[HTML][HTML] Modulation of FLT3-ITD and CDK9 in acute myeloid leukaemia cells by novel proteolysis targeting chimera (PROTAC)

E Řezníčková, S Krajčovičová, M Peřina… - European Journal of …, 2022 - Elsevier
Oncogenic mutations in gene encoding FLT3 kinase are often detected in acute myeloid
leukaemia (AML) patients, and several potent kinase inhibitors have been developed …

Degrading FLT3-ITD protein by proteolysis targeting chimera (PROTAC)

Y Chen, X Yuan, M Tang, M Shi, T Yang, K Liu… - Bioorganic …, 2022 - Elsevier
Clinical FLT3 mutations caused poor therapeutic benefits toward the present FLT3 inhibitors,
and degradation of the FLT3 mutant protein may be a promising alternative approach to …

Discovery of LWY713 as a potent and selective FLT3 PROTAC degrader with in vivo activity against acute myeloid leukemia

W Liu, Y Bai, L Zhou, J Jin, M Zhang, Y Wang… - European Journal of …, 2024 - Elsevier
Fms-like tyrosine kinase 3 (FLT3) has been validated as a therapeutic target for acute
myeloid leukemia (AML). While a number of FLT3 kinase inhibitors have been approved for …

Development of gilteritinib-based chimeric small molecules that potently induce degradation of FLT3-ITD protein

N Ohoka, M Suzuki, T Uchida, G Tsuji… - ACS Medicinal …, 2022 - ACS Publications
Internal tandem duplication (ITD) in the gene encoding FMS-like tyrosine kinase 3
(FLT3)(FLT3-ITD) is the most frequently observed mutation in acute myeloid leukemia …

Proteolysis-targeting chimera (PROTAC) modification of dovitinib enhances the antiproliferative effect against FLT3-ITD-positive acute myeloid leukemia cells

S Cao, L Ma, Y Liu, M Wei, Y Yao, C Li… - Journal of Medicinal …, 2021 - ACS Publications
Acute myeloid leukemia (AML) refers to one of the most lethal blood malignancies
worldwide. FLT3-ITD mutation is recognized as the most common one that predicted a …

FLT3-selective PROTAC: Enhanced safety and increased synergy with Venetoclax in FLT3-ITD mutated acute myeloid leukemia

Y Tan, L Xin, Q Wang, R Xu, X Tong, G Chen, L Ma… - Cancer letters, 2024 - Elsevier
Acute myeloid leukemia (AML) patients carrying Fms-like tyrosine kinase 3-internal tandem
duplication (FLT3-ITD) mutations often face a poor prognosis. While some FLT3 inhibitors …

Breakdown of the FLT3-ITD/STAT5 axis and synergistic apoptosis induction by the histone deacetylase inhibitor panobinostat and FLT3-specific inhibitors

K Pietschmann, HA Bolck, M Buchwald… - Molecular cancer …, 2012 - AACR
Activating mutations of the class III receptor tyrosine kinase FLT3 are the most frequent
molecular aberration in acute myeloid leukemia (AML). Mutant FLT3 accelerates …

Dual FLT3/TOPK inhibitor with activity against FLT3-ITD secondary mutations potently inhibits acute myeloid leukemia cell lines

N Dayal, C Opoku-Temeng, DE Hernandez… - Future Medicinal …, 2018 - Future Science
Aim: Approximately 30% of acute myeloid leukemia (AML) patients carry FLT3 tyrosine
kinase domain (TKD) mutations or internal tandem duplication (FLT3-ITD). Currently there is …

[HTML][HTML] A dual inhibitor overcomes drug-resistant FLT3-ITD acute myeloid leukemia

P Wang, X Xiao, Y Zhang, B Zhang, D Li, M Liu… - Journal of Hematology & …, 2021 - Springer
FLT3 mutations are the most frequently identified genetic alterations in acute myeloid
leukemia (AML) and are associated with poor prognosis. Multiple FLT3 inhibitors are in …

Antileukemic effects of novel first-and second-generation FLT3 inhibitors: structure-affinity comparison

E Weisberg, J Roesel, P Furet, G Bold… - Genes & …, 2010 - journals.sagepub.com
Constitutively activated mutant FLT3 has emerged as a promising target for therapy for the
subpopulation of acute myeloid leukemia (AML) patients who harbor it. The small molecule …