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Plos One : a Novel Synthetic Microtubule Inhibitor, Mpt0B214 Exhibits Antitumor Activity in Human Tumor Cells Through Mitochondria-dependent Intrinsic Pathway, Volume 8

By Villunger, Andreas

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Book Id: WPLBN0003942932
Format Type: PDF eBook :
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Reproduction Date: 2015

Title: Plos One : a Novel Synthetic Microtubule Inhibitor, Mpt0B214 Exhibits Antitumor Activity in Human Tumor Cells Through Mitochondria-dependent Intrinsic Pathway, Volume 8  
Author: Villunger, Andreas
Volume: Volume 8
Language: English
Subject: Journals, Science, Medical Science
Collections: Periodicals: Journal and Magazine Collection (Contemporary)
Historic
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Publisher: Plos

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Villunger, A. (n.d.). Plos One : a Novel Synthetic Microtubule Inhibitor, Mpt0B214 Exhibits Antitumor Activity in Human Tumor Cells Through Mitochondria-dependent Intrinsic Pathway, Volume 8. Retrieved from http://kindle.worldlibrary.net/


Description
Description : Agents that interfere with mitotic progression by disturbing microtubule dynamics are commonly used for cancer treatment. Previously, a series of aroylquinolone regioisomers as novel microtubule inhibitors were discovered. One of these new compounds, MPT0B214 inhibited tubulin polymerization through strongly binding to the tubulin’s colchicine-binding site and had cytotoxic activity in a variety of human tumor cell lines. After treatment with MPT0B214, KB cells were arrested in the G2-M phase before cell death occurred, which were associated with upregulation of cyclin B1, dephosphorylation of Cdc2, phosphorylation of Cdc25C and elevated expression of the mitotic marker MPM-2. Furthermore, the compound induced apoptotic cell death through mitochondria/caspase 9-dependent pathway. Notably, several KB-derived multidrugresistant cancer cell lines were also sensitive to MPT0B214 treatment. These findings showed that MPT0B214 is a potential compound in the treatment of various malignancies.

 

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