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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: sijm 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.
Screening of a PDE-focused library identifies imidazoles with in vitro and in vivo antischistosomal activity.
Botros SS, William S, Sabra AA, El-Lakkany NM, Seif El-Din SH, García-Rubia A, Sebastián-Pérez V, Blaazer AR, de Heuvel E, Sijm M, Zheng Y, Salado IG, Munday JC, Maes L, de Esch IJP, Sterk GJ, Augustyns K, Leurs R, Gil C, De Koning HP. Botros SS, et al. Among authors: sijm m. Int J Parasitol Drugs Drug Resist. 2019 Apr;9:35-43. doi: 10.1016/j.ijpddr.2019.01.001. Epub 2019 Jan 14. Int J Parasitol Drugs Drug Resist. 2019. PMID: 30669086 Free PMC article.
Efficacy of Novel Pyrazolone Phosphodiesterase Inhibitors in Experimental Mouse Models of Trypanosoma cruzi.
de Araújo JS, França da Silva C, Batista DDGJ, Nefertiti A, Fiuza LFA, Fonseca-Berzal CR, Bernardino da Silva P, Batista MM, Sijm M, Kalejaiye TD, de Koning HP, Maes L, Sterk GJ, Leurs R, Soeiro MNC. de Araújo JS, et al. Among authors: sijm m. Antimicrob Agents Chemother. 2020 Aug 20;64(9):e00414-20. doi: 10.1128/AAC.00414-20. Print 2020 Aug 20. Antimicrob Agents Chemother. 2020. PMID: 32601163 Free PMC article.
To Target or Not to Target Schistosoma mansoni Cyclic Nucleotide Phosphodiesterase 4A?
Zheng Y, Schroeder S, Kanev GK, Botros SS, William S, Sabra AA, Maes L, Caljon G, Gil C, Martinez A, Salado IG, Augustyns K, Edink E, Sijm M, de Heuvel E, de Esch IJP, van der Meer T, Siderius M, Sterk GJ, Brown D, Leurs R. Zheng Y, et al. Among authors: sijm m. Int J Mol Sci. 2023 Apr 6;24(7):6817. doi: 10.3390/ijms24076817. Int J Mol Sci. 2023. PMID: 37047792 Free PMC article.
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