Published online Mar 24, 2020. doi: 10.5306/wjco.v11.i3.110
Peer-review started: October 22, 2019
First decision: November 27, 2019
Revised: January 31, 2020
Accepted: February 8, 2020
Article in press: February 8, 2020
Published online: March 24, 2020
Cancer constitutes the second leading cause of death globally and is considered to have been responsible for an estimated 9.6 million fatalities in 2018. Although treatments against gastrointestinal tumors have recently advanced, those interventions can only be applied to a minority of patients at the time of diagnosis. Therefore, new therapeutic options are necessary for advanced stages of the disease. Glycosylation of antitumor agents, has been found to improve pharmacokinetic parameters, reduce side effects, and expand drug half-life in comparison with the parent compounds. In addition, glycosylation of therapeutic agents has been proven to be an effective strategy for their targeting tumor tissue, thereby reducing the doses of the glycodrugs administered to patients. This review focusses on the effect of the targeting properties of glycosylated antitumor agents on gastrointestinal tumors.
Core tip: In nature, glycosylation has proven an effective strategy for expanding the biologic information of biomolecules by adding a new level of structural diversity. The high specificity of the interaction with carbohydrates and the overexpression of carbohydrate receptors in tumoral cells that can be specifically targeted by glycodrugs enable a selective administration of those agents to the tumor tissues. Accordingly, the glycosylation of antitumor agents has been found to improve pharmacokinetic parameters, reduce side effects, expand drug half-life, and reduce the dosage of the consequent glycoderivatives.