Novel anthracycline-spacer-β-glucuronide, -β-glucoside, and -β-galactoside prodrugs for application in selective chemotherapy

Leenders, Ruben G.G.; Damen, Eric W. P.; Bijsterveld, Edward J. A.; Scheeren, Hans W.; Houba, P. H. J.; Meulen-Muileman, Ida H van der; Boven, Epie; Haisma, Hidde J.

doi:10.1016/s0968-0896(99)00095-4

Cited by 65 publications

(33 citation statements)

References 27 publications

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“…Sugar moieties, such as glucose, galactose, or glucuronic acid, have also been used as ways to improve the aqueous solubility of poorly water-soluble drugs. These prodrugs are bioconverted to their parent drug molecules by ␤-glucosidase, ␤-galactosidase, or ␤-glucuronidase and usually have spacers between the parent drug and the promoiety (Leenders et al, 1999).…”

Section: A Improving Formulation and Administrationmentioning

confidence: 99%

Prodrugs—from Serendipity to Rational Design

2011

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Section: A Improving Formulation and Administrationmentioning

confidence: 99%

Prodrugs—from Serendipity to Rational Design

2011

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“…therapy (Haisma et al, 1992(Haisma et al, , 1994Houba et al, 1996;Bakina et al, 1997;Desbene et al, 1998;Florent et al, 1998;Papot et al, 1998;Leenders et al, 1999) as reviewed extensively (Deonarain and Epenetos, 1994;Dubowchik and Walker, 1999;Huang and Oliff, 2001). These include glucuronidated prodrugs of doxorubicin, daunorubicin, and epirubicin, and these prodrugs have the general structure of anthracycline-spacer-glucuronic acid.…”

Section: Alkaline Phosphatase a Enzymology And Localization Of Alkalmentioning

confidence: 99%

Enzyme-Catalyzed Activation of Anticancer Prodrugs

2004

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“…Doxorubicin was derived from Pharmacia and Upjohn (Woerden, The Netherlands). The prodrug DOX-GA3 was synthesised as described (Leenders et al, 1999).…”

Section: Methodsmentioning

confidence: 99%

A fully human anti-Ep-CAM scFv-beta-glucuronidase fusion protein for selective chemotherapy with a glucuronide prodrug

et al. 2002

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Monoclonal antibodies against tumour-associated antigens could be useful to deliver enzymes selectively to the site of a tumour for activation of a non-toxic prodrug. A completely human fusion protein may be advantageous for repeated administration, as host immune responses may be avoided. We have constructed a fusion protein consisting of a human single chain Fv antibody, C28, against the epithelial cell adhesion molecule and the human enzyme b-glucuronidase. The sequences encoding C28 and human enzyme b-glucuronidase were joined by a sequence encoding a flexible linker, and were preceded by the IgGk signal sequence for secretion of the fusion protein. A CHO cell line was engineered to secrete C28-bglucuronidase fusion protein. Antibody specificity and enzyme activity were retained in the secreted fusion protein that had an apparent molecular mass of 100 kDa under denaturing conditions. The fusion protein was able to convert a non-toxic prodrug of doxorubicin, N-

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Novel anthracycline-spacer-β-glucuronide, -β-glucoside, and -β-galactoside prodrugs for application in selective chemotherapy

Cited by 65 publications

References 27 publications

Prodrugs—from Serendipity to Rational Design

Prodrugs—from Serendipity to Rational Design

Enzyme-Catalyzed Activation of Anticancer Prodrugs

A fully human anti-Ep-CAM scFv-beta-glucuronidase fusion protein for selective chemotherapy with a glucuronide prodrug

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