crenolanib-resistant FLT3 mutants don't bind crenolanib

Stable Identifier
R-HSA-9702583
Type
Reaction [transition]
Species
Homo sapiens
Compartment
Locations in the PathwayBrowser
General
SVG |   | PPTX  | SBGN
Click the image above or here to open this reaction in the Pathway Browser
The layout of this reaction may differ from that in the pathway view due to the constraints in pathway layout

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

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

Leukemia 2019
28851395 Molecular targeting in acute myeloid leukemia

Dubielecka, PM, Lim, SH, Raghunathan, VM

J Transl Med 2017
24227820 Crenolanib is a potent inhibitor of FLT3 with activity against resistance-conferring point mutants

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

Blood 2014
Participants
Participates
Normal reaction
Functional status

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

Status
Disease
Name Identifier Synonyms
cancer DOID:162 malignant tumor, malignant neoplasm, primary cancer
Authored
Reviewed
Created
Cite Us!