Targeting Glycosylation: A New Road for Cancer Drug Discovery

Trends Cancer. 2020 Sep;6(9):757-766. doi: 10.1016/j.trecan.2020.04.002. Epub 2020 May 4.

Abstract

Cancer is a deadly disease that encompasses numerous cellular modifications. Among them, alterations in glycosylation are a proven reliable hallmark of cancer, with most biomarkers used in the clinic detecting cancer-associated glycans. Despite their clear potential as therapy targets, glycans have been overlooked in drug discovery strategies. The complexity associated with the glycosylation process, and lack of specific methodologies to study it, have long hampered progress. However, recent advances in new methodologies, such as glycoengineering of cells and high-throughput screening (HTS), have opened new avenues of discovery. We envision that glycan-based targeting has the potential to start a new era of cancer therapy. In this article, we discuss the promise of cancer-associated glycosylation for the discovery of effective cancer drugs.

Keywords: cancer drugs; cancer treatment; glycosylation; high-throughput screening (HTS); target therapy.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Carcinogenesis / drug effects
  • Carcinogenesis / pathology
  • Cell Engineering
  • Cell Line, Tumor
  • Disease Models, Animal
  • Disease Progression
  • Drug Discovery / trends*
  • Drug Screening Assays, Antitumor / methods
  • Drug Screening Assays, Antitumor / trends
  • Glycosylation / drug effects
  • Glycosyltransferases / antagonists & inhibitors*
  • Glycosyltransferases / metabolism
  • High-Throughput Screening Assays
  • Humans
  • Molecular Targeted Therapy / methods
  • Molecular Targeted Therapy / trends
  • Neoplasms / drug therapy*
  • Neoplasms / pathology
  • Polysaccharides / antagonists & inhibitors*
  • Polysaccharides / metabolism

Substances

  • Antineoplastic Agents
  • Polysaccharides
  • Glycosyltransferases