Characterizing and overriding the structural mechanism of the quizartinib-resistant FLT3 “gatekeeper” F691L mutation with PLX3397
CC Smith, C Zhang, KC Lin, EA Lasater, Y Zhang… - Cancer discovery, 2015 - AACR
Tyrosine kinase domain mutations are a common cause of acquired clinical resistance to
tyrosine kinase inhibitors (TKI) used to treat cancer, including the FLT3 inhibitor quizartinib …
tyrosine kinase inhibitors (TKI) used to treat cancer, including the FLT3 inhibitor quizartinib …
Crystal structure of the FLT3 kinase domain bound to the inhibitor Quizartinib (AC220)
More than 30% of acute myeloid leukemia (AML) patients possess activating mutations in
the receptor tyrosine kinase FMS-like tyrosine kinase 3 or FLT3. A small-molecule inhibitor …
the receptor tyrosine kinase FMS-like tyrosine kinase 3 or FLT3. A small-molecule inhibitor …
Crenolanib is a selective type I pan-FLT3 inhibitor
CC Smith, EA Lasater, KC Lin… - Proceedings of the …, 2014 - National Acad Sciences
Tyrosine kinase inhibitors (TKIs) represent transformative therapies for several
malignancies. Two critical features necessary for maximizing TKI tolerability and response …
malignancies. Two critical features necessary for maximizing TKI tolerability and response …
Quizartinib (AC220) is a potent second generation class III tyrosine kinase inhibitor that displays a distinct inhibition profile against mutant-FLT3, -PDGFRA and -KIT …
KM Kampa-Schittenhelm, MC Heinrich, F Akmut… - Molecular cancer, 2013 - Springer
Background Activating mutations of class III receptor tyrosine kinases (RTK) FLT3, PDGFR
and KIT are associated with multiple human neoplasms including hematologic …
and KIT are associated with multiple human neoplasms including hematologic …
A novel irreversible FLT3 inhibitor, FF-10101, shows excellent efficacy against AML cells with FLT3 mutations
T Yamaura, T Nakatani, K Uda, H Ogura… - Blood, The Journal …, 2018 - ashpublications.org
An activating mutation of Fms-like tyrosine kinase 3 (FLT3) is the most frequent genetic
alteration associated with poor prognosis in acute myeloid leukemia (AML). Although many …
alteration associated with poor prognosis in acute myeloid leukemia (AML). Although many …
FLT3 D835 mutations confer differential resistance to type II FLT3 inhibitors
CC Smith, K Lin, A Stecula, A Sali, NP Shah - Leukemia, 2015 - nature.com
Activating mutations in FLT3 occur in~ 30% of adult acute myeloid leukemia, primarily
consisting of internal tandem duplication (ITD) mutations (~ 25%) and point mutations in the …
consisting of internal tandem duplication (ITD) mutations (~ 25%) and point mutations in the …
Transient exposure to quizartinib mediates sustained inhibition of FLT3 signaling while specifically inducing apoptosis in FLT3-activated leukemia cells
RN Gunawardane, RR Nepomuceno, AM Rooks… - Molecular cancer …, 2013 - AACR
Fms-like tyrosine kinase 3 (FLT3) is implicated in the pathogenesis of acute myeloid
leukemia (AML). FLT3-activating internal tandem duplication (ITD) mutations are found in …
leukemia (AML). FLT3-activating internal tandem duplication (ITD) mutations are found in …
[HTML][HTML] Effect of Fms-like tyrosine kinase 3 (FLT3) ligand (FL) on antitumor activity of gilteritinib, a FLT3 inhibitor, in mice xenografted with FL-overexpressing cells
T Kawase, T Nakazawa, T Eguchi, H Tsuzuki, Y Ueno… - Oncotarget, 2019 - ncbi.nlm.nih.gov
Therapeutic effects of FLT3 inhibitors have been reported in acute myeloid leukemia (AML)
with constitutively activating FLT3 mutations, including internal tandem duplication (ITD) and …
with constitutively activating FLT3 mutations, including internal tandem duplication (ITD) and …
[HTML][HTML] FLT3 activating mutations display differential sensitivity to multiple tyrosine kinase inhibitors
B Nguyen, AB Williams, DJ Young, H Ma, L Li… - Oncotarget, 2017 - ncbi.nlm.nih.gov
ABSTRACT Fms-like tyrosine kinase-3 (FLT3) is a receptor tyrosine kinase that normally
functions in hematopoietic cell survival, proliferation and differentiation. Constitutively …
functions in hematopoietic cell survival, proliferation and differentiation. Constitutively …
FLT3 inhibition and mechanisms of drug resistance in mutant FLT3-positive AML
An appealing therapeutic target for AML is constitutively activated, mutant FLT3, which is
expressed in a subpopulation of AML patients and is generally a poor prognostic indicator in …
expressed in a subpopulation of AML patients and is generally a poor prognostic indicator in …