Endostatin derivative angiogenesis inhibitors.
OBJECTIVE
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.


METHODS
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".


METHODS
Articles involved in the ES molecular structure modification and the original milestone articles were selected.


RESULTS
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.


CONCLUSIONS
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.
Zheng
Meng-jie
MJ
Department of New Drug R&D, Jiangsu Simcere Pharmaceutical R&D Co., Ltd., Jiangsu, China. zhengmengjie@simcere.com
D020533:Angiogenesis Inhibitors / Q000493:pharmacokinetics / Q000627:therapeutic use*; D000818:Animals; D043169:Endostatins / Q000493:pharmacokinetics / Q000627:therapeutic use*; D006801:Humans; D009389:Neovascularization, Pathologic / Q000188:drug therapy
D020533:Angiogenesis Inhibitors; D043169:Endostatins