pexidartinib-resistant FLT3 mutants

Stable Identifier
R-HSA-9702605
Type
Pathway
Species
Homo sapiens
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Pexidartinib is a type II tyrosine kinase inhibitor that is active against FLT3, including the quizartinib-resistant gatekeeper mutation F691L. Activating mutations at TKD aspartic acid residue 835 are resistant to pexidartinib-mediated inhibition, however (Smith et al, 2015a, b).

Literature References
PubMed ID Title Journal Year
25847190 Characterizing and Overriding the Structural Mechanism of the Quizartinib-Resistant FLT3 "Gatekeeper" F691L Mutation with PLX3397

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

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

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

Leukemia 2015
Participants
Participant Of
Disease
Name Identifier Synonyms
cancer 162 malignant tumor, malignant neoplasm, primary cancer
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