crenolanib-resistant FLT3 mutants don't bind crenolanib

Stable Identifier
R-HSA-9702583
Type
Reaction [transition]
Species
Homo sapiens
Compartment
plasma membrane
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crenolanib-resistant FLT3 mutants don't bind crenolanib
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Crenolanib is a second-generation, type I tyrosine kinase inhibitor with activity against FLT3 (reviewed in Daver et al, 2019; Lim et al, 2017). It is currently in phase III clinical trials for treatment of FLT3-positive AML. The following FLT3 mutants are resistant to crenolanib-mediated inhibition:

FLT3 F691L (Galanis et al, 2014)
FLT3 D835H (Galanis et al, 2014)

Literature References
PubMed ID Title Journal Year
28851395 Molecular targeting in acute myeloid leukemia

Lim, SH, Dubielecka, PM, Raghunathan, VM

J Transl Med 2017
30651634 Targeting FLT3 mutations in AML: review of current knowledge and evidence

Daver, N, Schlenk, RF, Russell, NH, Levis, MJ

Leukemia 2019
24227820 Crenolanib is a potent inhibitor of FLT3 with activity against resistance-conferring point mutants

Galanis, A, Ma, H, Rajkhowa, T, Ramachandran, A, Small, D, Cortes, J, Levis, M

Blood 2014
Participants
Input
Participant Of
hasEvent
Normal reaction
FLT3 binds type I TKI (Homo sapiens)
Disease
Name Identifier Synonyms
cancer 162 malignant tumor, malignant neoplasm, primary cancer
Authored
Rothfels, K  (2020-11-06)
Reviewed
Kazi, JU  (2020-11-06)
Created
Rothfels, K  (2020-10-01)
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