Structure-Based Design of a Potent, Selective, and Brain Penetrating PDE2 Inhibitor with Demonstrated Target Engagement

[Image: see text] Structure-guided design led to the identification of the novel, potent, and selective phosphodiesterase 2 (PDE2) inhibitor 12. Compound 12 demonstrated a >210-fold selectivity versus PDE10 and PDE11 and was inactive against all other PDE family members up to 10 μM. In vivo evalu...

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Auteurs principaux: Buijnsters, Peter, De Angelis, Meri, Langlois, Xavier, Rombouts, Frederik J. R., Sanderson, Wendy, Tresadern, Gary, Ritchie, Alison, Trabanco, Andrés A., VanHoof, Greet, Roosbroeck, Yves Van, Andrés, José-Ignacio
Format: Artigo
Langue:Inglês
Publié: American Chemical Society 2014
Accès en ligne:https://ncbi.nlm.nih.gov/pmc/articles/PMC4160764/
https://ncbi.nlm.nih.gov/pubmed/25221665
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml500262u
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