quizartinib-resistant FLT3 mutants don't bind quizartinib

Stable Identifier
Reaction [transition]
Homo sapiens
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The following FLT3 mutants are resistant to quizartinib (also known as AC220):
FLT3 A627P (Williams et al, 2013)
FLT3 F691L (Albers et al, 2013; Baker et al, 2013; Galanis et al, 2014; Smith et al, 2015; Williams et al, 2013)
FLT3 Y842C (partial: Williams et al, 2013)
FLT3 Y842H (partial: Albers et al, 2013)
FLT3 N676D (partial: Albers et al, 2013)
FLT3 D835A (Nguyen et al, 2017)
FLT3 D835F (Galanis et al, 2014; Smith et al, 2012; 2013;2015)
FLT3 D835H (Baker et al, 2013; Galanis et al, 2014; Smith et al, 2015)
FLT3 D835V (Galanis et al, 2014; Smith et al, 2012; 2013;2015)
FLT3 D835Y (Galanis et al, 2014; Moore et al, 2012: Nguyen et al, 2017; Smith et al, 2012; 2013;2015)
Literature References
PubMed ID Title Journal Year
28077790 FLT3 activating mutations display differential sensitivity to multiple tyrosine kinase inhibitors

Levis, M, Nguyen, B, Williams, AB, Small, D, Brown, P, Li, L, Young, DJ, Ma, H

Oncotarget 2017
23392356 The secondary FLT3-ITD F691L mutation induces resistance to AC220 in FLT3-ITD+ AML but retains in vitro sensitivity to PKC412 and Sunitinib

Yu, C, Albers, C, Verbeek, M, Duyster, J, Leischner, H, Illert, AL, von Bubnoff, N, Peschel, C

Leukemia 2013
22354205 Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns

Pearson, AD, Avery, S, Workman, P, Faisal, A, Mair, D, Atrash, B, Blagg, J, Bavetsias, V, Linardopoulos, S, Mirabella, F, Valenti, M, Eccles, SA, Moore, AS, de Haven Brandon, A, Sun, C, Swansbury, J, Gonzalez de Castro, D, Raynaud, FI

Leukemia 2012
23969938 Emergence of polyclonal FLT3 tyrosine kinase domain mutations during sequential therapy with sorafenib and sunitinib in FLT3-ITD-positive acute myeloid leukemia

Mullighan, CG, Baker, SD, Rubnitz, JE, Zimmerman, EI, Orwick, S, Inaba, H, Neale, GA, Zatechka, DS, Buaboonnam, J, Enemark, EJ, Shurtleff, S, Wang, YD, Olsen, SR

Clin. Cancer Res. 2013
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
Normal reaction
Functional status

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

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