Antitubercular drugs for an old target: GSK693 as a promising InhA direct inhibitor.

doi:10.1016/j.ebiom.2016.05.006

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Article

Antitubercular drugs for an old target: GSK693 as a promising InhA direct inhibitor.

EBioMedicine - 1 Jun 2016

Martínez-Hoyos María, Perez-Herran Esther, Gulten Gulcin, Encinas Lourdes, Álvarez-Gómez Daniel, Alvarez Emilio, Ferrer-Bazaga Santiago, García-Pérez Adolfo, Ortega Fátima, Angulo-Barturen Iñigo, Rullas-Trincado Joaquin, Blanco Ruano Delia, Torres Pedro, Castañeda Pablo, Huss Sophie, Fernández Menéndez Raquel, González Del Valle Silvia, Ballell Lluis, Barros David, Modha Sundip, Dhar Neeraj, Signorino-Gelo François, McKinney John D, García-Bustos Jose Francisco, Lavandera Jose Luis, Sacchettini James C, Jimenez M Soledad, Martín-Casabona Nuria, Castro-Pichel Julia, Mendoza-Losana Alfonso

Abstract excerpt

Despite being one of the first antitubercular agents identified, isoniazid (INH) is still the most prescribed drug for prophylaxis and tuberculosis (TB) treatment and, together with rifampicin, the pillars of current chemotherapy. A high percentage of isoniazid resistance is linked to mutations in the pro-drug activating enzyme KatG, so the discovery of direct inhibitors (DI) of the enoyl-ACP reductase (InhA) has...

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PMID: 27428438
DOI: 10.1016/j.ebiom.2016.05.006
PMCID: PMC4919555

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