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4,6-Diphenylpyridines as Promising Novel Anti-Influenza Agents Targeting the PA-PB1 Protein-Protein Interaction: Structure-Activity Relationships Exploration with the Aid of Molecular Modeling.
Trist IM, Nannetti G, Tintori C, Fallacara AL, Deodato D, Mercorelli B, Palù G, Wijtmans M, Gospodova T, Edink E, Verheij M, de Esch I, Viteva L, Loregian A, Botta M. Trist IM, et al. Among authors: edink e. J Med Chem. 2016 Mar 24;59(6):2688-703. doi: 10.1021/acs.jmedchem.5b01935. Epub 2016 Mar 11. J Med Chem. 2016. PMID: 26924568 Free article.
Synthesis and evaluation of analogs of the phenylpyridazinone NPD-001 as potent trypanosomal TbrPDEB1 phosphodiesterase inhibitors and in vitro trypanocidals.
Veerman J, van den Bergh T, Orrling KM, Jansen C, Cos P, Maes L, Chatelain E, Ioset JR, Edink EE, Tenor H, Seebeck T, de Esch I, Leurs R, Sterk GJ. Veerman J, et al. Among authors: edink ee. Bioorg Med Chem. 2016 Apr 1;24(7):1573-81. doi: 10.1016/j.bmc.2016.02.032. Epub 2016 Feb 26. Bioorg Med Chem. 2016. PMID: 26935942
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: edink e. 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: edink e. 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.
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: edink e. 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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