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DXS as a target for structure-based drug design.
Gierse RM, Redeem E, Diamanti E, Wrenger C, Groves MR, Hirsch AK. Gierse RM, et al. Future Med Chem. 2017 Jul;9(11):1277-1294. doi: 10.4155/fmc-2016-0239. Epub 2017 Jun 21. Future Med Chem. 2017. PMID: 28636418 Review.
Hit-optimization using target-directed dynamic combinatorial chemistry: development of inhibitors of the anti-infective target 1-deoxy-d-xylulose-5-phosphate synthase.
Jumde RP, Guardigni M, Gierse RM, Alhayek A, Zhu D, Hamid Z, Johannsen S, Elgaher WAM, Neusens PJ, Nehls C, Haupenthal J, Reiling N, Hirsch AKH. Jumde RP, et al. Among authors: gierse rm. Chem Sci. 2021 Apr 28;12(22):7775-7785. doi: 10.1039/d1sc00330e. Chem Sci. 2021. PMID: 34168831 Free PMC article.
Discovery of novel drug-like antitubercular hits targeting the MEP pathway enzyme DXPS by strategic application of ligand-based virtual screening.
Zhu D, Johannsen S, Masini T, Simonin C, Haupenthal J, Illarionov B, Andreas A, Awale M, Gierse RM, van der Laan T, van der Vlag R, Nasti R, Poizat M, Buhler E, Reiling N, Müller R, Fischer M, Reymond JL, Hirsch AKH. Zhu D, et al. Among authors: gierse rm. Chem Sci. 2022 Aug 8;13(36):10686-10698. doi: 10.1039/d2sc02371g. eCollection 2022 Sep 21. Chem Sci. 2022. PMID: 36320685 Free PMC article.
High Target Homology Does Not Guarantee Inhibition: Aminothiazoles Emerge as Inhibitors of Plasmodium falciparum.
Johannsen S, Gierse RM, Krüger A, Edwards RL, Nanna V, Fontana A, Zhu D, Masini T, de Carvalho LP, Poizat M, Kieftenbelt B, Hodge DM, Alvarez S, Bunt D, Lacour A, Shams A, Meissner KA, de Souza EE, Dröge M, van Vliet B, den Hartog J, Hutter MC, Held J, Odom John AR, Wrenger C, Hirsch AKH. Johannsen S, et al. Among authors: gierse rm. ACS Infect Dis. 2024 Mar 8;10(3):1000-1022. doi: 10.1021/acsinfecdis.3c00670. Epub 2024 Feb 17. ACS Infect Dis. 2024. PMID: 38367280 Free PMC article.
11 results