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From On-Target to Off-Target Activity: Identification and Optimisation of Trypanosoma brucei GSK3 Inhibitors and Their Characterisation as Anti-Trypanosoma brucei Drug Discovery Lead Molecules

Human African trypanosomiasis (HAT) is a life-threatening disease with approximately 30 000–40 000 new cases each year. Trypanosoma brucei protein kinase GSK3 short (TbGSK3) is required for parasite growth and survival. Herein we report a screen of a focused kinase library against T. brucei GSK3. Fr...

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Detalles Bibliográficos
Autores principales: Woodland, Andrew, Grimaldi, Raffaella, Luksch, Torsten, Cleghorn, Laura A T, Ojo, Kayode K, Van Voorhis, Wesley C, Brenk, Ruth, Frearson, Julie A, Gilbert, Ian H, Wyatt, Paul G
Formato: Online Artículo Texto
Lenguaje:English
Publicado: WILEY-VCH Verlag 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3728731/
https://www.ncbi.nlm.nih.gov/pubmed/23776181
http://dx.doi.org/10.1002/cmdc.201300072