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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Bibliografiset tiedot
Julkaisussa:J Med Chem
Päätekijät: 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
Aineistotyyppi: Artigo
Kieli:Inglês
Julkaistu: American Chemical Society 2018
Linkit: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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