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Copyright ©The Author(s) 2020. Published by Baishideng Publishing Group Inc. All rights reserved.
World J Clin Oncol. Mar 24, 2020; 11(3): 110-120
Published online Mar 24, 2020. doi: 10.5306/wjco.v11.i3.110
Glycoconjugation: An approach to cancer therapeutics
Maria I Molejon, Gisela Weiz, Javier D Breccia, Maria Ines Vaccaro
Maria I Molejon, Gisela Weiz, Javier D Breccia, Institute of Earth and Environmental Sciences from La Pampa (INCITAP), National University of La Pampa, School of Natural Sciences (CONICET-UNLPam), Santa Rosa 6300, La Pampa, Argentina
Maria I Molejon, Maria Ines Vaccaro, Institute of Biochemistry and Molecular Medicine (UBA-CONICET), Department of Pathophysiology, School of Pharmacy and Biochemistry, University of Buenos Aires, Buenos Aires C1113AAD, Argentina
Author contributions: Molejon MI and Weiz W reviewed and searched the literature, wrote the first draft of the manuscript, and prepared the table and the figure; Breccia JD and Vaccaro MI discussed the conclusions, and revised the manuscript, table, and figure; all the authors read and approved the final version of the manuscript.
Supported by the Agencia Nacional de Promoción Científica y Tecnológica, No. ANPCyT-PICT2018-02032 RES-2019-401-APN-DANPCYT#ANPCYT (To Molejon MI), No. ANPCyT-PICT2017-2070 RES-2017-310/18 (To Breccia JD), and No. ANPCyT-PICT2016-2258 RES-2017-285-APN-DANPCYT#MCT; University of Buenos Aires-UBACyT2018, RES(CS) Nº 1041/18 (To Vaccaro MI); the National Scientific and Technical Research Council (CONICET) and the National University of La Pampa. Weiz W is a CONICET postdoctoral fellow.
Conflict-of-interest statement: Authors declare no conflict of interests for this article.
Open-Access: This article is an open-access article that was selected by an in-house editor and fully peer-reviewed by external reviewers. It is distributed in accordance with the Creative Commons Attribution NonCommercial (CC BY-NC 4.0) license, which permits others to distribute, remix, adapt, build upon this work non-commercially, and license their derivative works on different terms, provided the original work is properly cited and the use is non-commercial. See: http://creativecommons.org/licenses/by-nc/4.0/
Corresponding author: Maria Ines Vaccaro, AGAF, PhD, Doctor, Professor, Superior Researcher, Chair Professor, Department of Physiopathology, University of Buenos Aires, Junín 954, Ciudad de Buenos Aires C1113AAD, Argentina. mvaccaro@ffyb.uba.ar
Received: October 22, 2019
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
Processing time: 146 Days and 11.1 Hours
Abstract

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.

Keywords: Glycosylation; Gastrointestinal cancers; Antitumoral agents; Therapeutic strategies; Drug targeting

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.