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The lectin-directed enzyme activated prodrug therapy (LEAPT) bipartite drug delivery system utilizes glycosylated enzyme, localized according to its sugar pattern, and capped prodrugs released by that enzyme. In this way, the sugar coat of a synthetic enzyme determines the site of release of a given drug. Here, prodrugs of doxorubicin and 5-fluorouracil capped by the nonmammalian l-rhamnosyl sugar unit have been efficiently synthesized and evaluated for use in the LEAPT system. Both are stable in blood, released by synthetically d-galactosylated rhamnosidase enzyme, and do not inhibit the uptake of the synthetic enzyme to its liver target. These results are consistent with their proposed mode of action and efficacy in models of liver cancer, and confirm modular flexibility in the drugs that may be used in LEAPT.

Original publication

DOI

10.3109/1061186X.2010.529909

Type

Journal article

Journal

J Drug Target

Publication Date

12/2010

Volume

18

Pages

794 - 802

Keywords

Animals, Antibiotics, Antineoplastic, Antimetabolites, Antineoplastic, Doxorubicin, Drug Delivery Systems, Fluorouracil, Glycoside Hydrolases, Lectins, Liver, Male, Prodrugs, Rabbits