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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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Pubblicato in:J Med Chem
Autori principali: 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
Natura: Artigo
Lingua:Inglês
Pubblicazione: American Chemical Society 2018
Accesso online: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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