crenolanib-resistant FLT3 mutants don't bind crenolanib

Stable Identifier
R-HSA-9702583
Type
Reaction [transition]
Species
Homo sapiens
Compartment
plasma membrane
ReviewStatus
5/5
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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
30651634 Targeting FLT3 mutations in AML: review of current knowledge and evidence

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

Leukemia 2019
28851395 Molecular targeting in acute myeloid leukemia

Lim, SH, Dubielecka, PM, Raghunathan, VM

J Transl Med 2017
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
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as an event of
Normal reaction
FLT3 binds type I TKI (Homo sapiens)
Functional status

Loss of function of crenolanib-resistant FLT3 mutants [plasma membrane]

Normal Entity
Disease Entity
Status
Disease
Name Identifier Synonyms
cancer DOID:162 malignant tumor, malignant neoplasm, primary cancer
Cross References
Mondo
Authored
Rothfels, K  (2020-11-06)
Reviewed
Kazi, JU  (2020-11-06)
Created
Rothfels, K  (2020-10-01)
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