Synthesis and in vitro testing of a pyropheophorbide-a-fullerene hexakis adduct immunoconjugate for photodynamic therapy

Rancan F, Helmreich M, Mölich A, Ermilov E, Jux N, Röder B, Hirsch A, Böhm F (2007)


Publication Type: Journal article, Original article

Publication year: 2007

Journal

Original Authors: Rancan F., Helmreich M., Mölich A., Ermilov E.A., Jux N., Röder B., Hirsch A., Böhm F.

Publisher: American Chemical Society

Book Volume: 18

Pages Range: 1078-1086

Journal Issue: 4

DOI: 10.1021/bc0603337

Abstract

The employment of carriers to enhance drug selectivity is one of the strategies to increase the efficacy and reduce the side effects of antitumor therapy. The concept of a modular carrier system (MCS) was developed to construct a complex drug having a high efficacy and selectivity. An MCS employs diverse units or modules: beside the therapeutic unit, an addressing unit (e.g., an antibody) serves to direct the drug to its target, and a multiplying unit has the role of increasing the number of biological active moieties the system can carry. In this paper, we report on the synthesis of a modular carrier system in which the role of multiplying unit is given to a [5:1]-fullerene hexakis adduct. This fullerene hexaadduct has five malonate spacers which can bind two therapeutic units (the photosensitizer pyropheophorbide-a) each, for a total of ten, and a longer malonate spacer which serves for the conjugation to the addressing unit, the monoclonal antibody rituximab. Confocal microscopy studies using Epstein-Barr virus-transformed B-lymphocytes and Jurkat cells showed that the antibody conjugate conserves the affinity for its receptor (CD20) and its selectivity toward CD20 positive B-lymphocytes. On the contrary, the antibody-free complex did not show any bounding or intracellular uptake. © 2007 American Chemical Society.

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How to cite

APA:

Rancan, F., Helmreich, M., Mölich, A., Ermilov, E., Jux, N., Röder, B.,... Böhm, F. (2007). Synthesis and in vitro testing of a pyropheophorbide-a-fullerene hexakis adduct immunoconjugate for photodynamic therapy. Bioconjugate Chemistry, 18(4), 1078-1086. https://dx.doi.org/10.1021/bc0603337

MLA:

Rancan, Fiorenza, et al. "Synthesis and in vitro testing of a pyropheophorbide-a-fullerene hexakis adduct immunoconjugate for photodynamic therapy." Bioconjugate Chemistry 18.4 (2007): 1078-1086.

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