National University of Singapore, Department of Pharmacy, 18 Science Drive 4, Singapore 117543, Singapore.
Expert Opin Drug Deliv. 2010 Feb;7(2):159-71. doi: 10.1517/17425240903468696.
Recently, there has been substantial progress in the development of integrin targeted pharmaceuticals and drug delivery systems. Integrin is an important member in the cell adhesion molecule family, which is involved in regulation of complex biological conditions, from keeping normal physiological activities to causing cellular dysfunction in diseased cells. Hence, it is timely to summarize the recent developments in integrin targeted drug and gene delivery systems to understand better their advantages and limitations.
In this review, advances in the discovery and clinical trials of these integrin antagonists against different integrin subunits are summarized and discussed. Besides using integrin inhibitor as a single therapeutic agent, integrin antagonists that were conjugated to cytotoxic drugs by synthetic chemistry or coupled to biomacromolecules by either DNA recombination technology or fusion protein technology for integrin targeted therapy have been explored. Furthermore, nanoparticles with integrin targeting ligands for both drug and gene delivery, typically for antiangiogenesis and anticancer therapy, are highlighted and evaluated.
This review sheds light on the future development of integrin targeted drug and/or gene delivery systems.
Although thus far there are still limitations, integrin targeted delivery systems have already shown their potential as important pharmaceuticals in the near future.
最近，整合素靶向药物和药物传递系统的发展取得了实质性进展。整合素是细胞黏附分子家族中的重要成员，参与调节复杂的生物状况，从维持正常生理活动到导致病变细胞的细胞功能障碍。因此，及时总结整合素靶向药物和基因传递系统的最新进展，有助于更好地了解它们的优势和局限性。
在这篇综述中，总结和讨论了针对不同整合素亚基的这些整合素拮抗剂的发现和临床试验进展。除了将整合素抑制剂用作单一治疗剂外，还通过合成化学将整合素拮抗剂与细胞毒性药物偶联，或者通过 DNA 重组技术或融合蛋白技术将其与生物大分子偶联，用于整合素靶向治疗也得到了探索。此外，还强调和评估了用于药物和基因传递的具有整合素靶向配体的纳米颗粒，通常用于抗血管生成和抗癌治疗。
本篇综述阐明了整合素靶向药物和/或基因传递系统的未来发展方向。
尽管到目前为止仍然存在一些限制，但整合素靶向传递系统已经显示出作为未来重要药物的潜力。
