Structure-Based Design of MptpB Inhibitors That Reduce Multidrug-Resistant Mycobacterium tuberculosis Survival and Infection Burden in Vivo

Mycobacterium tuberculosis protein-tyrosine-phosphatase B (MptpB) is a secreted virulence factor that subverts antimicrobial activity in the host. We report here the structure-based design of selective MptpB inhibitors that reduce survival of multidrug-resistant tuberculosis strains in macrophages a...

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Veröffentlicht in:	Journal of medicinal chemistry 2018-09, Vol.61 (18), p.8337-8352
Hauptverfasser:	Vickers, Clare F, Silva, Ana P. G, Chakraborty, Ajanta, Fernandez, Paulina, Kurepina, Natalia, Saville, Charis, Naranjo, Yandi, Pons, Miquel, Schnettger, Laura S, Gutierrez, Maximiliano G, Park, Steven, Kreiswith, Barry N, Perlin, David S, Thomas, Eric J, Cavet, Jennifer S, Tabernero, Lydia
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antitubercular Agents - chemistry Antitubercular Agents - pharmacology Bacterial Proteins - antagonists & inhibitors Bacterial Proteins - chemistry Drug Design Drug Resistance, Multiple - drug effects Female Guinea Pigs Macrophages - drug effects Macrophages - microbiology Macrophages - pathology Male Models, Molecular Molecular Structure Mycobacterium tuberculosis - drug effects Protein Conformation Protein Tyrosine Phosphatases - antagonists & inhibitors Protein Tyrosine Phosphatases - chemistry Structure-Activity Relationship Tuberculosis, Multidrug-Resistant - drug therapy Tuberculosis, Multidrug-Resistant - microbiology
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