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Details on Person FLT mutants bind type I TKIs
Class:Id Reaction:9702508
_displayName FLT mutants bind type I TKIs
_doRelease TRUE
_timestamp 2020-11-06 20:53:26
authored [InstanceEdit:9706566] Rothfels, Karen, 2020-11-06
compartment [Compartment:876] plasma membrane [Compartment:70101] cytosol
created [InstanceEdit:9702511] Rothfels, Karen, 2020-09-30
disease [Disease:1500689] cancer
edited [InstanceEdit:9706566] Rothfels, Karen, 2020-11-06
input [DefinedSet:9695790] type I FLT3-binding TKIs [cytosol] [DefinedSet:9702522] type I TKI sensitive FLT3 mutants [plasma membrane] [Homo sapiens]
isChimeric FALSE
literatureReference [LiteratureReference:9671447] Structural and clinical consequences of activation loop mutations in class III receptor tyrosine kinases [LiteratureReference:9695653] FLT3 Inhibitors in Acute Myeloid Leukemia: Current Status and Future Directions [LiteratureReference:9703031] The importance of FLT3 mutational analysis in acute myeloid leukemia [LiteratureReference:9683353] Targeting FLT3 mutations in AML: review of current knowledge and evidence [LiteratureReference:9699279] FLT3 D835 mutations confer differential resistance to type II FLT3 inhibitors [LiteratureReference:9699248] Crenolanib is a potent inhibitor of FLT3 with activity against resistance-conferring point mutants [LiteratureReference:9691838] Identification of driver and passenger mutations of FLT3 by high-throughput DNA sequence analysis and functional assessment of candidate alleles [LiteratureReference:9699345] Mutations of FLT3/ITD confer resistance to multiple tyrosine kinase inhibitors [LiteratureReference:9699384] The secondary FLT3-ITD F691L mutation induces resistance to AC220 in FLT3-ITD+ AML but retains in vitro sensitivity to PKC412 and Sunitinib [LiteratureReference:9699271] Emergence of polyclonal FLT3 tyrosine kinase domain mutations during sequential therapy with sorafenib and sunitinib in FLT3-ITD-positive acute myeloid leukemia [LiteratureReference:9702890] The effects of lestaurtinib (CEP701) and PKC412 on primary AML blasts: the induction of cytotoxicity varies with dependence on FLT3 signaling in both FLT3-mutated and wild-type cases [LiteratureReference:9699304] FMS-like tyrosine kinase 3-internal tandem duplication tyrosine kinase inhibitors display a nonoverlapping profile of resistance mutations in vitro [LiteratureReference:9699314] Gilteritinib is a clinically active FLT3 inhibitor with broad activity against FLT3 kinase domain mutations [LiteratureReference:9699321] Gilteritinib, a FLT3/AXL inhibitor, shows antileukemic activity in mouse models of FLT3 mutated acute myeloid leukemia [LiteratureReference:9697855] Pim-1 is up-regulated by constitutively activated FLT3 and plays a role in FLT3-mediated cell survival [LiteratureReference:9691830] SU5416 and SU5614 inhibit kinase activity of wild-type and mutant FLT3 receptor tyrosine kinase [LiteratureReference:9697850] Overexpression and constitutive activation of FLT3 induces STAT5 activation in primary acute myeloid leukemia blast cells [LiteratureReference:9702472] KW-2449, a novel multikinase inhibitor, suppresses the growth of leukemia cells with FLT3 mutations or T315I-mutated BCR/ABL translocation [LiteratureReference:9702959] FLT3 kinase inhibitor TTT-3002 overcomes both activating and drug resistance mutations in FLT3 in acute myeloid leukemia [LiteratureReference:9702964] TTT-3002 is a novel FLT3 tyrosine kinase inhibitor with activity against FLT3-associated leukemias in vitro and in vivo [LiteratureReference:9702972] The multitargeted receptor tyrosine kinase inhibitor linifanib (ABT-869) induces apoptosis through an Akt and glycogen synthase kinase 3β-dependent pathway
modified [InstanceEdit:9702648] Rothfels, Karen, 2020-10-01 [InstanceEdit:9702943] Rothfels, Karen, 2020-10-02 [InstanceEdit:9703062] Rothfels, Karen, 2020-10-05 [InstanceEdit:9706570] Rothfels, Karen, 2020-11-06 [InstanceEdit:9830342] Matthews, Lisa, 2023-03-08
name FLT mutants bind type I TKIs
normalReaction
output [Complex:9702642] type I TKI-sensitive FLT3 mutants:type I TKIs [plasma membrane] [Homo sapiens]
releaseDate 2020-12-08
reviewed [InstanceEdit:9706568] Kazi, Julhash U, 2020-11-06
reviewStatus [ReviewStatus:9821382] five stars
species [Species:48887] Homo sapiens
stableIdentifier [StableIdentifier:9702512] R-HSA-9702508.2
summation [Summation:9702922] Type I tyrosine kinase inhibitors bind to the ATP-binding si...
(hasEvent) [Pathway:9702509] FLT3 mutants bind TKIs [Homo sapiens]
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