Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity

[Image: see text] Several trypanosomatid cyclic nucleotide phosphodiesterases (PDEs) possess a unique, parasite-specific cavity near the ligand-binding region that is referred to as the P-pocket. One of these enzymes, Trypanosoma brucei PDE B1 (TbrPDEB1), is considered a drug target for the treatmen...

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Detalles Bibliográficos
Autores principales: Blaazer, Antoni R., Singh, Abhimanyu K., de Heuvel, Erik, Edink, Ewald, Orrling, Kristina M., Veerman, Johan J. N., van den Bergh, Toine, Jansen, Chimed, Balasubramaniam, Erin, Mooij, Wouter J., Custers, Hans, Sijm, Maarten, Tagoe, Daniel N. A., Kalejaiye, Titilola D., Munday, Jane C., Tenor, Hermann, Matheeussen, An, Wijtmans, Maikel, Siderius, Marco, de Graaf, Chris, Maes, Louis, de Koning, Harry P., Bailey, David S., Sterk, Geert Jan, de Esch, Iwan J. P., Brown, David G., Leurs, Rob
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2018
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5949723/
https://www.ncbi.nlm.nih.gov/pubmed/29672041
http://dx.doi.org/10.1021/acs.jmedchem.7b01670

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