ceritinib-resistant ALK mutants don't bind ceritinib

Stable Identifier
Reaction [transition]
Homo sapiens
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The following ALK mutants are resistant to inhibition by ceritinib:

ALK L1122V: Ceccon et al, 2015
ALK I1171S: Amin et al, 2016
ALK F1174C: Gainor et al, 2016; Friboulet et al, 2014
ALK F1174L: Gainor et al, 2016; Wang et al, 2017
ALK F1174V: Friboulet et al, 2014
ALK L1196M: Friboulet et al, 2014; Gainor et al, 2016; Ceccon et al, 2015
ALK L1198F: Ceccon et al, 2015
ALK G1202R: Gainor et al, 2016; Friboulet et al, 2014; Lee et al, 2019
ALK D1203N: Wang et al, 2017
ALK S1206C: Ceccon et al, 2015
ALK G1269A: Friboulet et al, 2014

Literature References
PubMed ID Title Journal Year
30683630 Efficacy and Safety of Lorlatinib in Korean Non-Small-Cell Lung Cancer Patients With ALK or ROS1 Rearrangement Whose Disease Failed to Respond to a Previous Tyrosine Kinase Inhibitor

Park, K, Choi, Y, Lee, J, Ahn, MJ, Lee, SH, Ahn, JS, Sun, JM

Clin Lung Cancer 2019
24675041 The ALK inhibitor ceritinib overcomes crizotinib resistance in non-small cell lung cancer

Sun, F, Crystal, AS, Awad, MM, Li, N, Friboulet, L, Michellys, PY, Kasibhatla, S, Lee, CC, Shaw, AT, Li, J, Harris, JL, Engelman, JA, Kim, S, Lockerman, EL, Yanagitani, N, Mahmood, S, Nishio, M, McNamara, P, Pferdekamper, AC, Hua, S, Fujita, N, Gainor, JF, Sun, X, Katayama, R

Cancer Discov 2014
27432227 Molecular Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in ALK-Rearranged Lung Cancer

Mino-Kenudson, M, Friboulet, L, Benes, CH, Engelman, JA, Yoda, S, DiCecca, RH, Digumarthy, S, Le, LP, Ritterhouse, LL, Lennerz, J, Sequist, LV, Muniappan, A, Parks, M, Gainor, JF, Schultz, K, Dardaei, L, Huynh, T, Iafrate, AJ, Keyes, C, Dias-Santagata, D, Heist, RS, Shaw, AT, Singh, M, Logan, J, Dagogo-Jack, I, Leshchiner, I, Channick, C, Lee, D, Chin, E, Lockerman, E, Getz, G, Gadgeel, S, Katayama, R

Cancer Discov 2016
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
25421750 Treatment Efficacy and Resistance Mechanisms Using the Second-Generation ALK Inhibitor AP26113 in Human NPM-ALK-Positive Anaplastic Large Cell Lymphoma

Piazza, R, Ceccon, M, Giudici, G, Mologni, L, Fontana, D, Gambacorti-Passerini, C, Pirola, A

Mol. Cancer Res. 2015
Normal reaction
Functional status

Loss of function of ceritinib-resistant ALK mutants [plasma membrane]

Name Identifier Synonyms
cancer DOID:162 malignant tumor, malignant neoplasm, primary cancer
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