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Title of Journal: Mol Cell Biochem

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Abbravation: Molecular and Cellular Biochemistry

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Springer US

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DOI

10.1016/0375-9474(90)90361-o

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ISSN

1573-4919

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The anticancer drug perillyl alcohol is a Na/KATP

Authors: Diogo G Garcia Lidia M F Amorim Mauro V de Castro Faria Aline S Freire Ricardo E Santelli Clóvis O Da Fonseca Thereza QuiricoSantos Patricia Burth
Publish Date: 2010/08/06
Volume: 345, Issue: 1-2, Pages: 29-34
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Abstract

The monoterpene perillyl alcohol POH is a drug used in the treatment of several malignant tumors including gliomas The present study defines a POH inhibitory effect on Na/KATPase activity from kidney and brain guinea pig extracts and from a human glioblastoma cell line This inhibition showed a high degree of selectivity toward the kidney enzyme expressing as do glioblastoma cells the α1 subunit Kinetic studies with purified enzymes showed a noncompetitive POH inhibition profile to Na+ and K+ and an uncompetitive inhibition towards ATP Furthermore potassium activated pnitrophenylphosfatase activity of these purified preparations was not inhibited by POH suggesting that this drug differently from the classical inhibitor ouabain acted in the initial phase of the enzyme’s catalytic cycle We suggest that POH antitumor action could be linked to its Na/KATPase binding propertiesThis work was supported by grants from Fundação de Amparo a Pesquisa do Estado do Rio de Janeiro FAPERJ Brazil Conselho Nacional de Pesquisas CNPq and Programa de Fomento à Pesquisa na Universidade Federal Fluminense FOPESQUFF The main authors and collaborators declare that have no potential conflicts of interest including patent applications/registrations and grants

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