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Synthesis and Biological Investigation of Phenothiazine-Based Benzhydroxamic Acids as Selective Histone Deacetylase 6 Inhibitors.
Vögerl K, Ong N, Senger J, Herp D, Schmidtkunz K, Marek M, Müller M, Bartel K, Shaik TB, Porter NJ, Robaa D, Christianson DW, Romier C, Sippl W, Jung M, Bracher F. Vögerl K, et al. Among authors: schmidtkunz k. J Med Chem. 2019 Feb 14;62(3):1138-1166. doi: 10.1021/acs.jmedchem.8b01090. Epub 2019 Feb 1. J Med Chem. 2019. PMID: 30645113 Free PMC article.
Structural basis for the inhibition of histone deacetylase 8 (HDAC8), a key epigenetic player in the blood fluke Schistosoma mansoni.
Marek M, Kannan S, Hauser AT, Moraes Mourão M, Caby S, Cura V, Stolfa DA, Schmidtkunz K, Lancelot J, Andrade L, Renaud JP, Oliveira G, Sippl W, Jung M, Cavarelli J, Pierce RJ, Romier C. Marek M, et al. Among authors: schmidtkunz k. PLoS Pathog. 2013;9(9):e1003645. doi: 10.1371/journal.ppat.1003645. Epub 2013 Sep 26. PLoS Pathog. 2013. PMID: 24086136 Free PMC article.
4-Acyl pyrroles: mimicking acetylated lysines in histone code reading.
Lucas X, Wohlwend D, Hügle M, Schmidtkunz K, Gerhardt S, Schüle R, Jung M, Einsle O, Günther S. Lucas X, et al. Among authors: schmidtkunz k. Angew Chem Int Ed Engl. 2013 Dec 23;52(52):14055-9. doi: 10.1002/anie.201307652. Epub 2013 Nov 24. Angew Chem Int Ed Engl. 2013. PMID: 24272870 No abstract available.
The discovery of a highly selective 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one SIRT2 inhibitor that is neuroprotective in an in vitro Parkinson's disease model.
Di Fruscia P, Zacharioudakis E, Liu C, Moniot S, Laohasinnarong S, Khongkow M, Harrison IF, Koltsida K, Reynolds CR, Schmidtkunz K, Jung M, Chapman KL, Steegborn C, Dexter DT, Sternberg MJ, Lam EW, Fuchter MJ. Di Fruscia P, et al. Among authors: schmidtkunz k. ChemMedChem. 2015 Jan;10(1):69-82. doi: 10.1002/cmdc.201402431. Epub 2014 Nov 13. ChemMedChem. 2015. PMID: 25395356
Selective Sirt2 inhibition by ligand-induced rearrangement of the active site.
Rumpf T, Schiedel M, Karaman B, Roessler C, North BJ, Lehotzky A, Oláh J, Ladwein KI, Schmidtkunz K, Gajer M, Pannek M, Steegborn C, Sinclair DA, Gerhardt S, Ovádi J, Schutkowski M, Sippl W, Einsle O, Jung M. Rumpf T, et al. Among authors: schmidtkunz k. Nat Commun. 2015 Feb 12;6:6263. doi: 10.1038/ncomms7263. Nat Commun. 2015. PMID: 25672491 Free PMC article.
Tofacitinib and analogs as inhibitors of the histone kinase PRK1 (PKN1).
Ostrovskyi D, Rumpf T, Eib J, Lumbroso A, Slynko I, Klaeger S, Heinzlmeir S, Forster M, Gehringer M, Pfaffenrot E, Bauer SM, Schmidtkunz K, Wenzler S, Metzger E, Kuster B, Laufer S, Schüle R, Sippl W, Breit B, Jung M. Ostrovskyi D, et al. Among authors: schmidtkunz k. Future Med Chem. 2016 Sep;8(13):1537-51. doi: 10.4155/fmc-2016-0132. Epub 2016 Aug 30. Future Med Chem. 2016. PMID: 27572962
32 results