NDLI: Inhibition of acetylpolyamine and spermine oxidases by the polyamine analogue chlorhexidine

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Inhibition of acetylpolyamine and spermine oxidases by the polyamine analogue chlorhexidine

Content Provider	Taylor & Francis Online
Author	Polticelli, Fabio Federico, Rodolfo Angelucci, Emanuela Mariottini, Paolo Cervelli, Manuela Fiorucci, Laura
Abstract	Acetylpolyamine and spermine oxidases are involved in the catabolism of polyamines. The discovery of selective inhibitors of these enzymes represents an important tool for the development of novel anti-neoplastic drugs. Here, a comparative study on acetylpolyamine and spermine oxidases inhibition by the polyamine analogue chlorhexidine is reported. Chlorhexidine is an antiseptic diamide, commonly used as a bactericidal and bacteriostatic agent. Docking simulations indicate that chlorhexidine binding to these enzymes is compatible with the stereochemical properties of both acetylpolyamine oxidase and spermine oxidase active sites. In fact, chlorhexidine is predicted to establish several polar and hydrophobic interactions with the active site residues of both enzymes, with binding energy values ranging from −7.6 to −10.6 kcal/mol. In agreement with this hypothesis, inhibition studies indicate that chlorhexidine behaves as a strong competitive inhibitor of both enzymes, values of Ki being 0.10 μM and 0.55 μM for acetylpolyamine oxidase and spermine oxidase, respectively.
Starting Page	463
Ending Page	467
Page Count	5
File Format	PDF HTM / HTML
ISSN	14756366 14756374
DOI	10.3109/14756366.2011.650691
Journal	Journal of Enzyme Inhibition and Medicinal Chemistry
Volume Number	28
Issue Number	3
Language	English
Publisher	Taylor & Francis
Publisher Date	2013-01-29
Access Restriction	Open
Subject Keyword	Spermine oxidase Acetylspermine oxidase Chlorhexidine Ki
Content Type	Text
Resource Type	Article
Subject	Drug Discovery Medicine Pharmacology

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