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Development of NGR-based anti-cancer agents for targeted therapeutics and imaging
Rongsheng E Wang1, Youhong Niu, Haifan Wu
1Department of Chemistry, Washington University in St Louis, St Louis, MO 63130, USA.
Abstract:
Besides the common issue of drug-resistance, the conventional approaches for cancer diagnostics and treatment are constantly challenged by poor selectivity and limited access to neoplastic cells, which not only lead to the dose-limiting effect on the tumor region, but also bring side-effects to healthy cells/tissues. In recent years, a novel strategy has arisen to target the vasculature of tumors for drug-delivery and molecular imaging, based on the success of anti-angiogenic therapy. In addition to being easily accessible, the endothelial cells of tumor vasculature are also genetically stable and thus do not develop drug-resistance, making them ideal targets for chemotherapeutics and biomedical imaging. Among various ligands identified so far, the Asn-Gly-Arg (NGR) tripeptide can specifically target the neovasculature via interaction with the aminopeptidase N (APN/CD13) receptor which is highly up-regulated in the membranes of endothelial tumor cells. NGR-directed drug delivery as well as molecular imaging have therefore been undergone development, and appear to be intriguing approaches in current cancer research. Herein we highlight some recent developments of the NGR peptide based cancer therapy including drug-delivery and imaging studies, with future perspectives. Some of these agents have been under clinical trials, indicating promising future for the NGR-based drugs.
Insights
The Asn-Gly-Arg (NGR) tripeptide targets tumor neovasculature, offering a novel approach for cancer diagnostics and treatment. This strategy overcomes drug resistance and improves selectivity, showing promise in clinical trials.
Area of Science:
- Oncology
- Molecular Imaging
- Drug Delivery
Background:
- Conventional cancer therapies face challenges with drug resistance, poor selectivity, and side effects.
- Targeting tumor vasculature offers an alternative strategy for improved drug delivery and molecular imaging.
- Endothelial cells of tumor vasculature are accessible and genetically stable, making them ideal targets.
Purpose of the Study:
- To review recent advancements in NGR peptide-based cancer therapy.
- To highlight NGR-directed drug delivery and molecular imaging approaches.
- To discuss future perspectives for NGR-based cancer treatments.
Main Methods:
- Focus on the Asn-Gly-Arg (NGR) tripeptide as a ligand for tumor neovasculature.
- Exploration of NGR interaction with aminopeptidase N (APN/CD13) receptor on tumor endothelial cells.
- Review of recent drug delivery and molecular imaging studies utilizing NGR.
Main Results:
- NGR specifically targets tumor neovasculature by binding to the APN/CD13 receptor.
- NGR-directed strategies demonstrate potential for enhanced cancer treatment and imaging.
- Several NGR-based agents are currently in clinical trials.
Conclusions:
- NGR-based cancer therapy represents a promising approach to overcome limitations of conventional treatments.
- Targeting tumor vasculature with NGR offers improved selectivity and reduced side effects.
- Ongoing clinical trials suggest a bright future for NGR-based drugs in oncology.
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