Saxena Deepanshi, Maitra Rahul, Bormon Rakhi, Czekanska Marta, Meiers Joscha, Titz Alexander, Verma Sandeep, Chopra Sidharth
Department of Molecular Microbiology and Immunology, CSIR-Central Drug Research Institute, Jankipuram Extension, Sitapur Road, Lucknow, 226031, UP, India.
Department of Chemistry, IIT Kanpur, Kanpur, 208016, UP, India.
NPJ Antimicrob Resist. 2023 Dec 20;1(1):17. doi: 10.1038/s44259-023-00016-1.
Emerging resistance to all available antibiotics highlights the need to develop new antibiotics with novel mechanisms of action. Most of the currently used antibiotics target Gram-positive bacteria while Gram-negative bacteria easily bypass the action of most drug molecules because of their unique outer membrane. This additional layer acts as a potent barrier restricting the entry of compounds into the cell. In this scenario, several approaches have been elucidated to increase the accumulation of compounds into Gram-negative bacteria. This review includes a brief description of the physicochemical properties that can aid compounds to enter and accumulate in Gram-negative bacteria and covers different strategies to target or bypass the outer membrane-mediated barrier in Gram-negative bacterial pathogens.
对所有现有抗生素产生的新耐药性凸显了开发具有新型作用机制的新抗生素的必要性。目前使用的大多数抗生素针对革兰氏阳性菌，而革兰氏阴性菌由于其独特的外膜，很容易避开大多数药物分子的作用。这一额外的层起到了强大的屏障作用，限制化合物进入细胞。在这种情况下，已经阐明了几种方法来增加化合物在革兰氏阴性菌中的积累。这篇综述简要描述了有助于化合物进入并在革兰氏阴性菌中积累的物理化学性质，并涵盖了针对革兰氏阴性菌病原体中由外膜介导的屏障或绕过该屏障的不同策略。
