ASP-3026-resistant ALK mutants

Stable Identifier
Homo sapiens
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ASP3026 is a second generation tyrosine kinase inhibitor with activity against ALK fusions in non-small cell lung cancers (NSCLC) and anaplastic large cell lymphomas (ALCLs). This pathway describes ALK mutants that are resistant to inhibition by ASP3026 (Amin et al, 2016; Katayama et al, 2014; George et al, 2008; Mori et al, 2014; reviewed Roskoski, 2013; Lovly and Pao, 2012)
Literature References
PubMed ID Title Journal Year
25228534 Two novel ALK mutations mediate acquired resistance to the next-generation ALK inhibitor alectinib

Okuno, Y, Iafrate, AJ, Friboulet, L, Koike, S, Shaw, AT, Engelman, JA, Khan, TM, Lockerman, EL, Takeuchi, K, Taiji, M, Fujita, N, Gainor, JF, Katayama, R

Clin Cancer Res 2014
18923525 Activating mutations in ALK provide a therapeutic target in neuroblastoma

Zozulya, S, George, RE, Gilliland, DG, Morris, SW, Luther, W, London, WB, Hanna, M, Meyerson, M, McGrady, P, Sanda, T, Gregor, VE, Look, AT, Zhang, J, Fröhling, S, Ahn, Y, Diller, L, Webb, TR, Zhou, W, Greulich, H, Gray, NS, Xue, L

Nature 2008
27009859 TKI sensitivity patterns of novel kinase-domain mutations suggest therapeutic opportunities for patients with resistant ALK+ tumors

Gokhale, V, Groysman, MJ, Pongtornpipat, P, Wang, M, Tapia, EO, Rajan, SS, Amin, AD, Schatz, JH, Li, L

Oncotarget 2016
22323827 Escaping ALK inhibition: mechanisms of and strategies to overcome resistance

Lovly, CM, Pao, W

Sci Transl Med 2012
23201355 Anaplastic lymphoma kinase (ALK): structure, oncogenic activation, and pharmacological inhibition

Roskoski, R

Pharmacol. Res. 2013
24419060 The selective anaplastic lymphoma receptor tyrosine kinase inhibitor ASP3026 induces tumor regression and prolongs survival in non-small cell lung cancer model mice

Soga, T, Kondoh, Y, Furutani, T, Shindou, N, Konagai, S, Ueno, Y, Sakagami, H, Kuromitsu, S, Mori, M, Kudoh, M, Saito, R, Doihara, H, Shimada, I, Fushiki, H, Mori, K

Mol Cancer Ther 2014
Name Identifier Synonyms
cancer DOID:162 malignant tumor, malignant neoplasm, primary cancer
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