2022
DOI: 10.1007/s11523-022-00919-5
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Prediction of Resistance Mutations Against Upcoming Anaplastic Lymphoma Kinase Inhibitors

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Cited by 5 publications
(5 citation statements)
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“…In this case, the patient experienced a PR and got a PFS of only 5 months. In previous studies, ALK G1202R has been shown to be resistant to ensartinib in patients with lung cancer ( 12 , 13 ), while I1171N was sensitive to ensartinib in cell lines ( 14 ). Here, we found that co-mutation of ALK I1171N and G1202R was resistant to ensartinib.…”
Section: Discussionmentioning
confidence: 90%
“…In this case, the patient experienced a PR and got a PFS of only 5 months. In previous studies, ALK G1202R has been shown to be resistant to ensartinib in patients with lung cancer ( 12 , 13 ), while I1171N was sensitive to ensartinib in cell lines ( 14 ). Here, we found that co-mutation of ALK I1171N and G1202R was resistant to ensartinib.…”
Section: Discussionmentioning
confidence: 90%
“…FEP has a unique advantage in quantitatively predicting the binding free energies of SMKIs and WT/mutant kinase, and therefore it can help medicinal chemists examine their design ideas before experimental validation. AI predictive methods, together with physics-based modeling and experimental prediction of resistance mutations, can predict the gatekeeper mutations of new drug targets and provide a useful forecast to aid in the discovery of resistance-causing gatekeeper mutations. AI generative models for generating new chemical structures are expected to expand the chemical space and provide new ideas for the design of SMKIs targeting gatekeeper mutations. , By incorporating medicinal chemists’ creativity with these new drug types and intelligent technologies, it is believed that targeting gatekeeper mutations will become a new paradigm in kinase drug development.…”
Section: Discussionmentioning
confidence: 99%
“…In another study, G1202R and I1171N mutants (alectinib-resistant) showed sensitivity to repotrectinib and ensartinib in Ba/F3 cells, respectively. The authors also predicted repotrectinib resistance mutations (G1202R + L1196M, F1174C/L/I, E1129V/K, C1156Y) (Doi et al, 2022).…”
Section: Anaplastic Lymphoma Kinase Inhibitors-resistance Mechanismsmentioning
confidence: 99%
“…Novel ALK TKIs represent a promising perspective regarding the compound mutations. For instance, Doi et al showed that TPX-0131 inhibits mutations composed of G1202R with L1196M, E1129V, and C1156Y (Doi et al, 2022).…”
Section: Anaplastic Lymphoma Kinase Inhibitors-resistance Mechanismsmentioning
confidence: 99%