國家衛生研究院 NHRI:Item 3990099045/7541
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    Please use this identifier to cite or link to this item: http://ir.nhri.org.tw/handle/3990099045/7541


    Title: MPT0B169, a new tubulin inhibitor, inhibits cell growth and induces G2/M Arrest in nonresistant and paclitaxel-resistant cancer cells
    Authors: Lee, WH;Liu, HE;Chang, JY;Liou, JP;Huang, HM
    Contributors: National Institute of Cancer Research
    Abstract: The polymerization of tubulin molecules forms microtubules which are considered an attractive target for cancer treatment. Herein, we synthesized a new tubulin inhibitor, MPT0B169 (2-dimethylamino-N-[1-(4-methoxy- benzenesulfonyl)-2, 3-dihydro-1H-indol-7-yl]-acetamide) and demonstrated its action in leukemia cell lines HL60 and NB4 and lymphoma cell line U937. We found that MPT0B169 prevented tubulin assembly by binding the colchicine-binding site of tubulin in vitro. MPT0B169 also induced tubulin depolymerization in vivo. MPT0B169 inhibited the growth of HL60, NB4, and U937 cells in dose- and time-dependent manners. It also inhibited the growth of paclitaxel-resistant cancer cells. In addition, MPT0B169 caused G2/M cell cycle arrest in nonresistant and paclitaxel-resistant cancer cells, with a concomitant increase in cyclin B1 levels and cyclin-dependent kinase 1 (CDK1) phosphorylation. These results suggest that MPT0B169, a tubulin inhibitor, inhibits cell growth and induces G2/M cell cycle arrest of cancer cells through the disruption of tubulin polymerization.
    Date: 2013-09
    Relation: Pharmacology. 2013 Sep;92(1-2):90-98.
    Link to: http://dx.doi.org/10.1159/000351852
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0031-7012&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000324357600014
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84884265374
    Appears in Collections:[Jang-Yang Chang] Periodical Articles

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