title: Development of efflux pump inhibitors in antituberculosis therapy.
abstract: Resistance and tolerance to antituberculosis (anti-TB) drugs, especially the first-line drugs, has become a serious problem in anti-TB therapy. Efflux of antimicrobial agents via bacterial efflux pumps is one of the main reasons for drug resistance. Efflux pump inhibitors (EPIs) bind to efflux pumps to inhibit drug efflux and thus enhance the drug effect and reduce drug resistance. Studies on EPIs targeting the efflux pumps of Mycobacterium tuberculosis (Mtb) help to understand Mtb resistance and to identify the potential drug target and are of significance in guiding the development of new anti-TB drugs and optimal combinations. Currently, there are many potential EPIs under study, but none of them has been used clinically for anti-TB therapy. In this article, we will provide an overview on the current development of EPIs targeting the efflux pumps of Mtb and discuss their potential clinical applications.
authors.affiliation: Army Tuberculosis Prevention and Control Key Laboratory, Beijing Key Laboratory of New Techniques of Tuberculosis Diagnosis and Treatment, Institute of Tuberculosis Research, The 309th Hospital of Chinese PLA, Beijing 100091, China. Electronic address: songlele@sina.com.
authors.forename: Lele
authors.initials: L
authors.lastname: Song
authors.affiliation: Army Tuberculosis Prevention and Control Key Laboratory, Beijing Key Laboratory of New Techniques of Tuberculosis Diagnosis and Treatment, Institute of Tuberculosis Research, The 309th Hospital of Chinese PLA, Beijing 100091, China. Electronic address: xueqiongwu@139.com.
authors.forename: Xueqiong
authors.initials: X
authors.lastname: Wu
mesh_terms: D000995:Antitubercular Agents / Q000302:isolation & purification* / Q000494:pharmacology*; D001693:Biological Transport, Active / Q000187:drug effects*; D055808:Drug Discovery; D009169:Mycobacterium tuberculosis / Q000187:drug effects*
chemical_list: D000995:Antitubercular Agents
keywords: CCCP; Efflux pump inhibitor; Mycobacterium tuberculosis; Reserpine; Tuberculosis; Verapamil