Discovery of a benzimidazole-based dual FLT3/TrKA inhibitor targeting acute myeloid leukemia

EME Dokla, AK Abdel-Aziz, SN Milik… - Bioorganic & Medicinal …, 2022 - Elsevier
FMS-like tyrosine kinase 3 (FLT3) enzyme overexpression and mutations are the most
common molecular abnormalities associated with acute myeloid leukemia (AML). In …

Identification of novel FLT3 kinase inhibitors

D Pauwels, H Klaassen, I Lahortiga, A Kilonda… - European Journal of …, 2013 - Elsevier
FLT3 and PDGFR tyrosine kinases are important targets for therapy of different types of
leukemia. Several FLT3/PDGFR inhibitors are currently under clinical investigation for …

[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 …

Antileukemic effects of the novel, mutant FLT3 inhibitor NVP-AST487: effects on PKC412-sensitive and-resistant FLT3-expressing cells

E Weisberg, J Roesel, G Bold, P Furet… - Blood, The Journal …, 2008 - ashpublications.org
An attractive target for therapeutic intervention is constitutively activated, mutant FLT3, which
is expressed in a subpopulation of patients with acute myelocyic leukemia (AML) and is …

FLT3-ITD-TKD dual mutants associated with AML confer resistance to FLT3 PTK inhibitors and cytotoxic agents by overexpression of Bcl-x (L)

K Bagrintseva, S Geisenhof, R Kern, S Eichenlaub… - Blood, 2005 - ashpublications.org
FLT3 (fms-like tyrosine kinase 3) is constitutively activated in about 30% of patients with
acute myeloid leukemia (AML) and represents a disease-specific molecular marker …

Discovery of benzimidazole-indazole derivatives as potent FLT3-tyrosine kinase domain mutant kinase inhibitors for acute myeloid leukemia

B Ko, Y Jang, MH Kim, TT Lam, HK Seo… - European Journal of …, 2023 - Elsevier
The FMS-like tyrosine kinase 3 (FLT3) gene encodes a class III receptor tyrosine kinase that
is expressed in hematopoietic stem cells. The mutations of FLT3 gene found in 30% of acute …

CHIR-258: a potent inhibitor of FLT3 kinase in experimental tumor xenograft models of human acute myelogenous leukemia

DE Lopes de Menezes, J Peng, EN Garrett… - Clinical Cancer …, 2005 - AACR
Purpose: Fms-like tyrosine kinase 3 (FLT3) encodes a receptor tyrosine kinase (RTK) for
which activating mutations have been identified in a proportion of acute myelogenous …

The irreversible FLT3 inhibitor FF-10101 is active against a diversity of FLT3 inhibitor resistance mechanisms

TT Ferng, D Terada, M Ando, TC Tarver… - Molecular cancer …, 2022 - AACR
Small-molecule FLT3 inhibitors have recently improved clinical outcomes for patients with
FLT3-mutant acute myeloid leukemia (AML) after many years of development, but resistance …

[HTML][HTML] PLX3397 is an investigational selective FLT3 inhibitor that retains activity against the clinically-relevant FLT3-ITD/F691L “gatekeeper” mutation in vitro

CC Smith, AE Perl, E Lasater, C Zhang, GR Jeschke… - Blood, 2011 - Elsevier
Abstract Abstract 764 Background: Activating mutations in FLT3 are detected in
approximately 30% of adult acute myeloid leukemia (AML) cases, most commonly involving …

Chemical space of FLT3 inhibitors as potential anti-AML drugs

QY Lan, YL Zhi, H Heng, JY Tian… - Recent Patents on …, 2017 - ingentaconnect.com
Background: FLT3 is a member of receptor tyrosine kinase III family, mainly expressed in
hematopoietic cells. The aberrant expression and function of FLT3 are strongly related to …