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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Detalhes bibliográficos
Publicado no:Bioorg Med Chem
Main Authors: De Fusco, Claudia, Brear, Paul, Iegre, Jessica, Georgiou, Kathy Hadje, Sore, Hannah F., Hyvönen, Marko, Spring, David R.
Formato: Artigo
Idioma:Inglês
Publicado em: Elsevier Science 2017
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5587527/
https://ncbi.nlm.nih.gov/pubmed/28495381
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmc.2017.04.037
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