Mar 21.

Abstract

Introduction: Tyrosine kinase 2 (Tyk2) is a Janus kinase family member that is crucial for signaling transduction in response to a wide variety of cytokines, including type I IFNs, IL-6, IL-10, IL-12 and IL-23. An appropriate expression of Tyk2-mediated signaling might be essential for maintaining normal immune responses.

Areas covered: This review summarizes that Tyk2 is essential for the differentiation and function of a wide variety of immune cells, including natural killer cells, B cells, as well as T helper cells. In addition, Tyk2-mediated signaling promoted the production of autoimmune-associated components, which is implicated in the pathogenesis of autoimmune diseases, such as rheumatoid arthritis, systemic lupus erythematosus, multiple sclerosis. Aberrant expression of Tyk2 was observed in many autoimmune conditions.

Expert opinion: Until recently, no patent filings had claimed selective inhibitors of Tyk2. Both CP-690,500 and CMP6 failed to be used in clinical treatment due to the difficulties of finding suitable selective leads or due to detrimental toxicities. Although the result of Cmpd1 is promising, it remains to be seen how specific the Tyk2 inhibitor is and how they are working. Currently, structure-based drug design (SBDD) technology has provided us with a quite useful window for SBDD of Tyk2 inhibitors.

Publication types

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

MeSH terms

  • Adaptive Immunity
  • Autoimmune Diseases / drug therapy*
  • Autoimmune Diseases / enzymology
  • Autoimmunity / physiology*
  • Dendritic Cells / drug effects
  • Dendritic Cells / enzymology
  • Dendritic Cells / immunology
  • Drug Design
  • Genetic Predisposition to Disease
  • Humans
  • Immunity, Cellular
  • Lymphocyte Subsets / drug effects
  • Lymphocyte Subsets / enzymology
  • Lymphocyte Subsets / immunology
  • Macrophages / drug effects
  • Macrophages / enzymology
  • Macrophages / immunology
  • Molecular Targeted Therapy*
  • Neutrophils / drug effects
  • Neutrophils / enzymology
  • Neutrophils / immunology
  • Piperidines / adverse effects
  • Piperidines / therapeutic use
  • Protein Kinase Inhibitors / pharmacology
  • Protein Kinase Inhibitors / therapeutic use*
  • Pyrimidines / adverse effects
  • Pyrimidines / therapeutic use
  • Pyrroles / adverse effects
  • Pyrroles / therapeutic use
  • TYK2 Kinase / antagonists & inhibitors*
  • TYK2 Kinase / genetics
  • TYK2 Kinase / physiology

Substances

  • Piperidines
  • Protein Kinase Inhibitors
  • Pyrimidines
  • Pyrroles
  • tofacitinib
  • TYK2 Kinase
  • TYK2 protein, human