Advances in MRSA drug discovery: where are we and where do we need to be?
Advances in MRSA drug discovery: where are we and where do we need to be?
复制标题
DOI：
10.1517/17460441.2013.807246
复制
发表时间：
2013-09
影响因子：
6.3
通讯作者：
Mitachi K
中科院分区：
文献类型：
--
作者：
Kurosu M;Siricilla S;Mitachi K
由于老年人和免疫功能低下患者的稳步增长以及多重耐药（MDR）菌株的出现，在过去十年中，耐甲氧西林金黄色葡萄球菌（MRSA）呈上升趋势。虽然只有有限数量的抗MRSA药物可用，但许多不同的联合抗微生物药物方案已用于治疗严重的MRSA感染。因此，在临床实践中增加几种新的抗葡萄球菌药物应拓宽治疗选择。由于MRSA是与抗菌素耐药性增加相关的最常见和最有问题的细菌之一，因此需要不断努力发现先导化合物以及开发替代疗法和更快的诊断方法，以确保有效的抗葡萄球菌治疗。本文总结了FDA批准的治疗MRSA感染的药物，临床试验中的药物，以及MRSA和相关革兰氏阳性菌感染的药物线索。此外，还简要讨论了抗葡萄球菌分子的作用方式和某些分子的耐药机制。目前正在进行临床试验的管道药物的数量并不特别令人鼓舞。对于重症患者的耐甲氧西林金黄色葡萄球菌感染，治疗选择有限且相当昂贵。这篇综述文章提供了临床试验中的抗葡萄球菌药物和有效对抗革兰氏阳性菌（包括MRSA）的抗菌分子的最新进展。这些抗菌药物的结构和生物学信息对于设计新的抗MRSA药物具有重要的指导意义。
Methicillin-resistant Staphylococcus aureus (MRSA) have been on the increase during the past decade, due to the steady growth of the elderly and immunocompromised patients, and the emergence of multi-drug-resistant (MDR) bacterial strains. Although, only a limited number of anti-MRSA drugs are available, a number of different combination antimicrobial drug regimens have been used to treat serious MRSA infections. Thus, addition of several new antistaphylococcal drugs into clinical practice should broaden therapeutic options. Because MRSA is one of the most common and problematic bacteria associated with increasing antimicrobial resistance, continuous efforts on discovery of lead compounds as well as development of alternative therapies and faster diagnostics to ensure effective antistaphylococcal therapy are required. This article summarizes the FDA approved drugs to treat MRSA infections, the drugs in clinical trials, and the drug leads for MRSA and related Gram-positive bacterial infections. In addition, the mode of action of antistaphylococcal molecules and resistant mechanisms of some molecules are briefly discussed. The number of pipeline drugs presently undergoing clinical trials is not particularly encouraging. There are limited and rather expensive therapeutic options for the infections by MRSA in the critically ill. This review article provides an update on antistaphylococcal drugs in clinical trials and antibacterial molecules effective against Gram-positive bacteria including MRSA. The structural and biological information of antibacterials summarized here are very useful for designing drug leads to develop into new anti-MRSA drugs.
登录
查看更多内容
影响因子：
4.9
作者：
Brown, Steven D.;Traczewski, Maria M.
通讯作者：
Traczewski, Maria M.
影响因子：
5.7
作者：
Bagnoli F;Bertholet S;Grandi G
通讯作者：
Grandi G
影响因子：
11.8
作者：
Boucher, Helen W.;Talbot, George H.;Bartlett, John
通讯作者：
Bartlett, John
影响因子：
82.9
作者：
Brötz-Oesterhelt, H;Beyer, D;Labischinski, H
通讯作者：
Labischinski, H
影响因子：
11.8
作者：
Anthony, Kara B.;Fishman, Neil O.;Lautenbach, Ebbing
通讯作者：
Lautenbach, Ebbing