[HTML][HTML] Sensitivity toward sorafenib and sunitinib varies between different activating and drug-resistant FLT3-ITD mutations
RK Kancha, R Grundler, C Peschel, J Duyster - Experimental hematology, 2007 - Elsevier
OBJECTIVE: Activating mutations in FLT3 are known to be a frequent transforming event in
acute myeloid leukemia. Small molecule–inhibitor therapy targeting the FLT3 kinase is …
acute myeloid leukemia. Small molecule–inhibitor therapy targeting the FLT3 kinase is …
Targeting AML-associated FLT3 mutations with a type I kinase inhibitor
LQM Jones, K Melgar, L Bolanos… - The Journal of …, 2020 - Am Soc Clin Investig
Tyrosine kinase domain (TKD) mutations contribute to acquired resistance to FMS-like
tyrosine kinase 3 (FLT3) inhibitors used to treat FLT3-mutant acute myeloid leukemia (AML) …
tyrosine kinase 3 (FLT3) inhibitors used to treat FLT3-mutant acute myeloid leukemia (AML) …
Discovery of N2-(4-Amino-cyclohexyl)-9-cyclopentyl-N6-(4-morpholin-4-ylmethyl-phenyl)-9H-purine-2,6-diamine as a Potent FLT3 Kinase Inhibitor for Acute …
T Gucky, E Reznickova… - Journal of Medicinal …, 2018 - ACS Publications
FLT3 tyrosine kinase is a potential drug target in acute myeloid leukemia (AML) because
patients with FLT3-ITD mutations respond poorly to standard cytotoxic agents and there is a …
patients with FLT3-ITD mutations respond poorly to standard cytotoxic agents and there is a …
Targeting FLT3 to treat leukemia
H Konig, M Levis - Expert opinion on therapeutic targets, 2015 - Taylor & Francis
Introduction: Approximately 23% of acute myeloid leukemia (AML) patients younger than 60
years of age carry a mutation in the transmembrane domain of the FMS-like tyrosine kinase …
years of age carry a mutation in the transmembrane domain of the FMS-like tyrosine kinase …
Illuminating the molecular mechanisms of tyrosine kinase inhibitor resistance for the FGFR1 gatekeeper mutation: the Achilles' heel of targeted therapy
Human fibroblast growth factor receptors (FGFRs) 1–4 are a family of receptor tyrosine
kinases that can serve as drivers of tumorigenesis. In particular, FGFR1 gene amplification …
kinases that can serve as drivers of tumorigenesis. In particular, FGFR1 gene amplification …
Prolonged exposure to FLT3 inhibitors leads to resistance via activation of parallel signaling pathways
Continuous treatment of malignancies with tyrosine kinase inhibitors (TKIs) may select for
resistant clones (ie, imatinib mesylate). To study resistance to TKIs targeting FLT3, a …
resistant clones (ie, imatinib mesylate). To study resistance to TKIs targeting FLT3, a …
Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD
CC Smith, EA Lasater, X Zhu, KC Lin… - Blood, The Journal …, 2013 - ashpublications.org
Secondary point mutations in the Fms-like tyrosine kinase 3 (FLT3) tyrosine kinase domain
(KD) are common causes of acquired clinical resistance to the FLT3 inhibitors AC220 …
(KD) are common causes of acquired clinical resistance to the FLT3 inhibitors AC220 …
The dual MEK/FLT3 inhibitor E6201 exerts cytotoxic activity against acute myeloid leukemia cells harboring resistance-conferring FLT3 mutations
W Zhang, G Borthakur, C Gao, Y Chen, H Mu… - Cancer research, 2016 - AACR
Fms-like tyrosine kinase 3 (FLT3) inhibition has elicited encouraging responses in acute
myeloid leukemia (AML) therapy. Unfortunately, unless combined with a bone marrow …
myeloid leukemia (AML) therapy. Unfortunately, unless combined with a bone marrow …
Enhancing antiproliferative activity and selectivity of a FLT-3 inhibitor by proteolysis targeting chimera conversion
GM Burslem, J Song, X Chen, J Hines… - Journal of the …, 2018 - ACS Publications
The receptor tyrosine kinase FLT-3 is frequently mutated in acute myeloid leukemia;
however, current small molecule inhibitors suffer from limited efficacy in the clinic …
however, current small molecule inhibitors suffer from limited efficacy in the clinic …
Reversal of Acquired Drug Resistance in FLT3-Mutated Acute Myeloid Leukemia Cells via Distinct Drug Combination Strategies
W Zhang, C Gao, M Konopleva, Y Chen… - Clinical Cancer …, 2014 - AACR
Purpose: FMS-like tyrosine kinase-3 (FLT3) internal tandem duplication (FLT3-ITD)
mutations are common in patients with acute myeloid leukemia (AML). These patients …
mutations are common in patients with acute myeloid leukemia (AML). These patients …