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Design,Synthesis,and Activity evaluation of a new 5-fluorouracil prodrug containing an Asn-Gly-Arg(NO2)COOCH3 tripeptide
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نویسنده
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luan y. ,jing f. ,zhang j. ,zou m. ,wang x. ,jia y. ,liu n. ,mou j. ,xu w.
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منبع
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protein and peptide letters - 2012 - دوره : 19 - شماره : 10 - صفحه:1122 -1131
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چکیده
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Aminopeptidase n (apn/cd13) of the m1 family is a broad specificity enzyme that is intimately involved in tumor angiogenesis and metastasis. asparagine-glycine-arginine (ngr) is a tumor-homing tripeptide,which can selectively combine with apn/cd13 that is overexpressed on the surface of some tumor cells. various anti-tumor drugs can be conjugated to ngr to improve selectivity,efficacy,and to decrease drug toxicity. in this study,a tripeptide ngr(no2) was synthesized and conjugated with 5-fluorouracil. the anti-tumor activities of this new prodrug were evaluated in vivo. more significant anti-tumor effects were observed over the parent 5-fluorouracil. © 2012 bentham science publishers.
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کلیدواژه
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5-fluorouracil; Aminopeptidase N; Angiogenesis; Antitumor; Metastasis; NGR
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آدرس
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institute of medicinal chemistry,school of pharmaceutical sciences,shandong university,44 west wenhua road,jinan,shandong, China, pharmacy department,affiliated hospital,medical college of qingdao university,16 jiangsu road,qingdao,shandong, China, institute of medicinal chemistry,school of pharmaceutical sciences,shandong university,44 west wenhua road,jinan,shandong, China, institute of medicinal chemistry,school of pharmaceutical sciences,shandong university,44 west wenhua road,jinan,shandong, China, institute of medicinal chemistry,school of pharmaceutical sciences,shandong university,44 west wenhua road,jinan,shandong, China, institute of medicinal chemistry,school of pharmaceutical sciences,shandong university,44 west wenhua road,jinan,shandong, China, institute of medicinal chemistry,school of pharmaceutical sciences,shandong university,44 west wenhua road,jinan,shandong, China, institute of medicinal chemistry,school of pharmaceutical sciences,shandong university,44 west wenhua road,jinan,shandong, China, institute of medicinal chemistry,school of pharmaceutical sciences,shandong university,44 west wenhua road,jinan,shandong, China
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Authors
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