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Details on Person Type II tyrosine kinase inhibitors bind to a hydrophobic reg...
| Class:Id | Summation:9702929 |
|---|---|
| _displayName | Type II tyrosine kinase inhibitors bind to a hydrophobic reg... |
| _timestamp | 2020-10-07 18:27:57 |
| created | [InstanceEdit:9702924] Rothfels, Karen, 2020-10-02 |
| modified | [InstanceEdit:9703028] Rothfels, Karen, 2020-10-03 [InstanceEdit:9703070] Rothfels, Karen, 2020-10-05 [InstanceEdit:9703715] Rothfels, Karen, 2020-10-06 [InstanceEdit:9704328] Rothfels, Karen, 2020-10-07 |
| text | Type II tyrosine kinase inhibitors bind to a hydrophobic region adjacent to the ATP-binding site that is only present in the inactive conformation of the receptor. As a consequence, type II inhibitors tend to be more effective against FLT3 with ITD than against FLT3 with activating mutations in the tyrosine kinase domain (reviewed in Klug et al, 2018; Larrosa-Garcia and Baer, 2017; Patnaik, 2018; Daver et al, 2019). The following FLT3 mutants are sensitive to these type II tyrosine kinase inhibitors: ponatinib: FLT3 D835G (Nguyen et al, 2017) FLT3 D835N (Nguyen et al, 2017) FLT3 Y591_V592insVDFREYEYDH (Nguyen et al, 2017) quizartinib: FLT3 E598_Y599insFDFREYE (Moore et al, 2012) FLT3 L610_E611insLKWEFPRENL (Peschel et al, 2017) FLT3 Y591_V592insVDFREYEYDH (Peschel et al, 2017) FLT3 F621L (Williams et al, 2013) FLT3 D835G (Nguyen et al, 2017) FLT3 D835H (Galanis et al, 2014) FLT3 D835N (Galanis et al, 2014; Nguyen et al, 2017) sorafenib: FLT3 N676D (Albers et al, 2013) FLT3 E598_Y599insFDFREYE (Moore et al, 2012) FLT3 D835G (Nguyen et al, 2017) FLT3 D835N (Nguyen et al, 2017) pexidartinib: FLT3 F691L (Smith et al, 2015) tandutinib: FLT3 D835A (Clark et al, 2004) FLT3 D835E (Clark et al, 2004) FLT3 D835H (Clark et al, 2004) FLT3 D835N (Clark et al, 2004) FLT3 I836del (Clark et al, 2004) FLT3 E598_Y599insFDFREYE (Kelly et al, 2002; Moore et al, 2012) carbozantinib: FLT3 L610_E611insLKWEFPRENL (Ko et al, 2019) sunitinib: FLT3 F663Q (Schittenhlem et al, 2006) FLT3 F691L (Albers et al, 2013) FLT3 Y842H (Albers et al, 2013) FLT3 N676D (Albers et al, 2013) FLT3 D835G (Nguyen et al, 2017) FLT3 D835N (Nguyen et al, 2017) FLT3 Y591_V592insVDFREYEYDH (Schittenhelm et al, 2006) |
| (summation) | [Reaction:9702510] FLT mutants bind type II TKIs [Homo sapiens] |
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