brigatinib-resistant ALK mutants don't bind brigatinib

Stable Identifier
R-HSA-9715356
Type
Reaction [transition]
Species
Homo sapiens
Compartment
cytosol, plasma membrane
ReviewStatus
5/5
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brigatinib-resistant ALK mutants don't bind brigatinib
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The following ALK mutants show resistance to brigatinib:

ALK L1122V: Ceccon et al, 2015
ALK I1171N: Ceccon et al, 2013
ALK 1171S: Amin et al, 2016
ALK I1171T: Katayama et al, 2021 (moderate)
ALK L1196M: Sharma et al, 2019; Ceccon et al, 2015 (moderate)
ALK L1198F: Ceccon et al, 2015
ALK G1202R: Sharma et al, 2019; Gainor et al, 2016
ALK D1203N: Gainor et al, 2016
ALK S1206C: Ceccon et al, 2015
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
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
23239810 Crizotinib-resistant NPM-ALK mutants confer differential sensitivity to unrelated Alk inhibitors

Ceccon, M, Mologni, L, Scapozza, L, Bisson, W, Gambacorti-Passerini, C

Mol. Cancer Res. 2013
31668326 A Compound L1196M/G1202R ALK Mutation in a Patient with ALK-Positive Lung Cancer with Acquired Resistance to Brigatinib Also Confers Primary Resistance to Lorlatinib

Cordani, N, Agustoni, F, Cortinovis, D, Arosio, G, Mologni, L, Sharma, GG, Pagni, F, Bidoli, P, Bisson, WH, Villa, M, Gambacorti-Passerini, C, Piazza, R

J Thorac Oncol 2019
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
Participants
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as an event of
Normal reaction
Liganded-ALK dimer binds type I ALK-binding TKIs (Homo sapiens)
Functional status

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

Normal Entity
Disease Entity
Status
Disease
Name Identifier Synonyms
cancer DOID:162 malignant tumor, malignant neoplasm, primary cancer
Authored
Rothfels, K  (2021-03-22)
Reviewed
Inghirami, G  (2021-05-04)
Created
Rothfels, K  (2021-02-17)
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