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PKC412 inhibits the zinc finger 198-fibroblast growth factor receptor 1 fusion tyrosine kinase and is active in treatment of stem cell myeloproliferative disorder.
Chen J, Deangelo DJ, Kutok JL, Williams IR, Lee BH, Wadleigh M, Duclos N, Cohen S, Adelsperger J, Okabe R, Coburn A, Galinsky I, Huntly B, Cohen PS, Meyer T, Fabbro D, Roesel J, Banerji L, Griffin JD, Xiao S, Fletcher JA, Stone RM, Gilliland DG. Chen J, et al. Proc Natl Acad Sci U S A. 2004 Oct 5;101(40):14479-84. doi: 10.1073/pnas.0404438101. Epub 2004 Sep 24. Proc Natl Acad Sci U S A. 2004. PMID: 15448205 Free PMC article.
Fibroblast growth factor receptor 3 associates with and tyrosine phosphorylates p90 RSK2, leading to RSK2 activation that mediates hematopoietic transformation.
Kang S, Elf S, Dong S, Hitosugi T, Lythgoe K, Guo A, Ruan H, Lonial S, Khoury HJ, Williams IR, Lee BH, Roesel JL, Karsenty G, Hanauer A, Taunton J, Boggon TJ, Gu TL, Chen J. Kang S, et al. Among authors: chen j. Mol Cell Biol. 2009 Apr;29(8):2105-17. doi: 10.1128/MCB.00998-08. Epub 2009 Feb 17. Mol Cell Biol. 2009. PMID: 19223461 Free PMC article.
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