ALK can be bound and inhibited by type I tyrosine kinase inh...

created [InstanceEdit:9702327] Rothfels, Karen, 2020-09-29
dbId 9702326
displayName ALK can be bound and inhibited by type I tyrosine kinase inh...
modified [InstanceEdit:9850795] Rothfels, Karen, 2023-10-12
schemaClass Summation
text ALK can be bound and inhibited by type I tyrosine kinase inhibitors. Type I inhibitors bind in the ATP-binding site of the active conformation and prevent activation of the kinase (reviewed in Klug et al 2018; Roskoski, 2013). Crizotinib was one the first ALK inhibitors to be approved for use in ALK+ cancers (reviewed in Rodig et al, 2010; Ou et al, 2011; Gambacorti et al, 2011). Accumulation of secondary mutations leads to acquired crizotinib resistance and has prompted the development of second-and third generation inhibitors such as ceritinib, alectinib, brigatinib and lorlatinib, among others (Ou et al, 2014; Ou et al, 2016; Shaw et al, 2015; Ceccon et al, 2013; Ceccon et al, 2015; Zhang et al, 2016; Shaw et al, 2014; Recondo et al, 2020; Galkin et al, 2006; reviewed in Della Corte et al, 2018). Resistance to ALK inhibitors has also been reported in the context of bypass tracks including activation of pim1 in neuroblastoma, IL10R-STAT3 in ALCL and EGFR in NSCLC (Trigg et al, 2019, Prokoph et al, 2020, Lin et al, 2017).
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