Developments of Fms-like Tyrosine Kinase 3 Inhibitors as Anticancer Agents for AML Treatment

C Ma, S Cui, R Xu - Current Medicinal Chemistry, 2024 - ingentaconnect.com
Background: FMS-like tyrosine kinase 3 (FLT3) is a commonly mutated gene in acute
myeloid leukemia. As a receptor tyrosine kinase (RTK), FLT3 plays a role in the proliferation …

Combating drug resistance in acute myeloid leukaemia by drug rotations: the effects of quizartinib and pexidartinib

J Yang, HJG Lindström, R Friedman - Cancer Cell International, 2021 - Springer
Background Acute myeloid leukaemia (AML) is an aggressive blood cancer. In
approximately 30% of the cases, driver mutations in the FLT3 gene are identified. FLT3 …

Prediction of resistance to small molecule FLT3 inhibitors: implications for molecularly targeted therapy of acute leukemia

J Cools, N Mentens, P Furet, D Fabbro, JJ Clark… - Cancer research, 2004 - AACR
Mutations in the receptor tyrosine kinase FLT3 occur frequently in patients with acute
myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL). Small molecules that …

Theoretical studies aimed at finding FLT3 inhibitors and a promising compound and molecular pattern with dual aurora B/FLT3 activity

ÍA Fernandes, D Braga Resende, TC Ramalho, K Kuca… - Molecules, 2020 - mdpi.com
FLT3 and dual Aurora B/FLT3 inhibitors have shown relevance in the search for promising
new anticancer compounds, mainly for acute myeloid leukemia (AML). This study was …

Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases

F Baska, A Sipos, Z Őrfi, Z Nemes, J Dobos… - European Journal of …, 2019 - Elsevier
Aberrant activation of FMS-like tyrosine receptor kinase 3 (FLT3) is implicated in the
pathogenesis of acute myeloid leukemia (AML) in 20–30% of patients. In this study we …

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) …

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 …

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 …

Molecular Modeling Studies of N-phenylpyrimidine-4-amine Derivatives for Inhibiting FMS-like Tyrosine Kinase-3

S Ghosh, S Keretsu, SJ Cho - International Journal of Molecular Sciences, 2021 - mdpi.com
Overexpression and frequent mutations in FMS-like tyrosine kinase-3 (FLT3) are considered
risk factors for severe acute myeloid leukemia (AML). Hyperactive FLT3 induces premature …

Flt3 receptor tyrosine kinase as a drug target in leukemia

D Schmidt-Arras, J Schwable… - Current …, 2004 - ingentaconnect.com
The hematopoietic class III receptor tyrosine kinase (RTK) Flt3 (Flk2, STK1) has recently
received much attention as a potential drug target. Activation of Flt3 by different types of …