pexidartinib-resistant FLT3 mutants don't bind pexidartinib

Stable Identifier
R-HSA-9702607
Type
Reaction [transition]
Species
Homo sapiens
Compartment
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The following FLT3 mutants are resistant to inhibition by pexidartinib:
FLT3 D835F (Smith et al, 2012; 2013; 2015a, b)
FLT3 D835H (Smith et al, 2012; 2013; 2015a, b)
FLT3 D835V (Smith et al, 2012; 2013; 2015a, b)
FLT3 D835Y (Smith et al, 2012; 2013; 2015a, b)

Literature References
PubMed ID Title Journal Year
23430109 Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD

Salerno, S, Zhu, X, Stewart, WK, Lasater, EA, Damon, LE, Shah, NP, Smith, CC, Lin, KC

Blood 2013
25847190 Characterizing and Overriding the Structural Mechanism of the Quizartinib-Resistant FLT3 "Gatekeeper" F691L Mutation with PLX3397

Habets, G, West, BL, Shah, NP, Smith, CC, Lin, KC, Spevak, W, Zhang, J, Sebra, R, Ibrahim, PN, Massi, E, Shellooe, R, Bashir, A, Powell, B, Zhang, C, Le, MH, Kasarskis, A, Burton, EA, Perl, A, Pendleton, M, Tsang, G, Hsu, HH, Carias, H, Matusow, B, Lasater, EA, Damon, LE, Zhang, Y, Bollag, G

2015
26108694 FLT3 D835 mutations confer differential resistance to type II FLT3 inhibitors

Shah, NP, Stecula, A, Smith, CC, Sali, A, Lin, K

Leukemia 2015
22504184 Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia

Perl, AE, Chin, CS, Schadt, EE, Shah, NP, Smith, CC, Kuriyan, J, Hunt, JP, Wang, Q, Salerno, S, Wang, S, Levis, MJ, Kasarskis, A, Zarrinkar, PP, Travers, KJ, Damon, LE

Nature 2012
Participants
Participates
Normal reaction
Functional status

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

Status
Disease
Name Identifier Synonyms
cancer DOID:162 malignant tumor, malignant neoplasm, primary cancer
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Reviewed
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