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[胸苷磷酸化酶(血小板衍生内皮细胞生长因子)对肿瘤血管生成的影响。酶抑制剂的催化活性]

[Influence of the thymidine phosphorylase (platelet-derived endothelial cell growth factor) on tumor angiogenesis. Catalytic activity of enzyme inhibitors].

作者信息

Miszczak-Zaborska Elzbieta, Smolarek Monika, Bartkowiak Jacek

机构信息

Department of Medical Biochemistry, Medical University of Lodz, 6/8 Mazowiecka St., 92-215 Lodz, Poland.

出版信息

Postepy Biochem. 2010;56(1):61-6.

Abstract

Thymidine phosphorylase, also known as platelet-derived endothelial cell growth factor, is a potent angiogenic factor. Thymidine phosphorylase is overexpressed in various human tumors and plays an important role in angiogenesis. A novel inhibitor of thymidine phosphorylase (TP), 5-chloro-6-[1-(2-iminopyrrolidinyl) methyl] uracil hydrochloride (TPI) is about 1000-fold more active than 6-amino-5-chlorouracil, one of the most potent TP inhibitors to 1999 year. Thymidine phosphorylase is also inhibited by 5'-O-trityl-inosine (KIN59) and related compounds, 2-deoxy-L-ribose and glycosides isolated from the bark of Symplocos racemosa.

摘要

胸苷磷酸化酶,也被称为血小板衍生内皮细胞生长因子,是一种强效血管生成因子。胸苷磷酸化酶在多种人类肿瘤中过度表达,并在血管生成中起重要作用。一种新型胸苷磷酸化酶(TP)抑制剂,5-氯-6-[1-(2-亚氨基吡咯烷基)甲基]尿嘧啶盐酸盐(TPI)的活性比6-氨基-5-氯尿嘧啶高约1000倍,6-氨基-5-氯尿嘧啶是1999年最有效的TP抑制剂之一。胸苷磷酸化酶也受到5'-O-三苯甲基肌苷(KIN59)及相关化合物、2-脱氧-L-核糖和从总状山矾树皮中分离出的糖苷的抑制。

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