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Exploration of the molecular architecture of the orthosteric binding site in the α4β2 nicotinic acetylcholine receptor with analogs of 3-(dimethylamino)butyl dimethylcarbamate (DMABC) and 1-(pyridin-3-yl)-1,4-diazepane.
Bach TB, Jensen AA, Petersen JG, Sørensen TE, Della Volpe S, Liu J, Blaazer AR, van Muijlwijk-Koezen JE, Balle T, Frølund B. Bach TB, et al. Among authors: blaazer ar. Eur J Med Chem. 2015 Sep 18;102:425-44. doi: 10.1016/j.ejmech.2015.07.024. Epub 2015 Jul 17. Eur J Med Chem. 2015. PMID: 26301559
From recipe to research: introducing undergraduate students to the nature of science using a hybrid practical course centred on drug discovery for neglected diseases.
Wijtmans M, Edink E, van Linden OP, Zheng Y, Blaazer AR, Siderius M, van Muijlwijk-Koezen JE. Wijtmans M, et al. Among authors: blaazer ar. Drug Discov Today. 2021 Jun;26(6):1359-1368. doi: 10.1016/j.drudis.2021.02.012. Epub 2021 Feb 18. Drug Discov Today. 2021. PMID: 33609778 Free article. Review.
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. 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 (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: blaazer ar. 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.
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: blaazer ar. 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.
FDA-approved drug screening in patient-derived organoids demonstrates potential of drug repurposing for rare cystic fibrosis genotypes.
de Poel E, Spelier S, Hagemeijer MC, van Mourik P, Suen SWF, Vonk AM, Brunsveld JE, Ithakisiou GN, Kruisselbrink E, Oppelaar H, Berkers G, de Winter de Groot KM, Heida-Michel S, Jans SR, van Panhuis H, Bakker M, van der Meer R, Roukema J, Dompeling E, Weersink EJM, Koppelman GH, Blaazer AR, Muijlwijk-Koezen JE, van der Ent CK, Beekman JM. de Poel E, et al. Among authors: blaazer ar. J Cyst Fibros. 2023 May;22(3):548-559. doi: 10.1016/j.jcf.2023.03.004. Epub 2023 May 3. J Cyst Fibros. 2023. PMID: 37147251
11 results