羧甲基普鲁兰多糖-肽-阿霉素缀合物的构效关系——肽间隔区的系统修饰
Structure-activity relationships of carboxymethylpullulan-peptide-doxorubicin conjugates--systematic modification of peptide spacers.
作者信息
Nogusa H, Yano T, Kashima N, Yamamoto K, Okuno S, Hamana H
机构信息
Drug Delivery System Institute, Ltd., Chiba, Japan.
出版信息
Bioorg Med Chem Lett. 2000 Feb 7;10(3):227-30. doi: 10.1016/s0960-894x(99)00678-2.
Abstract
A series of carboxymethylpullulan (CMPul)-doxorubicin (DXR) conjugates bound by peptide spacers of different compositions and lengths were prepared and evaluated for their in vivo antitumor effects. Systematic study of the peptide spacers indicated that CMPul-DXR conjugates bound via appropriate dipeptide spacers were more potent than DXR.
摘要
制备了一系列通过不同组成和长度的肽间隔基连接的羧甲基普鲁兰多糖（CMPul）-阿霉素（DXR）偶联物，并对其体内抗肿瘤效果进行了评估。对肽间隔基的系统研究表明，通过适当的二肽间隔基连接的CMPul-DXR偶联物比阿霉素更有效。
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