Mechanism of action of the des-F(6) quinolone BMS-284756 measured by supercoiling inhibition and cleavable complex assays

被引:14
作者
Wu, P [1 ]
Lawrence, LE [1 ]
Denbleyker, KL [1 ]
Barrett, JF [1 ]
机构
[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Wallingford, CT 06492 USA
关键词
D O I
10.1128/AAC.45.12.3660-3662.2001
中图分类号
Q93 [微生物学];
学科分类号
071005 [微生物学]; 100705 [微生物与生化药学];
摘要
BMS-284756 (T-3811ME), a novel des-F(6) quinolone, was tested in the supercoiling inhibition and cleavable complex assays against Escherichia coli DNA gyrase, a target of quinolones. The results suggest that BMS-284756 has the same mechanism of action against DNA gyrase as other quinolones and a similar level of potency.
引用
收藏
页码:3660 / 3662
页数:3
相关论文
共 13 条
[1]
TESTING POTENTIAL GYRASE INHIBITORS OF BACTERIAL-DNA GYRASE - A COMPARISON OF THE SUPERCOILING INHIBITION ASSAY AND CLEAVABLE COMPLEX ASSAY [J].
BARRETT, JF ;
BERNSTEIN, JI ;
KRAUSE, HM ;
HILLIARD, JJ ;
OHEMENG, KA .
ANALYTICAL BIOCHEMISTRY, 1993, 214 (01) :313-317
[2]
Bates A. D., 1993, DNA topology
[3]
DNA gyrase, topoisomerase IV, and the 4-quinolones [J].
Drlica, K ;
Zhao, XL .
MICROBIOLOGY AND MOLECULAR BIOLOGY REVIEWS, 1997, 61 (03) :377-+
[4]
Antibacterial spectrum of a novel des-fluoro(6) quinolone, BMS-284756 [J].
Fung-Tomc, JC ;
Minassian, B ;
Kolek, B ;
Huczko, E ;
Aleksunes, L ;
Stickle, T ;
Washo, T ;
Gradelski, E ;
Valera, L ;
Bonner, DP .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2000, 44 (12) :3351-3356
[5]
Selection and genetic characterization of Streptococcus pneumoniae mutants resistant to the des-F(6) quinolone BMS-284756 [J].
Hartman-Neumann, S ;
DenBleyker, K ;
Pelosi, LA ;
Lawrence, LE ;
Barrett, JF ;
Dougherty, TJ .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2001, 45 (10) :2865-2870
[6]
Mechanisms of fluoroquinolone resistance [J].
Hooper, DC .
DRUG RESISTANCE UPDATES, 1999, 2 (01) :38-55
[7]
SIGNIFICANCE OF THE METHYL-GROUP ON THE OXAZINE RING OF OFLOXACIN DERIVATIVES IN THE INHIBITION OF BACTERIAL AND MAMMALIAN TYPE-II TOPOISOMERASES [J].
HOSHINO, K ;
SATO, K ;
AKAHANE, K ;
YOSHIDA, A ;
HAYAKAWA, I ;
SATO, M ;
UNE, T ;
OSADA, Y .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1991, 35 (02) :309-312
[8]
The inhibition and selectivity of bacterial topoisomerases by BMS-284756 and its analogues [J].
Lawrence, LE ;
Wu, P ;
Fan, L ;
Gouveia, KE ;
Card, A ;
Casperson, M ;
Denbleyker, K ;
Barrett, JF .
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, 2001, 48 (02) :195-201
[9]
DNA GYRASE - STRUCTURE AND FUNCTION [J].
REECE, RJ ;
MAXWELL, A .
CRITICAL REVIEWS IN BIOCHEMISTRY AND MOLECULAR BIOLOGY, 1991, 26 (3-4) :335-375
[10]
DNA cleavage activities of Staphylococcus aureus gyrase and topoisomerase IV stimulated by quinolones and 2-pyridones [J].
Saiki, AYC ;
Shen, LL ;
Chen, CM ;
Baranowski, J ;
Lerner, CG .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1999, 43 (07) :1574-1577