Antituberculosis drugs: reducing efflux=increasing activity.

Autor: Rodrigues L; Grupo de Genética de Micobacterias, Departamento de Microbiología, Medicina Preventiva y Salud Pública, Facultad de Medicina and BIFI, Universidad de Zaragoza, Zaragoza, Spain; CIBER Enfermedades Respiratorias (CIBERES), Madrid, Spain; Fundación Agencia Aragonesa para la Investigación y Desarrollo (ARAID), Zaragoza, Spain., Parish T; TB Discovery Research, Infectious Disease Research Institute, Seattle, WA, USA., Balganesh M; AstraZeneca India Private Limited, Hebbal, Bangalore, India., Ainsa JA; Grupo de Genética de Micobacterias, Departamento de Microbiología, Medicina Preventiva y Salud Pública, Facultad de Medicina and BIFI, Universidad de Zaragoza, Zaragoza, Spain; CIBER Enfermedades Respiratorias (CIBERES), Madrid, Spain. Electronic address: ainsa@unizar.es.
Jazyk: angličtina
Zdroj: Drug discovery today [Drug Discov Today] 2017 Mar; Vol. 22 (3), pp. 592-599. Date of Electronic Publication: 2017 Jan 13.
DOI: 10.1016/j.drudis.2017.01.002
Abstrakt: In mycobacteria, it was assumed that efflux pumps only had a marginal role in drug resistance. In recent years, owing to the need to find novel drugs against multidrug-resistant tuberculosis, it has become clear that efflux should not be ignored. Although efflux inhibitors have been very useful for characterizing in vitro the properties of efflux pumps, their usefulness in vivo is limited because of their toxicity. Alternatively, programs aimed at discovering novel drugs for treating tuberculosis should implement strategies to characterize efflux liability of candidate drugs. Here, we present an experimental approach for studying efflux of compounds selected under the More Medicines for Tuberculosis research project, and a few examples of how, for tuberculosis drug discovery, efflux matters.
(Copyright © 2017 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE
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