Related Experiment Video
Updated: Oct 13, 2025
Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays
Published on: September 19, 2018
The Urokinase Receptor (uPAR) as a "Trojan Horse" in Targeted Cancer Therapy: Challenges and Opportunities
Virginia Metrangolo1,2, Michael Ploug1,2, Lars H Engelholm1,2
1The Finsen Laboratory, Rigshospitalet, DK-2200 Copenhagen, Denmark.
Abstract:
One of the largest challenges to the implementation of precision oncology is identifying and validating selective tumor-driving targets to enhance the therapeutic efficacy while limiting off-target toxicity. In this context, the urokinase-type plasminogen activator receptor (uPAR) has progressively emerged as a promising therapeutic target in the management of aggressive malignancies. By focalizing the plasminogen activation cascade and subsequent extracellular proteolysis on the cell surface of migrating cells, uPAR endows malignant cells with a high proteolytic and migratory potential to dissolve the restraining extracellular matrix (ECM) barriers and metastasize to distant sites. uPAR is also assumed to choreograph multiple other neoplastic stages via a complex molecular interplay with distinct cancer-associated signaling pathways. Accordingly, high uPAR expression is observed in virtually all human cancers and is frequently associated with poor patient prognosis and survival. The promising therapeutic potential unveiled by the pleiotropic nature of this receptor has prompted the development of distinct targeted intervention strategies. The present review will focus on recently emerged cytotoxic approaches emphasizing the novel technologies and related limits hindering their application in the clinical setting. Finally, future research directions and emerging opportunities in the field of uPAR targeting are also discussed.
Insights
Targeting the urokinase-type plasminogen activator receptor (uPAR) offers a promising strategy for precision oncology. This review explores novel cytotoxic approaches targeting uPAR to improve cancer therapy efficacy and reduce toxicity.
Area of Science:
- Molecular oncology
- Cancer biology
- Drug discovery
Background:
- Precision oncology faces challenges in identifying selective tumor targets to balance efficacy and toxicity.
- The urokinase-type plasminogen activator receptor (uPAR) is implicated in aggressive malignancies due to its role in extracellular matrix degradation and metastasis.
- High uPAR expression correlates with poor prognosis across various human cancers.
Purpose of the Study:
- To review recent cytotoxic strategies targeting uPAR in cancer therapy.
- To highlight novel technologies and their limitations for clinical application.
- To discuss future research directions and opportunities in uPAR-targeted interventions.
Main Methods:
- Literature review of emerging cytotoxic approaches targeting uPAR.
- Analysis of novel technologies and their associated clinical limitations.
- Discussion of future research avenues and emerging opportunities.
Main Results:
- uPAR plays a critical role in cancer cell migration, invasion, and metastasis by regulating the plasminogen activation cascade.
- uPAR is involved in multiple cancer signaling pathways, contributing to neoplastic progression.
- Various targeted intervention strategies are being developed to exploit uPAR's therapeutic potential.
Conclusions:
- uPAR represents a significant therapeutic target for aggressive cancers.
- Novel cytotoxic approaches show promise but face technological and clinical hurdles.
- Continued research into uPAR targeting is crucial for advancing precision oncology.
More Related Videos
Related Concept Videos
02:57Targeted Cancer Therapies
There are several types of targeted therapies against...
01:27Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
02:38Mitogens and the Cell Cycle