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	Design of nonpeptidic topomimetics of antiangiogenic proteins with antitumor activities
	Dings, R. P. M. ; Chen, X. M. ; Hellebrekers, Dmei ; van Eijk, L. I. ; Zhang, Y. ; Hoye, T. R. ; Griffioen, A. W. ; Mayo, K. H. ; Zhang Y(张颖)
	2006
关键词	TEREPHTHALAMIDE DERIVATIVES BETA-SHEET MIMETICS PEPTIDE ANGIOGENESIS ANGINEX CANCER INHIBITOR THERAPY POTENT
英文摘要	The inhibition of angiogenesis is a promising avenue for cancer treatment. Although some angiostatic compounds are in the process of development and testing, these often prove ineffective in vivo or have unwanted side effects. We have designed, synthesized, and evaluated a small library of nonpeptidic, calixarene-based protein surface topomimetics that display chemical substituents to approximate the molecular dimensions and amphipathic features (hydrophobic and positively charged residues) of the antiangiogenic peptide anginex, which, like many antiangiogenic proteins, consists primarily of an antiparallel beta-sheet structure as the functional unit. Two of the topomimetics (0118 and 1097) were potent angiogenesis inhibitors in vitro, as determined by endothelial cell proliferation, migration, and chick embryo chorioallantoic membrane assays. Moreover, both compounds were highly effective at inhibiting tumor angiogenesis and growth in two mouse models (MA148 human ovarian carcinoma and B16 murine melanoma). Our results demonstrate the feasibility of designing nonpeptidic protein surface topomimetics as novel pharmaceutical agents for clinical intervention against cancer through angiostatic or other mechanisms.
语种	英语
内容类型	期刊论文
源URL	[http://dspace.xmu.edu.cn/handle/2288/59336]
专题	材料学院－已发表论文
推荐引用方式 GB/T 7714	Dings, R. P. M.,Chen, X. M.,Hellebrekers, Dmei,et al. Design of nonpeptidic topomimetics of antiangiogenic proteins with antitumor activities[J],2006.
APA	Dings, R. P. M..,Chen, X. M..,Hellebrekers, Dmei.,van Eijk, L. I..,Zhang, Y..,...&张颖.(2006).Design of nonpeptidic topomimetics of antiangiogenic proteins with antitumor activities..
MLA	Dings, R. P. M.,et al."Design of nonpeptidic topomimetics of antiangiogenic proteins with antitumor activities".(2006).

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