Department of New Drug R&D, Jiangsu Simcere Pharmaceutical R&D Co., Ltd., Jiangsu, China.
Chin Med J (Engl). 2009 Aug 20;122(16):1947-51.
To throw light on the superiority of the anti-angiogenesis activity of endostatin (ES) derivatives by reviewing the recent progress in the field of ES molecular structure modification.
The data used in this article were mainly from PubMed with relevant English articles published from 1971 to May 2008. The search terms were "endostatin" and "angiothesis".
Articles involved in the ES molecular structure modification and the original milestone articles were selected.
A number of ES derivatives were designed and studied to improve its clinical relevance. The modified ES with polyethylene glycol (PEG), low molecular weight heparin (LMWH) and IgG Fc domain extended the circulation half-life. Meanwhile the recombinant ESs showed more potent anti-tumor activity than native ES in mouse xenografts. Mutated ES also changed its anti-angiogenesis activity.
The anti-angiogenesis treatment remains a promising tumor therapeutic strategy. New ES derivatives would be a good choice to meet the future challenge on clinical application of ES.
通过回顾近年来内皮抑素（ES）分子结构修饰领域的研究进展，阐明 ES 衍生物的抗血管生成活性优势。
本文资料主要来源于 PubMed，检索词为“endostatin”和“angiothesis”，检索时间为 1971 年 1 月至 2008 年 5 月，选择与 ES 分子结构修饰相关的研究原著。
选择 ES 分子结构修饰的相关研究和原始里程碑研究。
设计并研究了多种 ES 衍生物以提高其临床相关性。用聚乙二醇（PEG）、低分子量肝素（LMWH）和 IgG Fc 结构域修饰 ES 可延长其循环半衰期。同时，与天然 ES 相比，重组 ES 在小鼠异种移植模型中显示出更强的抗肿瘤活性。突变 ES 也改变了其抗血管生成活性。
抗血管生成治疗仍然是一种很有前途的肿瘤治疗策略。新型 ES 衍生物将是满足 ES 临床应用未来挑战的良好选择。
