A fragment-based approach leading to the discovery of a novel binding site and the selective CK2 inhibitor CAM4066

Recently we reported the discovery of a potent and selective CK2α inhibitor CAM4066. This compound inhibits CK2 activity by exploiting a pocket located outside the ATP binding site (αD pocket). Here we describe in detail the journey that led to the discovery of CAM4066 using the challenging fragment...

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Detalles Bibliográficos
Autores principales: De Fusco, Claudia, Brear, Paul, Iegre, Jessica, Georgiou, Kathy Hadje, Sore, Hannah F., Hyvönen, Marko, Spring, David R.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Science 2017
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5587527/
https://www.ncbi.nlm.nih.gov/pubmed/28495381
http://dx.doi.org/10.1016/j.bmc.2017.04.037

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5587527/
https://www.ncbi.nlm.nih.gov/pubmed/28495381
http://dx.doi.org/10.1016/j.bmc.2017.04.037

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