Trastuzumab (Herceptin®) is an FDA-approved therapeutic antibody currently employed in the treatment of metastatic stages of breast cancer. Herein, we propose a simple, fast and cost-effective methodology to conjugate trastuzumab with 22-mer 5’ thiol-modified ligonucleotides using a bifunctional crosslinker. The conjugates were successfully characterized by MALDI-ToF MS and SDS-PAGE, obviating the need for enzymatic digestion and difficult chromatographic separations. Furthermore, ELISA was performed to ensure that trastuzumab activity is not affected by oligonucleotide conjugation.
Decoration of trastuzumab with short oligonucleotides: synthesis and detailed characterization / Carvalho, A M; Manicardi, A; Montes, C V; Gunnoo, S B; Schneider, R J; Madder, A. - In: ORGANIC & BIOMOLECULAR CHEMISTRY. - ISSN 1477-0520. - 15:(2017), pp. 8923-8928. [10.1039/c7ob02216f]
Decoration of trastuzumab with short oligonucleotides: synthesis and detailed characterization
Manicardi A;
2017-01-01
Abstract
Trastuzumab (Herceptin®) is an FDA-approved therapeutic antibody currently employed in the treatment of metastatic stages of breast cancer. Herein, we propose a simple, fast and cost-effective methodology to conjugate trastuzumab with 22-mer 5’ thiol-modified ligonucleotides using a bifunctional crosslinker. The conjugates were successfully characterized by MALDI-ToF MS and SDS-PAGE, obviating the need for enzymatic digestion and difficult chromatographic separations. Furthermore, ELISA was performed to ensure that trastuzumab activity is not affected by oligonucleotide conjugation.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
