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Gewählte Publikation:

SHR Neuro Krebs Kardio Lipid

Mayr, C; Wagner, A; Loeffelberger, M; Bruckner, D; Jakab, M; Berr, F; Di Fazio, P; Ocker, M; Neureiter, D; Pichler, M; Kiesslich, T.
The BMI1 inhibitor PTC-209 is a potential compound to halt cellular growth in biliary tract cancer cells.
Oncotarget. 2016; 7(1):745-758 [OPEN ACCESS]
Web of Science PubMed PUBMED Central FullText FullText_MUG


Autor/innen der Med Uni Graz:
Pichler Martin

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Number of Figures: 7
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BMI1 is a core component of the polycomb repressive complex 1 (PRC1) and is up-regulated in biliary tract cancer (BTC), contributing to aggressive clinical features. In this study we investigated the cytotoxic effects of PTC-209, a recently developed inhibitor of BMI1, in BTC cells. PTC-209 reduced overall viability in BTC cell lines in a dose-dependent fashion (0.04 - 20 µM). Treatment with PTC-209 led to slightly enhanced caspase activity and stop of cell proliferation. Cell cycle analysis revealed that PTC-209 caused cell cycle arrest at the G1/S checkpoint. A comprehensive investigation of expression changes of cell cycle-related genes showed that PTC-209 caused significant down-regulation of cell cycle-promoting genes as well as of genes that contribute to DNA synthesis initiation and DNA repair, respectively. This was accompanied by significantly elevated mRNA levels of cell cycle inhibitors. In addition, PTC-209 reduced sphere formation and, in a cell line-dependent manner, aldehyde dehydrogease-1 positive cells. We conclude that PTC-209 might be a promising drug for future in vitro and in vivo studies in BTC.
Find related publications in this database (using NLM MeSH Indexing)
Antineoplastic Agents - pharmacology
Biliary Tract Neoplasms - genetics
Biliary Tract Neoplasms - metabolism
Biliary Tract Neoplasms - pathology
Cell Line, Tumor -
Cell Proliferation - drug effects
Cell Proliferation - genetics
Cell Survival - drug effects
Cell Survival - genetics
Cisplatin - pharmacology
Dose-Response Relationship, Drug -
Drug Synergism -
Flow Cytometry -
G1 Phase Cell Cycle Checkpoints - drug effects
G1 Phase Cell Cycle Checkpoints - genetics
Gene Expression Regulation, Neoplastic - drug effects
Heterocyclic Compounds, 2-Ring - pharmacology
Humans -
Immunohistochemistry -
Neoplastic Stem Cells - drug effects
Neoplastic Stem Cells - metabolism
Polycomb Repressive Complex 1 - antagonists & inhibitors
Polycomb Repressive Complex 1 - genetics
Polycomb Repressive Complex 1 - metabolism
Reverse Transcriptase Polymerase Chain Reaction -
Thiazoles - pharmacology

Find related publications in this database (Keywords)
biliary tract cancer
cell cycle arrest
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