Therapeutic Perspectives for cN-II in Cancer.

Lars   Petter   Jordheim; Laurent      Chaloin

doi:10.2174/0929867311320340008

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.

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