ceritinib-resistant ALK mutants don't bind ceritinib

Stable Identifier
R-HSA-9700658
Type
Reaction [transition]
Species
Homo sapiens
Compartment
cytosol, plasma membrane
ReviewStatus
5/5
Locations in the PathwayBrowser
Expand all
General
SVG | 
PNG
Low
Medium
High
 | PPTX  | SBGN
ceritinib-resistant ALK mutants don't bind ceritinib
Click the image above or here to open this reaction in the Pathway Browser
The layout of this reaction may differ from that in the pathway view due to the constraints in pathway layout
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
Participants
Input
Participates
as an event of
Normal reaction
Liganded-ALK dimer binds type I ALK-binding TKIs (Homo sapiens)
Functional status

Loss of function of ceritinib-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  (2020-09-16)
Cite Us!