The molecular mechanism behind resistance of the kinase FLT3 to the inhibitor quizartinib

R Friedman - Proteins: Structure, Function, and Bioinformatics, 2017 - Wiley Online Library
Fms‐like tyrosine kinase 3 (FLT3) is a receptor tyrosine kinase that is a drug target for
leukemias. Several potent inhibitors of FLT3 exist, and bind to the inactive form of the …

Deciphering the molecular mechanism of FLT3 resistance mutations

PS Georgoulia, S Bjelic, R Friedman - The FEBS Journal, 2020 - Wiley Online Library
FMS‐like tyrosine kinase 3 (FLT3) has been found to be mutated in~ 30% of acute myeloid
leukaemia patients. Small‐molecule inhibitors targeting FLT3 that are currently approved or …

Resistance to a tyrosine kinase inhibitor mediated by changes to the conformation space of the kinase

TS Freire, I Caracelli, J Zukerman-Schpector… - Physical Chemistry …, 2023 - pubs.rsc.org
Gilteritinib is a highly selective and effective inhibitor of the FLT3/ITD mutated protein, and is
used successfully in treating acute myeloid leukaemia (AML). Unfortunately, tumour cells …

FMS-like tyrosine kinase 3 (FLT3) inhibitors: Molecular docking and experimental studies

B Mashkani, MH Tanipour, M Saadatmandzadeh… - European journal of …, 2016 - Elsevier
Activating mutations in FMS-like tyrosine kinase 3 (FLT3) occur in 25% of acute lymphoid
and 30% of acute myeloid leukaemia cases. Therefore, FLT3 is a potential therapeutic target …

Crystal structure of the FLT3 kinase domain bound to the inhibitor Quizartinib (AC220)

JA Zorn, Q Wang, E Fujimura, T Barros, J Kuriyan - PloS one, 2015 - journals.plos.org
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 structural effect of FLT3 mutations at 835th position and their interaction with acute myeloid leukemia inhibitors: in silico approach

AM Al-Subaie, B Kamaraj - International journal of molecular sciences, 2021 - mdpi.com
FMS-like tyrosine kinase 3 (FLT3) gene mutations have been found in more than one-third of
Acute Myeloid Leukemia (AML) cases. The most common point mutation in FLT3 occurs at …

A molecular dynamics simulation study for variant drug responses due to FMS-like tyrosine kinase 3 G697R mutation

CC Lee, YC Chuang, YL Liu, CN Yang - RSC advances, 2017 - pubs.rsc.org
FMS-like tyrosine kinase 3 (FLT3) is an attractive target for acute myeloid leukemia. Recent
studies have suggested that the application of small-molecule kinase inhibitors is a …

Understanding gilteritinib resistance to FLT3-F691L mutation through an integrated computational strategy

S Zhou, B Yang, Y Xu, A Gu, J Peng, J Fu - Journal of Molecular Modeling, 2022 - Springer
FMS-like tyrosine kinase 3 (FLT3) serves as an important drug target for acute myeloid
leukemia (AML), and gene mutations of FLT3 have been closely associated with AML …

Insight into the inhibitor discrimination by FLT 3 F691L

S Verma, A Singh, A Kumari, B Pandey… - Chemical Biology & …, 2018 - Wiley Online Library
Fms‐like tyrosine kinase 3 (FLT 3) belongs to the receptor tyrosine kinase family and
expressed in hematopoietic progenitor cells. FLT 3 gene mutations are reported in~ 30% of …

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 …