Abstract
The cytoplasmic 5'-nucleotidase cN-II is involved in the regulation of endogenous pools of nucleosides and nucleotides together with nucleoside kinases and other intracellular enzymes. A series of results from studies on preclinical models and clinical samples constitutes the basis of the hypothesis in which cN-II is a therapeutic target in cancer. Indeed, the inhibition of its enzymatic activity seems interesting both to induce cell death directly and to increase the anticancer activity of cytotoxic agents used in cancer treatment. Here we will review the current knowledge of the enzymatic function of cN-II together with available structural data and the studies on cN-II in cancer cells and in samples from cancer patients. Recent and ongoing research on cN-II inhibitors is expected to confirm the druggability and the relevance of cN-II as a cancer drug target. Preliminary in vitro data and cancer cell models using cN-II inhibitors have already suggested the pivotal role of this enzyme as therapeutic target allowing the improvement of anticancer treatments.
Keywords: Cell models, clinical trials, cN-II, crystallography, enzymatic assay, inhibitor, virtual screening.
Current Medicinal Chemistry
Title:Therapeutic Perspectives for cN-II in Cancer.
Volume: 20 Issue: 34
Author(s): Lars Petter Jordheim and Laurent Chaloin
Affiliation:
Keywords: Cell models, clinical trials, cN-II, crystallography, enzymatic assay, inhibitor, virtual screening.
Abstract: The cytoplasmic 5'-nucleotidase cN-II is involved in the regulation of endogenous pools of nucleosides and nucleotides together with nucleoside kinases and other intracellular enzymes. A series of results from studies on preclinical models and clinical samples constitutes the basis of the hypothesis in which cN-II is a therapeutic target in cancer. Indeed, the inhibition of its enzymatic activity seems interesting both to induce cell death directly and to increase the anticancer activity of cytotoxic agents used in cancer treatment. Here we will review the current knowledge of the enzymatic function of cN-II together with available structural data and the studies on cN-II in cancer cells and in samples from cancer patients. Recent and ongoing research on cN-II inhibitors is expected to confirm the druggability and the relevance of cN-II as a cancer drug target. Preliminary in vitro data and cancer cell models using cN-II inhibitors have already suggested the pivotal role of this enzyme as therapeutic target allowing the improvement of anticancer treatments.
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Cite this article as:
Jordheim Petter Lars and Chaloin Laurent, Therapeutic Perspectives for cN-II in Cancer., Current Medicinal Chemistry 2013; 20 (34) . https://dx.doi.org/10.2174/0929867311320340008
DOI https://dx.doi.org/10.2174/0929867311320340008 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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