Selective Toxicity: The Activities of 4-Quinolones against Eukaryotic DNA Topoisomerases
Selective Toxicity: The Activities of 4-Quinolones against Eukaryotic DNA Topoisomerases
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选择性毒性：4-喹诺酮类药物对真核 DNA 拓扑异构酶的活性
DOI：
10.1007/978-1-4471-3449-7_11
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发表时间：
1990
期刊：
影响因子：
11.2
通讯作者：
P. McGuirk
中科院分区：
文献类型：
--
作者：
T. Gootz;J. Barrett;H. Holden;V. Ray;P. McGuirk
A number of new 4-quinolone antibacterials have been recently introduced for clinical use that have greater potency than the older analogs nalidixic acid and oxolinic acid (Andriole 1988; Bergan 1988). Like nalidixic acid, 4-quinolones are believed to inhibit bacterial growth by binding to the A subunit of DNA gyrase, a type II topoisomerase (Geliert et al. 1977). Since a homologous enzyme exists in the nucleus of eukaryotic cells, studies have been performed to examine the effects of 4-quinolones on this topoisomerase. Quinolones such as ciprofloxacin, norfloxacin, fleroxacin, and ofloxacin have, in general, been found to be only weak inhibitors of the eukaryotic enzyme in in vitro assays that measure the catalytic relaxation, unknotting, and catenation activities of the enzyme (Hussy et al. 1986; Riou et al. 1986). An alternative approach to assessing the effects of test agents on topoisomerases, involves measuring the extent of drug-enhanced DNA cleavage obtained in vitro in the presence of the enzyme. While DNA cleavage assays have been used to measure the effects of anti-tumour agents such as VP-16, VM-26, and ellipticine on eukaryotic topoisomerase II, 4-quinolones have not been extensively examined by this method. We have used four different topoisomerase II assay methods, including a non-radiolabeled DNA cleavage assay, for measuring the effects of some quinolones on purified calf thymus topoisomerase II. An experimental quinolone, CP-67,015, was found to elicit significant levels of DNA cleavage products in the presence of enzyme.
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DOI：
10.1073/pnas.81.5.1361
发表时间：
1984-01-01
期刊：
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA-BIOLOGICAL SCIENCES
影响因子：
--
作者：
NELSON, EM;TEWEY, KM;LIU, LF
通讯作者：
LIU, LF
DOI：
10.1016/s0021-9258(18)90729-5
发表时间：
1984-11
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
G. L. Chen;L. Yang;T. Rowe;B. Halligan;K. M. Tewey;L. Liu
通讯作者：
G. L. Chen;L. Yang;T. Rowe;B. Halligan;K. M. Tewey;L. Liu
影响因子：
56.9
作者：
TEWEY, KM;ROWE, TC;LIU, LF
通讯作者：
LIU, LF
影响因子：
14.9
作者：
LIU, LF;DAVIS, JL;CALENDAR, R
通讯作者：
CALENDAR, R
牛犊胸腺 II 型 DNA 拓扑异构酶的纯化和表征。
DOI：
--
发表时间：
1985
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
Halligan,BD;Edwards,KA;Liu,LF
通讯作者：
Liu,LF