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

Autor: An Matheeussen, Titilola D. Kalejaiye, Erik de Heuvel, A.R. Blaazer, A.K. Singh, Maikel Wijtmans, Wouter J. Mooij, Chris de Graaf, Maarten Sijm, Johan Veerman, Hermann Tenor, Chimed Jansen, Toine J. M. van den Bergh, David S. Bailey, Harry P. de Koning, Erin Balasubramaniam, Rob Leurs, Marco Siderius, David G. Brown, Iwan J. P. de Esch, Geert Jan Sterk, Louis Maes, Kristina M. Orrling, Daniel N. A. Tagoe, Hans Custers, Jane C. Munday, Ewald Edink

Publikováno v: Journal of Medicinal Chemistry
Journal of medicinal chemistry
Blaazer, A R, Singh, A K, De Heuvel, E, Edink, E, Orrling, K M, Veerman, J J N, Van Den Bergh, T, Jansen, C, Balasubramaniam, E, Mooij, W J, Custers, H, Sijm, M, Tagoe, D N A, Kalejaiye, T D, Munday, J C, Tenor, H, Matheeussen, A, Wijtmans, M, Siderius, M, De Graaf, C, Maes, L, De Koning, H P, Bailey, D S, Sterk, G J, De Esch, I J P, Brown, D G & Leurs, R 2018, ' Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity ', Journal of Medicinal Chemistry, vol. 61, no. 9, pp. 3870-3888 . https://doi.org/10.1021/acs.jmedchem.7b01670
Journal of Medicinal Chemistry, 61(9), 3870-3888. American Chemical Society

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 considere

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f099b2fe26db21d0211e62360e1d7c87
https://pubmed.ncbi.nlm.nih.gov/29672041