Arginine‐glycine‐aspartic acid (RGD) peptide family is known as the most prominent ligand for extracellular domain of integrin receptors. Specific expression of these receptors in various tissue of human body and tight association of their expression profile with various pathophysiological conditions made these receptors a suitable targeting candidate for several disease diagnosis and treatment as well as regeneration of various organs. For these reasons, various forms of RGD‐based integrins ligands have been greatly used in biomedical studies. Here, we summarized the last decade application progress of RGD for cancer theranostics, control of inflammation, thrombosis inhibition and critically discussed the effect of RGD peptides structure and sequence on the efficacy of gene/drug delivery systems in preclinical studies. Furthermore, we will show recent advances in application of RGD functionalized biomaterials for various tissue regenerations including cornea repair, artificial neovascularization and bone tissue regeneration. Finally, we analyzed clinically translatability of RGD peptides, considering examples of integrin ligands in clinical trials. In conclusion, prospects on using RGD peptide for precise drug delivery and biomaterial engineering are well discussed.

中文翻译：

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基于 RGD 的配体生物医学应用的最新进展：从精确的癌症治疗诊断到生物材料工程：系统评价。

精氨酸-甘氨酸-天冬氨酸 (RGD) 肽家族被认为是整合素受体胞外域最突出的配体。这些受体在人体各种组织中的特异性表达及其表达谱与各种病理生理条件的紧密关联，使这些受体成为多种疾病诊断和治疗以及各种器官再生的合适靶向候选物。由于这些原因，各种形式的基于 RGD 的整合素配体已被大量用于生物医学研究。在这里，我们总结了近十年来 RGD 在癌症治疗诊断、炎症控制、血栓形成抑制方面的应用进展，并在临床前研究中批判性地讨论了 RGD 肽结构和序列对基因/药物递送系统功效的影响。此外，我们将展示 RGD 功能化生物材料在各种组织再生（包括角膜修复、人工新血管形成和骨组织再生）中应用的最新进展。最后，我们考虑了临床试验中整合素配体的例子，分析了 RGD 肽的临床可译性。总之，对使用 RGD 肽进行精确药物递送和生物材料工程的前景进行了很好的讨论。