The ETS Inhibitors YK-4-279 and TK-216 Are Novel Antilymphoma Agents.
Animals
Antineoplastic Agents
/ pharmacology
Apoptosis
/ drug effects
Biomarkers, Tumor
Cell Line, Tumor
Cell Proliferation
/ drug effects
Disease Models, Animal
Drug Synergism
Gene Expression Profiling
Humans
Immunohistochemistry
Indoles
/ pharmacology
Lymphoma
/ drug therapy
Mice
Prognosis
Protein Binding
Protein Kinase Inhibitors
/ pharmacology
Proto-Oncogene Proteins c-ets
/ analysis
Transcriptome
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 08 2019
15 08 2019
Historique:
received:
20
08
2018
revised:
18
02
2019
accepted:
31
05
2019
pubmed:
12
6
2019
medline:
20
8
2020
entrez:
12
6
2019
Statut:
ppublish
Résumé
Transcription factors are commonly deregulated in cancer, and they have been widely considered as difficult to target due to their nonenzymatic mechanism of action. Altered expression levels of members of the ETS-transcription factors are often observed in many different tumors, including lymphomas. Here, we characterized two small molecules, YK-4-279 and its clinical derivative, TK-216, targeting ETS factors via blocking the protein-protein interaction with RNA helicases, for their antilymphoma activity. The study included preclinical YK-4-279 and TK-216 demonstrated an antitumor activity across several lymphoma cell lines, which we validated The ETS inhibitor YK-4-279 and its clinical derivative TK-216 represent a new class of agents with
Identifiants
pubmed: 31182435
pii: 1078-0432.CCR-18-2718
doi: 10.1158/1078-0432.CCR-18-2718
doi:
Substances chimiques
Antineoplastic Agents
0
Biomarkers, Tumor
0
Indoles
0
Protein Kinase Inhibitors
0
Proto-Oncogene Proteins c-ets
0
YK 4-279
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
5167-5176Informations de copyright
©2019 American Association for Cancer Research.