改良内皮抑素与眼部新生血管的研究进展(英文)

内皮抑素是一种强有力的内源性血管生成抑制因子。它抑制血管内皮细胞的增生,迁移,且无毒性、无耐药性。内皮抑素在体外不稳定,需长期大剂量用药,如何提高内皮抑素生物活性是当今一个热门话题。内皮抑素可以通过化学共价修饰或基因突变改变其结构,提高其稳定性与抑制新生血管活性。我们旨在探讨改良内皮抑素与眼部新生血管的研究进展,并讨论改良内皮抑素的优越性。研究改良内皮抑素也有助于我们了解内皮抑素作用的分子机制.改良内皮抑素有望作为一种新的血管生成抑制剂应用于临床,从而取代内皮抑素。

Recent advances on the modified endostatin and ocular neovascularization

Endostatin(ES), the C-terminal fragment of collagen XVIII, is a potent angiogenesis inhibitor. At present, there are a large number of research papers on ES. It has already been on clinical stage Ⅱ and been widely used in inhibition of neovascularization(NV). However, how to improve the bioactivity of ES is still a matter of ongoing discussion. The objective of this review is to elucidate the relationship between the modified ES and ocular neovascualrization, and to discuss the superiority based on the structure modification. The structure can be changed either by covalent modification or by genetical mutation. It is proposed that the secondary structral ES enhance the anti-angiogenic activity. Studies on modified ES also shed light on our understanding of the molecular action mechanisms of ES. Modified ES may be exploited as a new angiogenesis inhibitor for therapeutic applica-tions, in substitution of the native ES. Activity