Development of cancer vaccines from fully synthetic mucin-based glycopeptide antigens. A vision on mucins from the bioorganic chemistry perspective - Carbohydrate Chemistry: Chemical and Biological Approaches - page 552

Fig. 4 Fully synthetic trivalent constructs 59-62.
mouse sera were shown to react well with the MCF-7 breast cancer
cell line.
3.3.2 Unimolecular pentavalent vaccines. Having demonstrated the
potential to stimulate a multiantigenic immune response, we next
probed further by preparing the rather complex first-generation uni-
molecular pentavalent construct 63, which contains five different
prostate, breast and ovarian cancer-associated carbohydrate antigens,
including Globo-H, Le y , STn, TF and Tn (Fig. 5). Synthesis of this
construct was accomplished according to the cassette method of
glycopeptide assembly, from a relatively small Tn to highly complex
Globo-H antigen in order to increase synthetic eciency. This construct
was next subjected to the preparation of its corresponding KLH conjugate
(64) and Pam 3 Cys conjugate (65) as synthetic vaccines. 35 Preliminary
preclinical studies in mice indicated that the KLH conjugate 64 was
successful in inducing antibodies against all of the carbohydrate anti-
gens, with the exception of Le y . 38 Furthermore, FACS analysis revealed
that these antibodies were highly reactive against three different cell lines
overexpressing the target antigens, providing further support for the
viability of the unimolecular vaccine strategy.