GENERATION OF 5-FLUOROURACIL FROM 5-FLUOROCYTOSINE BY MONOCLONAL-ANTIBODY CYTOSINE DEAMINASE CONJUGATES

被引：79

作者：

SENTER, PD ^{[1
]}

SU, PCD ^{[1
]}

KATSURAGI, T ^{[1
]}

SAKAI, T ^{[1
]}

COSAND, WL ^{[1
]}

HELLSTROM, I ^{[1
]}

HELLSTROM, KE ^{[1
]}

机构：

[1] UNIV OSAKA PREFECTURE,COLL AGR,SAKAI,OSAKA 591,JAPAN

来源：

BIOCONJUGATE CHEMISTRY | 1991年 / 2卷 / 06期

关键词：

D O I：

10.1021/bc00012a012

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Cytosine deaminase (CDase) catalyzes the conversion of cytosine to uracil and is also able to convert the clinically used antifungal agent 5-fluorocytosine (5FC) into the anticancer drug 5-fluorouracil (5FU). The enzyme was purified from bakers' yeast in a six-step procedure. Studies indicated that bakers' yeast CDase had a molecular weight of approximately 32 kDa and was composed of two subunits of equal molecular weights. Monoclonal antibodies were covalently attached to CDase, forming conjugates that could bind to antigens on tumor cell surfaces. The combination of L6-CDase and 5FC was equivalent in cytotoxic activity to 5FU when tested against the H2981 human lung adenocarcinoma cell line (L6 positive, 1F5 negative). 5FC alone was noncytotoxic. The activation of 5FC was immunologically specific since 1F5-CDase did not enhance 5FC activity.

引用

页码：447 / 451

页数：5

共 27 条

[1] A CYTO-TOXIC AGENT CAN BE GENERATED SELECTIVELY AT CANCER SITES [J].