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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Publicado no:J Med Chem
Main Authors: 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: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2018
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5949723/
https://ncbi.nlm.nih.gov/pubmed/29672041
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.7b01670
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