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Design, Synthesis and Biological Characterization of Histone Deacetylase 8 (HDAC8) Proteolysis Targeting Chimeras (PROTACs) with Anti-Neuroblastoma Activity.
Darwish S, Ghazy E, Heimburg T, Herp D, Zeyen P, Salem-Altintas R, Ridinger J, Robaa D, Schmidtkunz K, Erdmann F, Schmidt M, Romier C, Jung M, Oehme I, Sippl W. Darwish S, et al. Among authors: schmidtkunz k. Int J Mol Sci. 2022 Jul 7;23(14):7535. doi: 10.3390/ijms23147535. Int J Mol Sci. 2022. PMID: 35886887 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.
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.
Identification of a small-molecule ligand of the epigenetic reader protein Spindlin1 via a versatile screening platform.
Wagner T, Greschik H, Burgahn T, Schmidtkunz K, Schott AK, McMillan J, Baranauskienė L, Xiong Y, Fedorov O, Jin J, Oppermann U, Matulis D, Schüle R, Jung M. Wagner T, et al. Among authors: schmidtkunz k. Nucleic Acids Res. 2016 May 19;44(9):e88. doi: 10.1093/nar/gkw089. Epub 2016 Feb 17. Nucleic Acids Res. 2016. PMID: 26893353 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
Metabolic Response to XD14 Treatment in Human Breast Cancer Cell Line MCF-7.
Pan D, Kather M, Willmann L, Schlimpert M, Bauer C, Lagies S, Schmidtkunz K, Eisenhardt SU, Jung M, Günther S, Kammerer B. Pan D, et al. Among authors: schmidtkunz k. Int J Mol Sci. 2016 Oct 24;17(10):1772. doi: 10.3390/ijms17101772. Int J Mol Sci. 2016. PMID: 27783056 Free PMC article.
32 results