HER2 Specific Tumor Targeting with Dendrimer Conjugated Anti-HER2 mAb

Abstract

In the present study, we report the synthesis and human growth factor receptor-2 (HER2) specific tumor targeting\nproperties of a dendrimer conjugated to anti-HER2 mAb (monoclonal antibody) conjugate. The polyamidoamine\n(PAMAM) dendrimer generation five (G5) was labeled with alexaFluor 488 and conjugated to anti-HER2 mAb.\nThe binding and internalization of the antibody-conjugated dendrimer to HER2-expressing cells was evaluated\nby flow cytometry and confocal microscopy. Uniquely, the conjugate demonstrated cellular uptake and\ninternalization in HER2-expressing cells as compared to free antibody. The time course of internalization and\nblocking experiments with free antibody suggest that the rapid and efficient cellular internalization of the\ndendrimer−antibody conjugate was achieved without alterations in specificity of targeting. Animal studies\ndemonstrated that the conjugate targets HER2-expressing tumors.