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Page 1
First-in-Class Selective Inhibitors of the Lysine Acetyltransferase KAT8.
Fiorentino F, Sementilli S, Menna M, Turrisi F, Tomassi S, Pellegrini FR, Iuzzolino A, D'Acunzo F, Feoli A, Wapenaar H, Taraglio S, Fraschetti C, Del Bufalo D, Sbardella G, Dekker FJ, Paiardini A, Trisciuoglio D, Mai A, Rotili D. Fiorentino F, et al. Among authors: wapenaar h. J Med Chem. 2023 May 25;66(10):6591-6616. doi: 10.1021/acs.jmedchem.2c01937. Epub 2023 May 8. J Med Chem. 2023. PMID: 37155735 Free PMC article.
Enzyme kinetics and inhibition of histone acetyltransferase KAT8.
Wapenaar H, van der Wouden PE, Groves MR, Rotili D, Mai A, Dekker FJ. Wapenaar H, et al. Eur J Med Chem. 2015 Nov 13;105:289-96. doi: 10.1016/j.ejmech.2015.10.016. Epub 2015 Oct 22. Eur J Med Chem. 2015. PMID: 26505788 Free PMC article.
The relevance of Ki calculation for bi-substrate enzymes illustrated by kinetic evaluation of a novel lysine (K) acetyltransferase 8 inhibitor.
Wapenaar H, van den Bosch T, Leus NGJ, van der Wouden PE, Eleftheriadis N, Hermans J, Hailu GS, Rotili D, Mai A, Dömling A, Bischoff R, Haisma HJ, Dekker FJ. Wapenaar H, et al. Eur J Med Chem. 2017 Aug 18;136:480-486. doi: 10.1016/j.ejmech.2017.05.015. Epub 2017 May 5. Eur J Med Chem. 2017. PMID: 28527406 Free PMC article.
A 6-alkylsalicylate histone acetyltransferase inhibitor inhibits histone acetylation and pro-inflammatory gene expression in murine precision-cut lung slices.
van den Bosch T, Leus NGJ, Wapenaar H, Boichenko A, Hermans J, Bischoff R, Haisma HJ, Dekker FJ. van den Bosch T, et al. Among authors: wapenaar h. Pulm Pharmacol Ther. 2017 Jun;44:88-95. doi: 10.1016/j.pupt.2017.03.006. Epub 2017 Mar 16. Pulm Pharmacol Ther. 2017. PMID: 28323055 Free PMC article.
Discovery of chromenes as inhibitors of macrophage migration inhibitory factor.
Kok T, Wapenaar H, Wang K, Neochoritis CG, Zarganes-Tzitzikas T, Proietti G, Eleftheriadis N, Kurpiewska K, Kalinowska-Tłuścik J, Cool RH, Poelarends GJ, Dömling A, Dekker FJ. Kok T, et al. Among authors: wapenaar h. Bioorg Med Chem. 2018 Mar 1;26(5):999-1005. doi: 10.1016/j.bmc.2017.12.032. Epub 2017 Dec 24. Bioorg Med Chem. 2018. PMID: 29428527 Free PMC article.
Structure-kinetic relationships--an overlooked parameter in hit-to-lead optimization: a case of cyclopentylamines as chemokine receptor 2 antagonists.
Vilums M, Zweemer AJ, Yu Z, de Vries H, Hillger JM, Wapenaar H, Bollen IA, Barmare F, Gross R, Clemens J, Krenitsky P, Brussee J, Stamos D, Saunders J, Heitman LH, Ijzerman AP. Vilums M, et al. Among authors: wapenaar h. J Med Chem. 2013 Oct 10;56(19):7706-14. doi: 10.1021/jm4011737. Epub 2013 Sep 27. J Med Chem. 2013. PMID: 24028535
DNMT3B PWWP mutations cause hypermethylation of heterochromatin.
Taglini F, Kafetzopoulos I, Rolls W, Musialik KI, Lee HY, Zhang Y, Marenda M, Kerr L, Finan H, Rubio-Ramon C, Gautier P, Wapenaar H, Kumar D, Davidson-Smith H, Wills J, Murphy LC, Wheeler A, Wilson MD, Sproul D. Taglini F, et al. Among authors: wapenaar h. EMBO Rep. 2024 Mar;25(3):1130-1155. doi: 10.1038/s44319-024-00061-5. Epub 2024 Jan 30. EMBO Rep. 2024. PMID: 38291337 Free PMC article.
11 results