Anticancer activity of a novel small molecule tubulin inhibitor STK899704

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Anticancer activity of a novel small molecule tubulin inhibitor STK899704
K Sakchaisri; Sun Ok Kim; Joonsung HwangNak Kyun SoungKyung Ho Lee; Tae Woong Choi; Yongjun Lee; Chan-Mi Park; N R Thimmegowda; Phil Young Lee; B Shwetha; G Srinivasrao; T T H Pham; Jae-Hyuk Jang; H W Yum; Y J Surh; K S Lee; H Park; Seung Jun Kim; Y T Kwon; Jong Seog Ahn; Bo Yeon Kim
Bibliographic Citation
PLoS One, vol. 12, no. 3, pp. e0173311-e0173311
Publication Year
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.
Public Library of Science
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Ochang Branch Institute > Chemical Biology Research Center > 1. Journal Articles
Critical Diseases Diagnostics Convergence Research Center > 1. Journal Articles
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