Tyrosine kinase inhibitors bind and inhibit cytosolic FGFR1 fusion dimer phosphorylation

Stable Identifier
Reaction [binding]
Homo sapiens
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In a murine mouse model of ZNF198-FGFR1-induced EMS, treatment with the FGFR-inhibitor Midostaurin (PKC412) resulted in prolonged survival (Chen, 2004). Similarly, growth of ZNF-198-FGFR1-, FGFR1OP2-FGFR1-, and BCR-FGFR1-expressing lines is blocked by treatment with FGFR-inhibitors (Demiroglu, 2001; Gu, 2006; Chase, 2007; Zhen, 2007; Wasag, 2011).

Literature References
PubMed ID Title Journal Year
11739186 The t(8;22) in chronic myeloid leukemia fuses BCR to FGFR1: transforming activity and specific inhibition of FGFR1 fusion proteins

Demiroglu, A, Steer, EJ, Heath, C, Taylor, K, Bentley, M, Allen, SL, Koduru, P, Brody, JP, Hawson, G, Rodwell, R, Doody, ML, Carnicero, F, Reiter, A, Goldman, JM, Melo, JV, Cross, NC

Blood 2001
16946300 Phosphotyrosine profiling identifies the KG-1 cell line as a model for the study of FGFR1 fusions in acute myeloid leukemia

Gu, TL, Goss, VL, Reeves, C, Popova, L, Nardone, J, Macneill, J, Walters, DK, Wang, Y, Rush, J, Comb, MJ, Druker, BJ, Polakiewicz, RD

Blood 2006
15448205 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

Proc Natl Acad Sci U S A 2004
17698633 Activity of TKI258 against primary cells and cell lines with FGFR1 fusion genes associated with the 8p11 myeloproliferative syndrome

Chase, A, Grand, FH, Cross, NC

Blood 2007
17533378 Indirubin-3'-monoxime inhibits autophosphorylation of FGFR1 and stimulates ERK1/2 activity via p38 MAPK

Zhen, Y, Sørensen, V, Jin, Y, Suo, Z, Wied?ocha, A

Oncogene 2007
21330321 The kinase inhibitor TKI258 is active against the novel CUX1-FGFR1 fusion detected in a patient with T-lymphoblastic leukemia/lymphoma and t(7;8)(q22;p11)

Wasag, B, Lierman, E, Meeus, P, Cools, J, Vandenberghe, P

Haematologica 2011
Participant Of
Name Identifier Synonyms
precursor lymphoblastic lymphoma/leukemia 5600
subacute leukemia 3264
myelodysplastic myeloproliferative cancer 4972 Myeloproliferative/Myelodysplastic syndromes, unclassifiable myelodysplastic myeloproliferative disease, Unclassifiable Myeloproliferative/Myelodysplastic syndrome, Myelodysplastic/myeloproliferative disease (morphologic abnormality)
cancer 162 malignant tumor, malignant neoplasm, primary cancer
chronic myeloid leukemia 8552 CML, chronic myelogenous leukemia, no ICD-O subtype (morphologic abnormality), chronic myeloid leukemia, disease (disorder), chronic myeloid leukemia without mention of remission, CML - chronic Myelogenous Leukemia, chronic myeloid leukemia in remission (disorder), Myeloid Leukemia, chronic, CML in Remission, chronic myeloid leukemia in remission, chronic myeloid leukaemia, chronic myeloid leukemia NOS (disorder)
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