Related Experiment Video
Updated: Aug 16, 2026

Pretargeted Radioimmunotherapy Based on the Inverse Electron Demand Diels-Alder Reaction
Published on: January 29, 2019
Receptor-targeted cancer therapy
1Department of Pathology and Laboratory Medicine, University of Pennsylvania School of Medicine, Philadelphia, PA 19104-6082, USA.
Abstract:
Insight into the molecular mechanisms of malignant transformation is changing the way cancer is being treated. Conventional treatment strategies target the DNA of all dividing cells, resulting in a significantly increased risk of collateral toxicity. In addition, the accumulation of multiple mutations leads to drug resistance in many cancer cells. Targeted strategies have now been developed that specifically disrupt oncogenically active cell surface receptors and endogenous signaling molecules. These agents have a much greater selectivity for tumor tissue and decreased risk of side effects. Increased signaling through ErbB receptors via gene amplification, overexpression, and mutation has been implicated in many human cancers and associated with poor prognosis. Interruption of this process has been shown to cause antitumor effects. Downregulation of the ErbB receptors, HER-2/neu, and later EGFR, with monoclonal antibodies was the first demonstration of targeted therapy. Subsequently, the ErbB tyrosine kinase domain has been successfully targeted with small molecule inhibitors. The development of novel ErbB-directed entities is ongoing, with particular promise being shown by strategies targeting receptor interaction in oligomeric complexes.
Insights
Targeted cancer therapies disrupt oncogenic signaling pathways, offering greater tumor selectivity and fewer side effects than traditional chemotherapy. Research focuses on novel ErbB-directed agents targeting receptor interactions for improved cancer treatment.
Area of Science:
- Molecular oncology and targeted cancer therapy.
- Cell surface receptor signaling pathways.
Background:
- Conventional cancer treatments targeting DNA cause significant toxicity and drug resistance.
- Targeted strategies offer improved selectivity by disrupting oncogenic signaling molecules.
- ErbB receptor signaling is implicated in numerous cancers, correlating with poor prognosis.
Purpose of the Study:
- To review the evolution and promise of ErbB-directed targeted cancer therapies.
- To highlight advancements in targeting receptor tyrosine kinases and their interactions.
Main Methods:
- Review of targeted therapy development, including monoclonal antibodies and small molecule inhibitors.
- Focus on strategies disrupting ErbB receptor signaling pathways (e.g., HER-2/neu, EGFR).
- Exploration of novel approaches targeting receptor oligomeric complexes.
Main Results:
- Monoclonal antibodies targeting ErbB receptors (HER-2/neu, EGFR) demonstrated early success in targeted therapy.
- Small molecule inhibitors targeting the ErbB tyrosine kinase domain are effective.
- Ongoing development shows promise for novel ErbB-directed entities.
Conclusions:
- Targeted therapies, particularly those directed at ErbB receptors, offer improved cancer treatment outcomes.
- Strategies inhibiting receptor interactions within oligomeric complexes represent a promising future direction.
More Related Videos
10:46A Flow Cytometry-Based Cell Surface Protein Binding Assay for Assessing Selectivity and Specificity of an Anticancer Aptamer
Published on: September 13, 2022
09:56A Nonviral Approach to Generate Transient Chimeric Antigen Receptor T Cells Using mRNA for Cancer Immunotherapy
Published on: February 21, 2025
Related Concept Videos
Targeted Cancer Therapies
There are several types of targeted therapies against specific...
Receptor Tyrosine Kinases
Targeted Cancer Therapies
There are several types of targeted therapies against specific...
Treatment Resistent Cancers
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
Tumor Immunotherapy