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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. Among authors: domling a. 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.
MCR synthesis of a tetracyclic tetrazole scaffold.
Patil P, Khoury K, Herdtweck E, Dömling A. Patil P, et al. Among authors: domling a. Bioorg Med Chem. 2015 Jun 1;23(11):2699-715. doi: 10.1016/j.bmc.2014.12.021. Epub 2014 Dec 20. Bioorg Med Chem. 2015. PMID: 25630499 Free PMC article.
Synthesis and Enantiomeric Separation of a Novel Spiroketal Derivative: A Potent Human Telomerase Inhibitor with High in Vitro Anticancer Activity.
Fuggetta MP, De Mico A, Cottarelli A, Morelli F, Zonfrillo M, Ulgheri F, Peluso P, Mannu A, Deligia F, Marchetti M, Roviello G, Reyes Romero A, Dömling A, Spanu P. Fuggetta MP, et al. Among authors: domling a. J Med Chem. 2016 Oct 13;59(19):9140-9149. doi: 10.1021/acs.jmedchem.6b01046. Epub 2016 Sep 19. J Med Chem. 2016. PMID: 27592503
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: domling a. 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.
260 results