Internal tandem duplication mutations in the tyrosine kinase domain of FLT3 display a higher oncogenic potential than the activation loop D835Y mutation
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DOI: 10.1007/s00277-018-3245-5
Abstract: Acute myeloid leukemia (AML) remains the most common form of acute leukemia among adults and accounts for a large number of leukemia-related deaths. Mutations in FMS-like tyrosine kinase 3 (FLT3) is one of the most… read more here.
Keywords: kinase domain; flt3; domain; tyrosine kinase ... See more keywords
Pre-transplant FLT3/ITD status predicts outcome in FLT3-mutated acute myeloid leukemia following allogeneic stem cell transplantation
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DOI: 10.1007/s00277-020-04026-1
Abstract: Acute myeloid leukemia (AML) with fetal liver tyrosine kinase 3 (FLT3) internal tandem duplication (ITD) is associated with poor prognosis, and allogeneic stem cell transplantation (Allo-SCT) seems to be the preferred therapeutic approach. However, the… read more here.
Keywords: flt3; transplant; flt3 mrd; transplantation ... See more keywords
Preclinical activity and a pilot phase I study of pacritinib, an oral JAK2/FLT3 inhibitor, and chemotherapy in FLT3-ITD-positive AML
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DOI: 10.1007/s10637-019-00786-4
Abstract: SummaryActivating FLT3 internal tandem duplication (FLT3-ITD) mutations in acute myeloid leukemia (AML) associate with inferior outcomes. We determined that pacritinib, a JAK2/FLT3 inhibitor, has in vitro activity against FLT3-ITD and tyrosine kinase domain (TKD) mutations.… read more here.
Keywords: chemotherapy; inhibitor; flt3; cohort ... See more keywords
Significance of FLT3-tyrosine kinase domain mutation as a prognostic factor for acute myeloid leukemia
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DOI: 10.1007/s12185-019-02720-z
Abstract: The prognostic significance of FLT3-tyrosine kinase domain (TKD) mutations remains unknown. To investigate the prognostic impact of FLT3-TKD, 676 de novo acute myeloid leukemia (AML), we retrospectively analyzed cases and conducted a review of the… read more here.
Keywords: positive cases; flt3; significance flt3; flt3 tkd ... See more keywords
Combined inhibition of PI3Kδ and FLT3 signaling exerts synergistic antitumor activity and overcomes acquired drug resistance in FLT3-activated acute myeloid leukemia.
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DOI: 10.1016/j.canlet.2018.01.071
Abstract: PI3Kδ and FLT3 are frequently activated in acute myeloid leukemia (AML) and have been implicated as potential therapeutic targets. In this report, we demonstrate that combined inhibition of PI3Kδ and FLT3 exerts synergistic antitumor activity… read more here.
Keywords: flt3 activated; pi3k flt3; combined inhibition; flt3 ... See more keywords
Discovery of 4-piperazinyl-2-aminopyrimidine derivatives as dual inhibitors of JAK2 and FLT3.
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DOI: 10.1016/j.ejmech.2019.111590
Abstract: Hybridization strategy is an effective strategy to obtain multi-target inhibitors in drug design. In this study, we assembled the pharmacophores of momelotinib and tandutinib to get a series of 4-piperazinyl-2-aminopyrimidine derivatives. All compounds were tested… read more here.
Keywords: piperazinyl aminopyrimidine; aminopyrimidine derivatives; jak2 flt3; flt3 ... See more keywords
Discovery and development of extreme selective inhibitors of the ITD and D835Y mutant FLT3 kinases.
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DOI: 10.1016/j.ejmech.2019.111710
Abstract: 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 identified a highly selective (phenylethenyl)quinazoline compound family as… read more here.
Keywords: development extreme; discovery development; flt3; extreme selective ... See more keywords
Discovery of novel 4-azaaryl-N-phenylpyrimidin-2-amine derivatives as potent and selective FLT3 inhibitors for acute myeloid leukaemia with FLT3 mutations.
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DOI: 10.1016/j.ejmech.2021.113215
Abstract: Feline McDonough sarcoma (FMS)-like tyrosine kinase 3 (FLT3) is one of the most pursued targets in the treatment of acute myeloid leukaemia (AML) as its gene amplification and mutations, particularly internal tandem duplication (ITD), contribute… read more here.
Keywords: flt3; myeloid leukaemia; azaaryl phenylpyrimidin; acute myeloid ... See more keywords
3002 – REPROGRAMMING OF SERINE METABOLISM IS A METABOLIC VULNERABILITY IN FMS-LIKE TYROSINE KINASE 3 (FLT3) MUTANT ACUTE MYELOID LEUKAEMIA
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DOI: 10.1016/j.exphem.2020.09.024
Abstract: Mutations in the FMS-like tyrosine kinase 3 (FLT3) gene occur in approximately 30% of all acute myeloid leukaemias (AMLs) and are associated with poor prognosis. The clinical utility of FLT3 inhibitor monotherapy has been limited… read more here.
Keywords: synthesis; flt3 mutant; flt3; aml ... See more keywords
Subcellular localization of the FLT3-ITD oncogene plays a significant role in the production of NOX- and p22phox-derived reactive oxygen species in acute myeloid leukemia.
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DOI: 10.1016/j.leukres.2016.11.006
Abstract: Internal tandem duplication of the juxtamembrane domain of FMS-like tyrosine kinase 3 (FLT3-ITD) receptor is the most prevalent FLT3 mutation accounting for 20% of acute myeloid leukemia (AML) patients. FLT3-ITD mutation results in ligand-independent constitutive… read more here.
Keywords: production; p22phox; flt3; acute myeloid ... See more keywords
Discovery of a Potent FLT3 Inhibitor (LT-850-166) with the Capacity of Overcoming a Variety of FLT3 Mutations.
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DOI: 10.1021/acs.jmedchem.1c01196
Abstract: Secondary mutations of FLT3 have become the main mechanism of FLT3 inhibitor resistance that presents a significant clinical challenge. Herein, a series of pyrazole-3-amine derivatives were synthesized and optimized to overcome the common secondary resistance… read more here.
Keywords: flt3 inhibitor; discovery potent; variety; flt3 ... See more keywords