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Title: Anticancer activity of a novel small molecule tubulin inhibitor STK899704
Authors: Krisada Sakchaisri
Sun Ok Kim
Joonsung Hwang
Nak Kyun Soung
Kyung Ho Lee
Tae Woong Choi
Yongjun Lee
Chan Mi Park
Naraganahalli R. Thimmegowda
Phil Young Lee
Bettaswamigowda Shwetha
Ganipisetti Srinivasrao
Thi Thu Huong Pham
Jae Hyuk Jang
Hye Won Yum
Young Joon Surh
Kyung S. Lee
Hwangseo Park
Seung Jun Kim
Yong Tae Kwon
Jong Seog Ahn
Bo Yeon Kim
Korea Research Institute of Bioscience and Biotechnology
Mahidol University
Hanoi University of Sciences
Seoul National University
National Cancer Institute
Sejong University
Keywords: Agricultural and Biological Sciences;Biochemistry, Genetics and Molecular Biology
Issue Date: 1-Mar-2017
Citation: PLoS ONE. Vol.12, No.3 (2017)
Abstract: We have identified the small molecule STK899704 as a structurally novel tubulin inhibitor. STK899704 suppressed the proliferation of cancer cell lines from various origins with IC50 values ranging from 0.2 to 1.0 μM. STK899704 prevented the polymerization of purified tubulin in vitro and also depolymerized microtubule in cultured cells leading to mitotic arrest, associated with increased Cdc25C phosphorylation and the accumulation of both cyclin B1 and polo-like kinase 1 (Plk1), and apoptosis. Unlike many anticancer drugs such as Taxol and doxorubicin, STK899704 effectively displayed antiproliferative activity against multidrug-resistant cancer cell lines. The proposed binding mode of STK899704 is at the interface between αβ-tubulin heterodimer overlapping with the colchicine-binding site. Our in vivo carcinogenesis model further showed that STK 899704 is potent in both the prevention and regression of tumors, remarkably reducing the number and volume of skin tumor by STK899704 treatment. Moreover, it was significant to note that the efficacy of STK899704 was surprisingly comparable to 5-fluorouracil, a widely used anticancer therapeutic. Thus, our results demonstrate the potential of STK899704 to be developed as an anticancer chemotherapeutic and an alternative candidate for existing therapies.
ISSN: 19326203
Appears in Collections:Scopus 2016-2017

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