Combining Neratinib with CDK4/6, mTOR, and MEK Inhibitors in Models of HER2-positive Cancer.
Animals
Antineoplastic Combined Chemotherapy Protocols
/ pharmacology
Apoptosis
Biomarkers, Tumor
/ antagonists & inhibitors
Breast Neoplasms
/ drug therapy
Cell Proliferation
Colorectal Neoplasms
/ drug therapy
Cyclin-Dependent Kinase 4
/ antagonists & inhibitors
Cyclin-Dependent Kinase 6
/ antagonists & inhibitors
Esophageal Neoplasms
/ drug therapy
Everolimus
/ administration & dosage
Female
Gene Expression Regulation, Neoplastic
/ drug effects
Humans
MAP Kinase Kinase 1
/ antagonists & inhibitors
Mice
Mice, Inbred NOD
Mice, Nude
Mice, SCID
Piperazines
/ administration & dosage
Protein Kinase Inhibitors
/ pharmacology
Pyrazoles
/ administration & dosage
Pyridines
/ administration & dosage
Pyridones
/ administration & dosage
Pyrimidines
/ administration & dosage
Pyrimidinones
/ administration & dosage
Quinolines
/ administration & dosage
Receptor, ErbB-2
/ metabolism
TOR Serine-Threonine Kinases
/ antagonists & inhibitors
Tumor Cells, Cultured
Xenograft Model Antitumor Assays
Journal
Clinical cancer research : an official journal of the American Association for Cancer Research
ISSN: 1557-3265
Titre abrégé: Clin Cancer Res
Pays: United States
ID NLM: 9502500
Informations de publication
Date de publication:
15 03 2021
15 03 2021
Historique:
received:
12
08
2020
revised:
16
10
2020
accepted:
23
12
2020
pubmed:
9
1
2021
medline:
8
2
2022
entrez:
8
1
2021
Statut:
ppublish
Résumé
Neratinib is an irreversible, pan-HER tyrosine kinase inhibitor that is FDA approved for HER2-overexpressing/amplified (HER2 Cell viability, colony formation assays, and Western blotting were used to determine the effect of neratinib In HER2 Taken together, our results provide strong preclinical evidence for combining neratinib with CDK4/6, mTOR, and MEK inhibitors for the treatment of HER2
Identifiants
pubmed: 33414137
pii: 1078-0432.CCR-20-3017
doi: 10.1158/1078-0432.CCR-20-3017
pmc: PMC8075007
mid: NIHMS1659035
doi:
Substances chimiques
Biomarkers, Tumor
0
Piperazines
0
Protein Kinase Inhibitors
0
Pyrazoles
0
Pyridines
0
Pyridones
0
Pyrimidines
0
Pyrimidinones
0
Quinolines
0
trametinib
33E86K87QN
Everolimus
9HW64Q8G6G
MTOR protein, human
EC 2.7.1.1
ERBB2 protein, human
EC 2.7.10.1
Receptor, ErbB-2
EC 2.7.10.1
TOR Serine-Threonine Kinases
EC 2.7.11.1
CDK4 protein, human
EC 2.7.11.22
CDK6 protein, human
EC 2.7.11.22
Cyclin-Dependent Kinase 4
EC 2.7.11.22
Cyclin-Dependent Kinase 6
EC 2.7.11.22
MAP Kinase Kinase 1
EC 2.7.12.2
MAP2K1 protein, human
EC 2.7.12.2
palbociclib
G9ZF61LE7G
sapanisertib
JGH0DF1U03
neratinib
JJH94R3PWB
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Langues
eng
Sous-ensembles de citation
IM
Pagination
1681-1694Subventions
Organisme : NCI NIH HHS
ID : P30 CA016672
Pays : United States
Organisme : NCI NIH HHS
ID : U54 CA224065
Pays : United States
Organisme : NCATS NIH HHS
ID : UL1 TR003167
Pays : United States
Informations de copyright
©2021 American Association for Cancer Research.
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