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Cancer therapy with iRGD as a tumor-penetrating peptide
Anbazhagan Thirumalai1, Koyeli Girigoswami1, Pragya Pallavi1
1Chettinad Hospital and Research Institute (CHRI), Chettinad Academy of Research and Education (CARE), Medical Bionanotechnology, Faculty of Allied Health Sciences, TN-603103 Kelambakkam, Chennai, India.
Abstract:
One of the primary threats in tumor treatment revolves around the limited ability to penetrate tumor sites, leading to reduced therapeutic effectiveness, which remains a critical concern. Recently gaining importance are novel peptides, namely CRGDK/RGPD/EC (iRGD), that possess enhanced tumor-penetrating and inhibitory properties. These peptides specifically target and penetrate tumors by binding to αvβ integrins, namely αvβ3 and αvβ5, as well as NRP-1 receptors. Remarkably abundant on both the vasculature and tumor cell surfaces, these peptides show promising potential for improving tumor treatment outcomes. As a result, iRGD penetrated deep into the tumor tissues with biological products, contrast agents (imaging agents), antitumor drugs, and immune modulators after co-injecting them with peptides or chemically linked to peptides. The synthesis of iRGD peptides is a relatively straightforward process compared to the synthesis of other traditional peptides, and they significantly improved tumor tissue penetration inhibiting tumor metastasis effectively. Recent studies demonstrate the effectiveness of iRGD-driven dual-targeting chemotherapeutics on cancer cells, and the nanocarriers were modified with iRGD, serving as a favorable delivery strategy of payloads for deeper tumor regions. This review aims to provide an overview to emphasize the recent advancements and advantages of iRGD in treating and imaging various cancers.
Insights
Novel peptides called iRGD (CRGDK/RGPD/EC) enhance tumor penetration for improved cancer treatment and imaging. These peptides target specific receptors, delivering drugs and imaging agents deeper into tumors effectively.
Area of Science:
- Oncology
- Biochemistry
- Nanotechnology
Background:
- Limited tumor penetration reduces therapeutic effectiveness in cancer treatment.
- Novel peptides, including iRGD (CRGDK/RGPD/EC), show enhanced tumor-penetrating and inhibitory properties.
- iRGD peptides target αvβ integrins (αvβ3, αvβ5) and NRP-1 receptors abundant on tumor vasculature and cells.
Purpose of the Study:
- To review recent advancements and advantages of iRGD peptides in cancer treatment and imaging.
- To highlight iRGD's potential in improving drug delivery and therapeutic outcomes.
- To emphasize iRGD's role in enhancing tumor penetration for various cancer therapies.
Main Methods:
- Co-injection or chemical linkage of iRGD peptides with therapeutic agents, imaging agents, or immune modulators.
- Modification of nanocarriers with iRGD for targeted payload delivery.
- Evaluation of iRGD-driven dual-targeting chemotherapeutics for cancer cell treatment.
Main Results:
- iRGD peptides facilitate deep penetration of therapeutic and imaging agents into tumor tissues.
- Simple synthesis of iRGD peptides compared to traditional peptides.
- Significant improvement in tumor tissue penetration and effective inhibition of tumor metastasis.
- Demonstrated effectiveness of iRGD-modified nanocarriers for delivering payloads to deeper tumor regions.
Conclusions:
- iRGD peptides represent a promising strategy for enhancing tumor treatment and imaging.
- Their ability to target specific receptors and improve penetration offers significant advantages over conventional methods.
- Further research into iRGD-driven therapies holds potential for improved cancer patient outcomes.
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