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Updated: Aug 24, 2026

Testing Targeted Therapies in Cancer using Structural DNA Alteration Analysis and Patient-Derived Xenografts
Published on: July 25, 2020
Novel approaches for targeted cancer therapy
Veronique Guillemard1, H Uri Saragovi
1Departments of Pharmacology and Therapeutics, Oncology, and the Cancer Center, McGill University, Montreal, Quebec, Canada. uri@pharma.mcgill.ca
Abstract:
The clinical use of chemotherapeutic agents against malignant tumors is successful in many cases but suffers from major drawbacks. One drawback is lack of selectivity, which leads to severe side effects and limited efficacy; and another is the emergence/selection of drug-resistance. To limit non-specific toxicity and to improve the efficiency of cancer therapy, "tumor markers", which are proteins generally overexpressed on the surface of tumor cells, can be selectively targeted. Growth factor receptors are one of the most extensively studied tumor markers. The implication of growth factor receptors in the pathogenesis and evolution of cancer has clearly been established and therefore, provides a rationale for therapeutic intervention. The targeting of cytotoxic substances to tumor markers with "magic bullets" is an old idea that raised high expectations but also disappointment. Over the past decade, newly gained understanding of mechanisms for targeted therapy have brought new hopes. Pharmacological agents that selectively target and block the action of growth factors and their receptors have been attempted, such as monoclonal antibodies (mAbs) (whole molecule or fragments), bispecific antibodies, mAbs conjugated to drugs, toxins or radioisotopes, small peptidic and peptidomimetic molecules in free form or conjugated to drugs, anti-sense oligonucleotides, immunoliposomes-encapsulated drugs, and small molecule inhibitors. This review will focus on current developments of selective targeting and bypassing drug resistance in the management of growth factor receptor-overexpressing tumors.
Insights
Targeting tumor markers like growth factor receptors offers a way to improve cancer therapy by reducing side effects and overcoming drug resistance. This review explores advancements in selective targeting strategies for these overexpressed proteins.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Chemotherapy faces challenges like lack of selectivity, leading to severe side effects and drug resistance in cancer treatment.
- Tumor markers, particularly growth factor receptors overexpressed on cancer cells, present viable targets for selective cancer therapy.
- Targeted delivery of cytotoxic agents, an old concept, is being revitalized by new understanding of targeted therapy mechanisms.
Purpose of the Study:
- To review current developments in selective targeting strategies for growth factor receptor-overexpressing tumors.
- To explore methods for overcoming drug resistance in cancer management through targeted approaches.
- To highlight advancements in therapeutic interventions focusing on specific tumor markers.
Main Methods:
- Review of pharmacological agents designed for selective targeting of growth factor receptors.
- Analysis of various therapeutic modalities including monoclonal antibodies, small molecules, and drug conjugates.
- Examination of strategies to bypass or overcome drug resistance in targeted cancer therapy.
Main Results:
- Numerous targeted agents, including monoclonal antibodies and small molecule inhibitors, have been developed to block growth factor receptor action.
- Diverse delivery systems such as immunoliposomes and antibody-drug conjugates enhance targeted delivery and efficacy.
- Emerging strategies show promise in overcoming resistance mechanisms associated with targeted therapies.
Conclusions:
- Selective targeting of growth factor receptors holds significant potential for improving cancer treatment efficacy and reducing toxicity.
- Continued research into novel targeted agents and drug delivery systems is crucial for advancing cancer therapy.
- Bypassing drug resistance through innovative targeting strategies is key to long-term patient benefit in managing receptor-overexpressing tumors.
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