Design and Synthesis of Selective Phosphodiesterase 4D (PDE4D) Allosteric Inhibitors for the Treatment of Fragile X Syndrome and Other Brain Disorders

Novel pyridine- and pyrimidine-based allosteric inhibitors are reported that achieve PDE4D subtype selectivity through recognition of a single amino acid difference on a key regulatory domain, known as UCR2, that opens and closes over the catalytic site for cAMP hydrolysis. The design and optimizati...

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Опубликовано в: :J Med Chem
Главные авторы: Gurney, Mark E., Nugent, Richard A., Mo, Xuesheng, Sindac, Janice A., Hagen, Timothy J., Fox, David, O’Donnell, James M., Zhang, Chong, Xu, Ying, Zhang, Han-Ting, Groppi, Vincent E., Bailie, Marc, White, Ronald E., Romero, Donna L., Vellekoop, A. Samuel, Walker, Joel R., Surman, Matthew D., Zhu, Lei, Campbell, Robert F.
Формат: Artigo
Язык:Inglês
Опубликовано: 2019
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Article
Online-ссылка:https://ncbi.nlm.nih.gov/pmc/articles/PMC7444661/
https://ncbi.nlm.nih.gov/pubmed/31013090
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.9b00193
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