Integrin Targeting and Beyond: Enhancing Cancer Treatment with Dual-Targeting RGD (Arginine–Glycine–Aspartate) Strategies

Integrins, an important superfamily of cell adhesion receptors, play an essential role in cancer progression, metastasis, and angiogenesis, establishing them as prime targets for both diagnostic and therapeutic applications. Despite their significant potential, integrin-targeted therapies have faced...

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Main Authors: Bojana Bogdanović, Daniel Fagret, Catherine Ghezzi, Christopher Montemagno
Format: Article
Language:English
Published: MDPI AG 2024-11-01
Series:Pharmaceuticals
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Online Access:https://www.mdpi.com/1424-8247/17/11/1556
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author Bojana Bogdanović
Daniel Fagret
Catherine Ghezzi
Christopher Montemagno
author_facet Bojana Bogdanović
Daniel Fagret
Catherine Ghezzi
Christopher Montemagno
author_sort Bojana Bogdanović
collection DOAJ
description Integrins, an important superfamily of cell adhesion receptors, play an essential role in cancer progression, metastasis, and angiogenesis, establishing them as prime targets for both diagnostic and therapeutic applications. Despite their significant potential, integrin-targeted therapies have faced substantial challenges in clinical trials, including variable efficacy and unmet high expectations. Nevertheless, the consistent expression of integrins on tumor and stromal cells underscores their ongoing relevance and potential. Traditional RGD-based imaging and therapeutic agents have faced limitations, such as inconsistent target expression and rapid systemic clearance, which have reduced their effectiveness. To overcome these challenges, recent research has focused on advancing RGD-based strategies and exploring innovative solutions. This review offers a thorough analysis of the latest developments in the RGD–integrin field, with a particular focus on addressing previous limitations. It delves into new dual-targeting approaches and cutting-edge RGD-based agents designed to improve both tumor diagnosis and therapeutic outcomes. By examining these advancements, this review illuminates new pathways for enhancing the specificity and efficacy of integrin-targeted therapies, paving the way for more effective cancer diagnosis and treatment strategies.
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spelling doaj-art-452104bc430f447698ecf1b7a7c970672025-08-20T02:48:07ZengMDPI AGPharmaceuticals1424-82472024-11-011711155610.3390/ph17111556Integrin Targeting and Beyond: Enhancing Cancer Treatment with Dual-Targeting RGD (Arginine–Glycine–Aspartate) StrategiesBojana Bogdanović0Daniel Fagret1Catherine Ghezzi2Christopher Montemagno3INSERM, CHU Grenoble Alpes, Laboratory of Bioclinical Radiopharmaceutics, University Grenoble Alpes, 38000 Grenoble, FranceINSERM, CHU Grenoble Alpes, Laboratory of Bioclinical Radiopharmaceutics, University Grenoble Alpes, 38000 Grenoble, FranceINSERM, CHU Grenoble Alpes, Laboratory of Bioclinical Radiopharmaceutics, University Grenoble Alpes, 38000 Grenoble, FranceBiomedical Department, Centre Scientifique de Monaco, 98000 Monaco, MonacoIntegrins, an important superfamily of cell adhesion receptors, play an essential role in cancer progression, metastasis, and angiogenesis, establishing them as prime targets for both diagnostic and therapeutic applications. Despite their significant potential, integrin-targeted therapies have faced substantial challenges in clinical trials, including variable efficacy and unmet high expectations. Nevertheless, the consistent expression of integrins on tumor and stromal cells underscores their ongoing relevance and potential. Traditional RGD-based imaging and therapeutic agents have faced limitations, such as inconsistent target expression and rapid systemic clearance, which have reduced their effectiveness. To overcome these challenges, recent research has focused on advancing RGD-based strategies and exploring innovative solutions. This review offers a thorough analysis of the latest developments in the RGD–integrin field, with a particular focus on addressing previous limitations. It delves into new dual-targeting approaches and cutting-edge RGD-based agents designed to improve both tumor diagnosis and therapeutic outcomes. By examining these advancements, this review illuminates new pathways for enhancing the specificity and efficacy of integrin-targeted therapies, paving the way for more effective cancer diagnosis and treatment strategies.https://www.mdpi.com/1424-8247/17/11/1556RGD-binding integrinαvβ3dual targetingtheranosticsolid tumorsPET imaging
spellingShingle Bojana Bogdanović
Daniel Fagret
Catherine Ghezzi
Christopher Montemagno
Integrin Targeting and Beyond: Enhancing Cancer Treatment with Dual-Targeting RGD (Arginine–Glycine–Aspartate) Strategies
Pharmaceuticals
RGD-binding integrin
αvβ3
dual targeting
theranostic
solid tumors
PET imaging
title Integrin Targeting and Beyond: Enhancing Cancer Treatment with Dual-Targeting RGD (Arginine–Glycine–Aspartate) Strategies
title_full Integrin Targeting and Beyond: Enhancing Cancer Treatment with Dual-Targeting RGD (Arginine–Glycine–Aspartate) Strategies
title_fullStr Integrin Targeting and Beyond: Enhancing Cancer Treatment with Dual-Targeting RGD (Arginine–Glycine–Aspartate) Strategies
title_full_unstemmed Integrin Targeting and Beyond: Enhancing Cancer Treatment with Dual-Targeting RGD (Arginine–Glycine–Aspartate) Strategies
title_short Integrin Targeting and Beyond: Enhancing Cancer Treatment with Dual-Targeting RGD (Arginine–Glycine–Aspartate) Strategies
title_sort integrin targeting and beyond enhancing cancer treatment with dual targeting rgd arginine glycine aspartate strategies
topic RGD-binding integrin
αvβ3
dual targeting
theranostic
solid tumors
PET imaging
url https://www.mdpi.com/1424-8247/17/11/1556
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