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A new strategy for hit generation: Novel in cellulo active inhibitors of CYP121A1 from Mycobacterium tuberculosis via a combined X-ray crystallographic and phenotypic screening approach (XP screen)

There is a pressing need for new drugs against tuberculosis (TB) to combat the growing resistance to current antituberculars. Herein a novel strategy is described for hit generation against promising TB targets involving X-ray crystallographic screening in combination with phenotypic screening. This...

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Detalles Bibliográficos
Autores principales: Frederickson, Martyn, Selvam, Irwin R., Evangelopoulos, Dimitrios, McLean, Kirsty J., Katariya, Mona M., Tunnicliffe, Richard B., Campbell, Bethany, Kavanagh, Madeline E., Charoensutthivarakul, Sitthivut, Blankley, Richard T., Levy, Colin W., de Carvalho, Luiz Pedro S., Leys, David, Munro, Andrew W., Coyne, Anthony G., Abell, Chris
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Editions Scientifiques Elsevier 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8856928/
https://www.ncbi.nlm.nih.gov/pubmed/35065413
http://dx.doi.org/10.1016/j.ejmech.2022.114105