Enzyme and Proton-Activated Prodrugs for a Selective Cancer Therapy

Authors: Tietze, L. F.; Feuerstein, T.

Source: Current Pharmaceutical Design, Volume 9, Number 26, October 2003 , pp. 2155-2175(21)

Publisher: Bentham Science Publishers

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Abstract:

This review is a survey of two approaches for a selective anticancer therapy that are based on a specific cleavage of specially designed non-toxic prodrugs with the liberation of a cytotoxic compound either by antibody-enzyme conjugates targeted to tumor-associated antigens or by acid-catalyzed hydrolysis of the prodrugs due to the increased concentration of hydronium ions in malignant tissue under hyperglycemic conditions. Herein, the design, synthesis and the biological testing of prodrugs are described.

Keywords: adept; antitumor agents; cancer therapy; enzymes; glycosides; monoclonal antibodies; prodrugs

Document Type: Review article

DOI: http://dx.doi.org/10.2174/1381612033454072

Affiliations: 1: Institute of Organic Chemistry of the Georg-August-University Gottingen, Tammannstrasse 2, 37077 Gottingen, Germany.

Publication date: 2003-10-01

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Current Pharmaceutical Design publishes timely in-depth reviews covering all aspects of current research in rational drug design. Each issue is devoted to a single major therapeutic area. A Guest Editor who is an acknowledged authority in a therapeutic field has solicits for each issue comprehensive and timely reviews from leading researchers in the pharmaceutical industry and academia.

Each thematic issue of Current Pharmaceutical Design covers all subject areas of major importance to modern drug design, including: medicinal chemistry, pharmacology, drug targets and disease mechanism.