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Updated: Dec 22, 2025

Glycomics-Guided Glycoproteomics Facilitates Comprehensive Profiling of the Glycoproteome in Complex Tumor Microenvironments
Published on: February 7, 2025
Targeting Glycosylation: A New Road for Cancer Drug Discovery
Ana Filipa Costa1, Diana Campos1, Celso A Reis2
1i3S - Instituto de Investigação e Inovação em Saúde, Universidade do Porto, 4200-135 Porto, Portugal; IPATIMUP - Institute of Molecular Pathology and Immunology, University of Porto, 4200-135 Porto, Portugal.
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.
Insights
Alterations in cancer cell glycosylation are key biomarkers. New methods now enable glycan-based drug discovery for effective cancer therapies.
Area of Science:
- Biochemistry
- Oncology
- Glycobiology
Background:
- Aberrant glycosylation is a hallmark of cancer, with cancer-associated glycans serving as crucial biomarkers.
- Despite their therapeutic potential, glycans have been historically underutilized in cancer drug discovery due to complexity and methodological limitations.
Purpose of the Study:
- To highlight the promise of targeting cancer-associated glycosylation for novel drug development.
- To discuss recent advances in methodologies that facilitate glycan-focused cancer research.
Main Methods:
- Review of current understanding of cancer-associated glycosylation.
- Discussion of emerging techniques including glycoengineering and high-throughput screening (HTS).
Main Results:
- Glycosylation alterations are a reliable indicator of cancer.
- Recent technological advancements are overcoming previous barriers in studying glycans.
- Glycan-based targeting presents a promising frontier for cancer therapy.
Conclusions:
- Targeting cancer-associated glycans offers a significant opportunity for developing effective cancer drugs.
- Advancements in glycoengineering and HTS are paving the way for a new era in cancer therapeutics.
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