Please use this identifier to cite or link to this item:
Title: Structure-based design of MptpB inhibitors that reduce multi-drug-resistant mycobacterium tuberculosis survival and infection burden in vivo
Author: Vickers, Clare F.
Silva, Ana P. G.
Chakraborty, Ajanta
Fernandez, Paulina
Kurepina, Natalia
Saville, Charis
Naranjo, Yandi
Pons Vallès, Miquel
Schnettger, Laura S.
Gutierrez, Maximiliano G.
Park, Steven
Keiswirth, Barry N.
Perlin, David S.
Thomas, Eric J.
Cavet, Jennifer S.
Tabernero, Lydia
Keywords: Fosforilació
Issue Date: 28-Aug-2018
Publisher: American Chemical Society
Abstract: 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 and enhance killing efficacy by first-line antibiotics. Monotherapy with an orally bioavailable MptpB inhibitor reduces infection burden in acute and chronic guinea pig models and improves the overall pathology. Our findings provide a new paradigm for tuberculosis treatment
Note: Versió postprint del document publicat a:
It is part of: Journal of Medicinal Chemistry, 2018, vol. 61, num. 18, p. 8337-8352
Related resource:
ISSN: 0022-2623
Appears in Collections:Articles publicats en revistes (Química Inorgànica i Orgànica)

Files in This Item:
File Description SizeFormat 
682384.pdf8.82 MBAdobe PDFView/Open

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.