Recent efforts in the design and synthesis of potential anti-cancer vaccines
based on carbohydrates are outlined, covering literature up to 2012. This approach
capitalises on the fact that cancer cells often display alterations in their glycan repertoire
if compared to normal cells, resulting in the accumulation of new structures, usually
referred as to tumour-associated carbohydrate antigens (TACA). Several preclinical and
clinical studies demonstrate that naturally acquired, passively administered, or actively
induced antibodies against TACAs are able to eliminate circulating tumour cells and
micro-metastases in cancer patients. TACAs can be ideal candidates to elicit an
antitumor immune response, however they are often not immunogenic enough to induce
protection, since many of them are of embryonic origin or expressed in normal tissue,
even if at low levels, and consequently tolerated by the immune system. Approaches
toward breaking self-tolerance in the design of novel glycocnjugates structures, together
with new conjugation methods appeared in the last years will be considered.
Keywords: Glycopeptides, glyconanoparticles, tumour-associated carbohydrate
antigens, glycoconjugates, anti-tumour vaccines.