title: Inhibitors of mycobacterial efflux pumps as potential boosters for anti-tubercular drugs.
abstract: Tuberculosis is one of the major causes of infection across the world. The emergence of multi-, extensively- and totally drug-resistant strains of Mycobacterium tuberculosis contributes to the lack of therapeutic options available. The mechanisms associated with this resistance could involve mutations in genes coding for target proteins, decreased permeability, increased efflux and so on. Resistance mediated by efflux systems has become more relevant, since these systems help the bacteria to extrude antibiotics until relevant mutations emerge and become established in the population. Therefore, compounds that inhibit these transport systems are of major importance and have been studied in the last few years. Not only do these compounds act on the bacterial efflux systems but they have also been explored for their dual role as boosters of the macrophage-infected cells. The search for novel compounds or combinations of adjuvant compounds and antibiotics to treat mycobacterial multidrug-resistant infections has become a major goal in the treatment of these diseases.
authors.affiliation: Grupo de Micobactérias, Unidade de Microbiologia Médica, Instituto de Higiene e Medicina Tropical, Universidade Nova de Lisboa, Rua da Junqueira 100, 1349-008 Lisbon, Portugal. mviveiros@ihmt.unl.pt
authors.forename: Miguel
authors.initials: M
authors.lastname: Viveiros
authors.forename: Marta
authors.initials: M
authors.lastname: Martins
authors.forename: Liliana
authors.initials: L
authors.lastname: Rodrigues
authors.forename: Diana
authors.initials: D
authors.lastname: Machado
authors.forename: Isabel
authors.initials: I
authors.lastname: Couto
authors.forename: José
authors.initials: J
authors.lastname: Ainsa
authors.forename: Leonard
authors.initials: L
authors.lastname: Amaral
mesh_terms: D000995:Antitubercular Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D001426:Bacterial Proteins / Q000037:antagonists & inhibitors* / Q000235:genetics; D001692:Biological Transport / Q000187:drug effects / Q000235:genetics; D024881:Drug Resistance, Bacterial / Q000187:drug effects / Q000235:genetics; D004357:Drug Synergism; D004359:Drug Therapy, Combination / Q000379:methods / Q000639:trends; D006801:Humans; D026901:Membrane Transport Proteins / Q000187:drug effects / Q000235:genetics; D008954:Models, Biological; D009169:Mycobacterium tuberculosis / Q000187:drug effects* / Q000235:genetics; D018088:Tuberculosis, Multidrug-Resistant / Q000188:drug therapy
chemical_list: D000995:Antitubercular Agents; D001426:Bacterial Proteins; D026901:Membrane Transport Proteins