Essential biphasic role for JAK3 catalytic activity in IL-2 receptor signaling

Nat Chem Biol. 2016 May;12(5):373-9. doi: 10.1038/nchembio.2056. Epub 2016 Mar 28.

Abstract

To drive lymphocyte proliferation and differentiation, common γ-chain (γc) cytokine receptors require hours to days of sustained stimulation. JAK1 and JAK3 kinases are found together in all γc-receptor complexes, but how their respective catalytic activities contribute to signaling over time is not known. Here we dissect the temporal requirements for JAK3 kinase activity with a selective covalent inhibitor (JAK3i). By monitoring phosphorylation of the transcription factor STAT5 over 20 h in CD4(+) T cells stimulated with interleukin 2 (IL-2), we document a second wave of signaling that is much more sensitive to JAK3i than the first wave. Selective inhibition of this second wave is sufficient to block cyclin expression and entry to S phase. An inhibitor-resistant JAK3 mutant (C905S) rescued all effects of JAK3i in isolated T cells and in mice. Our chemical genetic toolkit elucidates a biphasic requirement for JAK3 kinase activity in IL-2-driven T cell proliferation and will find broad utility in studies of γc-receptor signaling.

Publication types

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

MeSH terms

  • Animals
  • Apoptosis
  • CD4-Positive T-Lymphocytes / drug effects
  • CD4-Positive T-Lymphocytes / physiology
  • Cells, Cultured
  • Female
  • Gene Expression Regulation / physiology
  • Interferon-gamma
  • Interleukin-2 / genetics
  • Interleukin-2 / metabolism
  • Janus Kinase 3 / genetics
  • Janus Kinase 3 / metabolism*
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Mutagenesis, Site-Directed
  • Receptors, Interleukin-2 / genetics
  • Receptors, Interleukin-2 / metabolism*
  • Signal Transduction*

Substances

  • Interleukin-2
  • Receptors, Interleukin-2
  • Interferon-gamma
  • Jak3 protein, mouse
  • Janus Kinase 3

Associated data

  • PubChem-Substance/312338201
  • PubChem-Substance/312338202
  • PubChem-Substance/312338203
  • PubChem-Substance/312338204
  • PubChem-Substance/312338205
  • PubChem-Substance/312338206
  • PubChem-Substance/312338207
  • PubChem-Substance/312338208
  • PubChem-Substance/312338209
  • PubChem-Substance/312338210