Glycoconjugation: An approach to cancer therapeutics.

Published on Mar 24, 2020in World journal of clinical oncology
· DOI :10.5306/WJCO.V11.I3.110
Maria I Molejon1
Estimated H-index: 1
(National University of La Pampa),
Gisela Weiz1
Estimated H-index: 1
(National University of La Pampa)
+ 1 AuthorsMaria I. Vaccaro27
Estimated H-index: 27
(UBA: University of Buenos Aires)
Sources
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.
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The synthesis of rhamnosylated compounds has gained great importance since these compounds have potential therapeutic applications. The enzymatic approaches for glycosylation of bioactive molecules have been well developed; however, the enzymatic rhamnosylation has been largely hindered by lacking of the glycosyl donor for rhamnosyltransferases. Here, we employed an α-l-rhamnosidase from Alternaria sp. L1 (RhaL1) to perform one-step rhamnosylation of anticancer drugs, including 2′-deoxy-5-fluoro...
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Cancer is an important global issue with increasing incidence and mortality, placing a substantial burden on the healthcare system. Colorectal cancer is the third most common cancer diagnosed among men and women in US. It is estimated that in 2018 there will be 319,160 new diagnosis and 160,820 deaths related to cancer of the digestive system including both genders in the United States alone. Considering limited success of chemotherapy, radiotherapy, and surgery in treatment of these cancer pati...
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#186Mohsen Naghavi (UW: University of Washington)H-Index: 142
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Glycosylation is the most complex post-translational modification of proteins. Altered glycans on the tumor- and host-cell surface and in the tumor microenvironment have been identified to mediate critical events in cancer pathogenesis and progression. Tumor-associated glycan changes comprise increased branching of N-glycans, higher density of O-glycans, generation of truncated versions of normal counterparts, and generation of unusual forms of terminal structures arising from sialylation and fu...
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