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CD44: a validated target for improved delivery of cancer therapeutics
Sukhen C Ghosh1, Sultan Neslihan Alpay, Jim Klostergaard
1The University of Texas, Institute of Molecular Medicine, Health Science Center, Center for Molecular Imaging, 1825 Pressler Street, SRB 330C, Houston, TX 77030, USA.
Introduction:
Advances in cancer therapeutics, namely more effective and less toxic treatments, will occur with targeting strategies that enhance the tumor biodistribution and thwart normal tissue exposure of the drug. This review focuses on cancer drug targeting approaches that exploit the expression of the cell-surface proteoglycan family, CD44, on the tumor cell surface followed by some form of ligand binding and induced CD44 internalization and intracellular drug release: in effect using this as a 'Trojan Horse' to more selectively access tumor cells.
Areas Covered:
This review defines the origins of evidence for a linkage between CD44 expression and malignancy, and invokes contemporary views of the importance of putative CD44(+) cancer stem cells in disease resistance. Although the primary emphasis is on the most advanced and developed paths, those that have either made it to the clinic or are well-poised to get there, a wide scope of additional approaches at various preclinical stages is also briefly reviewed.
Expert Opinion:
The future should see development of drug targeting approaches that exploit CD44 expression on CSCs/TICs, including applications to cytotoxic agents currently in the clinic.
Insights
Targeting cancer stem cells (CSCs) via CD44, a cell-surface proteoglycan, offers a promising strategy for developing more effective and less toxic cancer therapeutics. This approach utilizes CD44 as a
Area of Science:
- Oncology
- Molecular Biology
- Drug Delivery
Background:
- Cancer therapeutics require strategies to improve tumor drug distribution and reduce normal tissue exposure.
- CD44, a cell-surface proteoglycan, is expressed on tumor cells and can be exploited for targeted drug delivery.
- CD44 expression is linked to malignancy and the role of cancer stem cells (CSCs) in therapeutic resistance.
Purpose of the Study:
- To review CD44-targeted cancer drug delivery strategies.
- To explore the use of CD44 as a 'Trojan Horse' for selective tumor cell drug uptake.
- To discuss the clinical and preclinical development of these targeting approaches.
Main Methods:
- Review of evidence linking CD44 expression to malignancy.
- Analysis of contemporary research on CD44(+) cancer stem cells (CSCs) and therapeutic resistance.
- Evaluation of advanced and preclinical CD44-targeting drug delivery strategies.
Main Results:
- CD44 expression on tumor cells provides a target for drug delivery systems.
- Ligand binding to CD44 can induce internalization and intracellular drug release.
- CD44-targeted approaches are advancing towards clinical application.
Conclusions:
- Future cancer therapeutics will likely leverage CD44 targeting on CSCs/TICs.
- Applications include the use of existing cytotoxic agents delivered via CD44-targeted strategies.
- This approach holds potential for more selective and effective cancer treatment.
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