Bogdanović Bojana, Fagret Daniel, Ghezzi Catherine, Montemagno Christopher
INSERM, CHU Grenoble Alpes, Laboratory of Bioclinical Radiopharmaceutics, University Grenoble Alpes, 38000 Grenoble, France.
Biomedical Department, Centre Scientifique de Monaco, 98000 Monaco, Monaco.
Pharmaceuticals (Basel). 2024 Nov 20;17(11):1556. doi: 10.3390/ph17111556.
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.
整合素是细胞黏附受体的一个重要超家族，在癌症进展、转移和血管生成中发挥着至关重要的作用，使其成为诊断和治疗应用的主要靶点。尽管具有巨大潜力，但整合素靶向疗法在临床试验中面临着重大挑战，包括疗效不一和未满足的高期望。然而，整合素在肿瘤细胞和基质细胞上的持续表达凸显了它们持续的相关性和潜力。传统的基于RGD的成像和治疗剂面临着局限性，如靶点表达不一致和快速的全身清除，这降低了它们的有效性。为了克服这些挑战，最近的研究集中在推进基于RGD的策略和探索创新解决方案。本综述对RGD-整合素领域的最新进展进行了全面分析，特别关注解决以前的局限性。它深入探讨了旨在改善肿瘤诊断和治疗结果的新的双靶向方法和基于RGD的前沿药物。通过研究这些进展，本综述阐明了提高整合素靶向疗法特异性和疗效的新途径，为更有效的癌症诊断和治疗策略铺平了道路。
