JAK protein kinase inhibitors

Drug News Perspect. 2005 Jun;18(5):305-10. doi: 10.1358/dnp.2005.18.5.904198.

Abstract

In humans, the Janus protein tyrosine kinase family (JAKs) contains four members: JAK1, JAK2, JAK3 and TYK2. JAKs phosphorylate signal transducers and activators of transcription (STATs) simultaneously with other phosphorylations required for activation, and there are several cellular mechanisms in place to inhibit JAK/STAT signaling. That one might be able to modulate selected JAK/STAT-mediated cellular signals by inhibiting JAK kinase activity to effect a positive therapeutic outcome is a tantalizing prospect, as yet incompletely realized. While current data suggest no therapeutic use for JAK1 and TYK2 inhibition, JAK2 inhibition seems a promising but not definitively tested mechanism for treatment of leukemia. More promising, however, are data indicating a possible therapeutic use of JAK3 inhibition. The restriction of the JAK3-deficient phenotype to the hematopoietic system and the resulting profound immune suppression suggest that JAK3 could be a target for immunosuppressive therapies used to prevent organ transplant rejection.

Publication types

  • Review

MeSH terms

  • Animals
  • Drug Design
  • Enzyme Inhibitors / pharmacology
  • Forecasting
  • Gene Expression Regulation / drug effects
  • Humans
  • Janus Kinase 1
  • Janus Kinase 2
  • Janus Kinase 3
  • Mannich Bases / pharmacology
  • Piperidines
  • Protein-Tyrosine Kinases / antagonists & inhibitors*
  • Protein-Tyrosine Kinases / metabolism
  • Proto-Oncogene Proteins / antagonists & inhibitors
  • Proto-Oncogene Proteins / metabolism
  • Pyrimidines / pharmacology
  • Pyrroles / pharmacology
  • Quinazolines / pharmacology
  • Signal Transduction / drug effects
  • TYK2 Kinase

Substances

  • Enzyme Inhibitors
  • Mannich Bases
  • NC 1153
  • Piperidines
  • Proto-Oncogene Proteins
  • Pyrimidines
  • Pyrroles
  • Quinazolines
  • WHI P131
  • tofacitinib
  • Protein-Tyrosine Kinases
  • JAK1 protein, human
  • JAK2 protein, human
  • JAK3 protein, human
  • Janus Kinase 1
  • Janus Kinase 2
  • Janus Kinase 3
  • TYK2 Kinase
  • TYK2 protein, human