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9674504
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Avipritinib, crenolanib, pazopanib and other type I tyrosine...
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Summation
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Avipritinib, crenolanib, pazopanib and other type I tyrosine kinase inhibitors bind to the active form of the PDGF receptors and prevent their trans-autophosphorylation (reviewed in Roskoski, 2018; Klug et al, 2018; Papadopoulos and Lennartsson, 2016). PDGFRA receptors with mutations that strongly promote the active state, such as mutations in the kinase domain or the gatekeeper mutation T674I tend to be sensitive to type I TKIs. In contrast, the extracellular domain mutation Y288C is resistant to type I TKIs (Ip et al, 2018; reviewed in Roskoski, 2018; Klug et al, 2018).