Antiproliferative in vitro effects of BI 2536-mediated PLK1 inhibition on cervical adenocarcinoma cells

Antiproliferative in vitro effects of BI 2536-mediated PLK1 inhibition on cervical adenocarcinoma cells

Author Pezuk, Julia A. Google Scholar
Brassesco, Maria Sol Google Scholar
Oliveira, Jaqueline C. Google Scholar
Morales, Andressa G. Google Scholar
Montaldi, Ana P. Google Scholar
Sakamoto-Hojo, Elza T. Google Scholar
Scrideli, Carlos A. Google Scholar
Tone, Luiz G. Google Scholar
Institution Universidade de São Paulo (USP)
Universidade Federal de São Paulo (UNIFESP)
Abstract Cervical adenocarcinoma is one of the most common gynecological malignancies. Despite the improvements in multimodality treatment, advanced disease is still associated with a significantly poor prognosis making the search for more effective therapeutic agents imperative. BI 2536, an unambiguous inhibitor of Polo-like kinase 1 (PLK1), has shown anticancer activity in a variety of tumor cell types. Herein, we present more evidence of the antiproliferative effects of this drug on HeLa cells. Nanomolar concentrations (10-100 nmol/l) of the drug significantly decreased cell proliferation and clonogenic capacity. Our results also demonstrate that inhibition of PLK1 promoted G2/M arrest and resulted in a dramatic increase in the mitotic index after 24 h of treatment. Apoptosis onset was evinced by the accumulation of a sub-G1 population as well as by a significant increase in caspase-3 activity at longer periods of exposure. Taken together, our results reinforce the prospect of directing against PLK1 as a potential therapeutic target to be evaluated in different preclinical models for cervical carcinoma.
Keywords Cervical carcinoma
BI 2536
Mitotic arrest
Language English
Date 2013-02-01
Published in Clinical and Experimental Medicine. New York: Springer, v. 13, n. 1, p. 75-80, 2013.
ISSN 1591-8890 (Sherpa/Romeo, impact factor)
Publisher Springer
Extent 75-80
Access rights Closed access
Type Article
Web of Science ID WOS:000314710800008

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