Please use this identifier to cite or link to this item:
http://hdl.handle.net/2445/138558
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DC Field | Value | Language |
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dc.contributor.author | Vickers, Clare F. | - |
dc.contributor.author | Silva, Ana P. G. | - |
dc.contributor.author | Chakraborty, Ajanta | - |
dc.contributor.author | Fernandez, Paulina | - |
dc.contributor.author | Kurepina, Natalia | - |
dc.contributor.author | Saville, Charis | - |
dc.contributor.author | Naranjo, Yandi | - |
dc.contributor.author | Pons Vallès, Miquel | - |
dc.contributor.author | Schnettger, Laura S. | - |
dc.contributor.author | Gutierrez, Maximiliano G. | - |
dc.contributor.author | Park, Steven | - |
dc.contributor.author | Keiswirth, Barry N. | - |
dc.contributor.author | Perlin, David S. | - |
dc.contributor.author | Thomas, Eric J. | - |
dc.contributor.author | Cavet, Jennifer S. | - |
dc.contributor.author | Tabernero, Lydia | - |
dc.date.accessioned | 2019-07-30T07:05:23Z | - |
dc.date.available | 2019-08-28T05:10:20Z | - |
dc.date.issued | 2018-08-28 | - |
dc.identifier.issn | 0022-2623 | - |
dc.identifier.uri | http://hdl.handle.net/2445/138558 | - |
dc.description.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 | - |
dc.format.extent | 16 p. | - |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | American Chemical Society | - |
dc.relation.isformatof | Versió postprint del document publicat a: https://doi.org/10.1021/acs.jmedchem.8b00832 | - |
dc.relation.ispartof | Journal of Medicinal Chemistry, 2018, vol. 61, num. 18, p. 8337-8352 | - |
dc.relation.uri | https://doi.org/10.1021/acs.jmedchem.8b00832 | - |
dc.rights | (c) American Chemical Society , 2018 | - |
dc.source | Articles publicats en revistes (Química Inorgànica i Orgànica) | - |
dc.subject.classification | Fosforilació | - |
dc.subject.classification | Tuberculosi | - |
dc.subject.other | Phosphorylation | - |
dc.subject.other | Tuberculosis | - |
dc.title | Structure-based design of MptpB inhibitors that reduce multi-drug-resistant mycobacterium tuberculosis survival and infection burden in vivo | - |
dc.type | info:eu-repo/semantics/article | - |
dc.type | info:eu-repo/semantics/acceptedVersion | - |
dc.identifier.idgrec | 682384 | - |
dc.date.updated | 2019-07-30T07:05:24Z | - |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | - |
dc.identifier.pmid | 30153005 | - |
Appears in Collections: | Articles publicats en revistes (Química Inorgànica i Orgànica) |
Files in This Item:
File | Description | Size | Format | |
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682384.pdf | 8.82 MB | Adobe PDF | View/Open |
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