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Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity.
Blaazer AR, Singh AK, de Heuvel E, Edink E, Orrling KM, Veerman JJN, van den Bergh T, Jansen C, Balasubramaniam E, Mooij WJ, Custers H, Sijm M, Tagoe DNA, Kalejaiye TD, Munday JC, Tenor H, Matheeussen A, Wijtmans M, Siderius M, de Graaf C, Maes L, de Koning HP, Bailey DS, Sterk GJ, de Esch IJP, Brown DG, Leurs R. Blaazer AR, et al. Among authors: siderius m. J Med Chem. 2018 May 10;61(9):3870-3888. doi: 10.1021/acs.jmedchem.7b01670. Epub 2018 May 1. J Med Chem. 2018. PMID: 29672041 Free PMC article.
Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors.
de Heuvel E, Singh AK, Edink E, van der Meer T, van der Woude M, Sadek P, Krell-Jørgensen MP, van den Bergh T, Veerman J, Caljon G, Kalejaiye TD, Wijtmans M, Maes L, de Koning HP, Jan Sterk G, Siderius M, de Esch IJP, Brown DG, Leurs R. de Heuvel E, et al. Among authors: siderius m. Bioorg Med Chem. 2019 Sep 15;27(18):3998-4012. doi: 10.1016/j.bmc.2019.06.027. Epub 2019 Jun 18. Bioorg Med Chem. 2019. PMID: 31327675 Free article.
Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors (Part 2).
de Heuvel E, Singh AK, Boronat P, Kooistra AJ, van der Meer T, Sadek P, Blaazer AR, Shaner NC, Bindels DS, Caljon G, Maes L, Sterk GJ, Siderius M, Oberholzer M, de Esch IJP, Brown DG, Leurs R. de Heuvel E, et al. Among authors: siderius m. Bioorg Med Chem. 2019 Sep 15;27(18):4013-4029. doi: 10.1016/j.bmc.2019.06.026. Epub 2019 Jul 5. Bioorg Med Chem. 2019. PMID: 31378593 Free article.
Cloning and functional complementation of ten Schistosoma mansoni phosphodiesterases expressed in the mammalian host stages.
Munday JC, Kunz S, Kalejaiye TD, Siderius M, Schroeder S, Paape D, Alghamdi AH, Abbasi Z, Huang SX, Donachie AM, William S, Sabra AN, Sterk GJ, Botros SS, Brown DG, Hoffman CS, Leurs R, de Koning HP. Munday JC, et al. Among authors: siderius m. PLoS Negl Trop Dis. 2020 Jul 30;14(7):e0008447. doi: 10.1371/journal.pntd.0008447. eCollection 2020 Jul. PLoS Negl Trop Dis. 2020. PMID: 32730343 Free PMC article.
Discovery of Diaryl Ether Substituted Tetrahydrophthalazinones as TbrPDEB1 Inhibitors Following Structure-Based Virtual Screening.
de Heuvel E, Kooistra AJ, Edink E, van Klaveren S, Stuijt J, van der Meer T, Sadek P, Mabille D, Caljon G, Maes L, Siderius M, de Esch IJP, Sterk GJ, Leurs R. de Heuvel E, et al. Among authors: siderius m. Front Chem. 2021 Jan 21;8:608030. doi: 10.3389/fchem.2020.608030. eCollection 2020. Front Chem. 2021. PMID: 33553105 Free PMC article.
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