Author/Editor		Rožman, Kaja; Sosič, Izidor; Fernandez-Menendez, Raquel; Young, Robert J.; Mendoza-Losana, Alfonso; Gobec, Stanislav; Encinas, Lourdes
Title		A new 'golden age' for the antitubercular target InhA
Type		članek
Vol. and No.		Letnik 22, št. 3
Publication year		2017
Volume		str. 492-502
ISSN		1878-5832 - Drug discovery today
Language		eng
Abstract		The increasing prevalence of multidrug-resistant strains of Mycobacterium tuberculosis is the main contributing factor in unfavorable outcomes in the treatment of tuberculosis. Studies suggest that direct inhibitors of InhA, an enoyl-ACP-reductase, might yield promising clinical candidates that can be developed into new antitubercular drugs. In this review, we describe the application of different hit-identification strategies to InhA, which clearly illustrate the druggability of its active site through distinct binding mechanisms. We further characterize four classes of InhA inhibitors that show novel binding modes, and provide evidence of their successful target engagement as well as their in vivo activity.
Keywords		tubercolosis InhA screening technologies structure-guided design InhA inhibitors