流出
铜绿假单胞菌
生物信息学
微生物学
假单胞菌科
生物
化学
细菌
生物化学
基因
遗传学
作者
Suzanne Abdelmalek,Malak Hajar,Luma Salah,Heba Abdel‐Halim
出处
期刊:Microbial Drug Resistance
[Mary Ann Liebert]
日期:2023-12-26
标识
DOI:10.1089/mdr.2023.0126
摘要
The emergence of multidrug-resistant Pseudomonas aeruginosa possesses a significant public health concern. Constitutively expressed MexAB–OprM efflux pumps in P. aeruginosa significantly contribute to its resistance to a variety of antibiotics. The development of efflux pump inhibitors (EPIs) has emerged as an attractive strategy in reversing antibiotic resistance. In this study, structure-based virtual screening techniques were used for the identification of new MexAB–OprM efflux inhibitors. The predicted poses were thoroughly filtered by induced fit docking procedures followed by in vitro microbiological assays for the validation of in silico results. Two compounds, NSC-147850 and NSC-112703, were able to restore tetracycline susceptibility in MexAB–OprM overexpressing Pseudomonas aeruginosa ATCC® 27853™ strain. This correlation observed between in silico screening and positive efflux inhibitory activity in vitro suggests that NSC-147850 and NSC-112703 have potential as EPIs and may be effective in combination therapy against drug-resistant strains of P. aeruginosa.
科研通智能强力驱动
Strongly Powered by AbleSci AI