Cossu Jordan, Thoreau Fabien, Boturyn Didier
University Grenoble Alpes, CNRS, DCM UMR 5250, F-38000 Grenoble, France.
University Poitiers, Inst Chim Milieux & Mat Poitiers IC2MP, UMR CNRS 7285, F-86073 Poitiers, France.
Pharmaceutics. 2023 Feb 4;15(2):525. doi: 10.3390/pharmaceutics15020525.
RGD peptides have received a lot of attention over the two last decades, in particular to improve tumor therapy through the targeting of the αVβ3 integrin receptor. This review focuses on the molecular design of multimeric RGD compounds, as well as the design of suitable linkers for drug delivery. Many examples of RGD-drug conjugates have been developed, and we show the importance of RGD constructs to enhance binding affinity to tumor cells, as well as their drug uptake. Further, we also highlight the use of RGD peptides as theranostic systems, promising tools offering dual modality, such as tumor diagnosis and therapy. In conclusion, we address the challenging issues, as well as ongoing and future development, in comparison with large molecules, such as monoclonal antibodies.
在过去二十年中，RGD肽受到了广泛关注，特别是在通过靶向αVβ3整合素受体改善肿瘤治疗方面。本综述重点关注多聚体RGD化合物的分子设计以及用于药物递送的合适连接子的设计。已经开发了许多RGD-药物偶联物的实例，我们展示了RGD构建体对于增强与肿瘤细胞的结合亲和力及其药物摄取的重要性。此外，我们还强调了RGD肽作为治疗诊断系统的用途，这是一种具有肿瘤诊断和治疗等双重功能的有前景的工具。总之，与大分子如单克隆抗体相比，我们讨论了其中的挑战性问题以及当前和未来的发展情况。
