MET activation confers resistance to cetuximab, and prevents HER2 and HER3 upregulation in head and neck cancer.
Animals
Cell Line, Tumor
Cetuximab
/ pharmacokinetics
Drug Resistance, Neoplasm
Enzyme Activation
Gene Expression
Head and Neck Neoplasms
/ drug therapy
Humans
Indoles
/ pharmacology
MAP Kinase Signaling System
Mice
Mice, Inbred NOD
Mice, SCID
Proto-Oncogene Proteins c-met
/ metabolism
Random Allocation
Receptor, ErbB-2
/ antagonists & inhibitors
Receptor, ErbB-3
/ antagonists & inhibitors
Squamous Cell Carcinoma of Head and Neck
/ drug therapy
Sulfones
/ pharmacology
Up-Regulation
Xenograft Model Antitumor Assays
MET
cetuximab
drug resistance
head and neck cancer
signaling
Journal
International journal of cancer
ISSN: 1097-0215
Titre abrégé: Int J Cancer
Pays: United States
ID NLM: 0042124
Informations de publication
Date de publication:
01 08 2019
01 08 2019
Historique:
received:
23
08
2018
revised:
11
12
2018
accepted:
15
01
2019
pubmed:
30
1
2019
medline:
18
12
2019
entrez:
30
1
2019
Statut:
ppublish
Résumé
An understanding of the mechanisms underlying acquired resistance to cetuximab is urgently needed to improve cetuximab efficacy in patients with head and neck squamous cell carcinoma (HNSCC). Here, we present a clinical observation that MET pathway activation constitutes the mechanism of acquired resistance to cetuximab in a patient with HNSCC. Specifically, RNA sequencing and mass spectrometry analysis of cetuximab-sensitive (Cetux
Identifiants
pubmed: 30694565
doi: 10.1002/ijc.32170
pmc: PMC6554031
mid: NIHMS1017191
doi:
Substances chimiques
5-((2,6-dichlorobenzyl)sulfonyl)-3-((3,5-dimethyl-4-((2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl)carbonyl)-1H-pyrrol-2-yl)methylene)-1,3-dihydro-2H-indol-2-one
0
Indoles
0
Sulfones
0
ERBB2 protein, human
EC 2.7.10.1
ERBB3 protein, human
EC 2.7.10.1
MET protein, human
EC 2.7.10.1
Proto-Oncogene Proteins c-met
EC 2.7.10.1
Receptor, ErbB-2
EC 2.7.10.1
Receptor, ErbB-3
EC 2.7.10.1
Cetuximab
PQX0D8J21J
Types de publication
Case Reports
Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Research Support, U.S. Gov't, Non-P.H.S.
Langues
eng
Sous-ensembles de citation
IM
Pagination
748-762Subventions
Organisme : NCI NIH HHS
ID : P30 CA008748
Pays : United States
Informations de copyright
© 2019 UICC.
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