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Title 

Anticancer activity of a novel small molecule tubulin inhibitor STK899704

Authors 

K SakchaisriSun Ok KimJoonsung HwangNak Kyun SoungKyung Ho LeeTae Woong ChoiYongjun LeeChan-Mi ParkN R ThimmegowdaPhil Young LeeB ShwethaG SrinivasraoT T H PhamJae-Hyuk JangH W YumY J SurhK S LeeH ParkSeung Jun KimY T KwonJong Seog AhnBo Yeon Kim

Publisher 

Public Library of Science

Issue Date 

2017

Citation 

Plos One

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 

1932-6203

Link 

http://dx.doi.org/10.1371/journal.pone.0173311

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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