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Page 1
Evaluation of phthalazinone phosphodiesterase inhibitors with improved activity and selectivity against Trypanosoma cruzi.
De Araújo JS, da Silva PB, Batista MM, Peres RB, Cardoso-Santos C, Kalejaiye TD, Munday JC, De Heuvel E, Sterk GJ, Augustyns K, Salado IG, Matheeussen A, De Esch I, De Koning HP, Leurs R, Maes L, Soeiro MNC. De Araújo JS, et al. Among authors: de heuvel e. J Antimicrob Chemother. 2020 Apr 1;75(4):958-967. doi: 10.1093/jac/dkz516. J Antimicrob Chemother. 2020. PMID: 31860098
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: de koning hp, de heuvel e, de graaf c, de esch ijp. 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: de koning hp, de heuvel e, de esch ijp. 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.
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. 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. 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.
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: de heuvel e. Int J Mol Sci. 2023 Apr 6;24(7):6817. doi: 10.3390/ijms24076817. Int J Mol Sci. 2023. PMID: 37047792 Free PMC article.
Discovery of small molecule vanin inhibitors: new tools to study metabolism and disease.
Jansen PA, van Diepen JA, Ritzen B, Zeeuwen PL, Cacciatore I, Cornacchia C, van Vlijmen-Willems IM, de Heuvel E, Botman PN, Blaauw RH, Hermkens PH, Rutjes FP, Schalkwijk J. Jansen PA, et al. Among authors: de heuvel e. ACS Chem Biol. 2013 Mar 15;8(3):530-4. doi: 10.1021/cb3006424. Epub 2013 Jan 2. ACS Chem Biol. 2013. PMID: 23270378
Stable pantothenamide bioisosteres: novel antibiotics for Gram-positive bacteria.
Jansen PAM, van der Krieken DA, Botman PNM, Blaauw RH, Cavina L, Raaijmakers EM, de Heuvel E, Sandrock J, Pennings LJ, Hermkens PHH, Zeeuwen PLJM, Rutjes FPJT, Schalkwijk J. Jansen PAM, et al. Among authors: de heuvel e. J Antibiot (Tokyo). 2019 Sep;72(9):682-692. doi: 10.1038/s41429-019-0196-6. Epub 2019 Jun 6. J Antibiot (Tokyo). 2019. PMID: 31171848 Free PMC article.
27 results