Astacin Proteases


  • Dorner J, Korn P, Gruhle K, Ramsbeck D, Garamus VM, Lilie H, Meister A, Schwieger C, Ihling C, Sinz A, Drescher S. A diazirine-modified membrane lipid to study peptide/lipid interactions - chances and challenges. Chemistry. 27 (2021), 59, Seite 14586-14593. doi: 10.1002/chem.202102048
  • Linnert M, Fritz C, Jäger C, Schlenzig D, Ramsbeck D, Kleinschmidt M, Wermann M, Demuth HU, Parthier C, Schilling S. Structure and dynamics of Meprin β in complex with a hydroxamate-based inhibitor. Int J Mol Sci. 22 (2021), 11, 5651. doi: 10.3390/ijms22115651
  • Ramsbeck D, Taudte N, Jänckel N, Strich S, Rahfeld J-U, Buchholz M. Tetrahydroimidazo[4,5-c]pyridine-based inhibitors of Porphyromonas gingivalis glutaminyl cyclase. Pharmaceuticals 14 (2021), 12, 1206. doi: 10.3390/ph14121206
  • Tan K, Jäger C, Körschgen H, Geissler S, Schlenzig D, Buchholz M, Stöcker W, Ramsbeck D. Heteroaromatic inhibitors of the astacin proteinases meprin α, meprin β and ovastacin discovered by a scaffold-hopping approach. ChemMedChem. (2021), 16, 6, Seite 976-988. doi: 10.1002/cmdc.202000822
  • Taudte N, Linnert M, Rahfeld J-U, Piechotta A, Ramsbeck D, Buchholz M, Kolenko P, Parthier C, Houston J A, Veillard F, Eick S, Potempa J, Schilling S, Demuth H-U, Stubbs M T. Mammalian-like type II glutaminyl cyclases in Porphyromonas gingivalis and other oral pathogenic bacteria as targets for treatment of periodontitis. J Biol Chem. (2021), 296, 100263. doi: 10.1016/j.jbc.2021.100263
  • Gnoth K, Piechotta A, Kleinschmidt M, Konrath S, Schenk M, Taudte N, Ramsbeck D, Nykiel V, Geißler S, Eichentopf R, Barendrecht S, Hartlage-Rübsamen M, Demuth H-U, Roßner S, Cynis H, Rahfeld J-U, Schilling S. Targeting isoaspartate-modified Aβ rescues behavioral deficits in transgenic mice with Alzheimer’s disease-like pathology. Alzheimer's research & therapy 12 (2020) Artikel-Nr.: 149, 20 Seiten.
  • Körschgen H, Jäger C, Tan K, Buchholz M, Stöcker W, Ramsbeck D. A Primary Evaluation of Potential Small-Molecule Inhibitors of the Astacin Metalloproteinase Ovastacin, a Novel Drug Target in Female Infertility Treatment. ChemMedChem, 2020; 15 (16): 1499-1504.
  • Kupski O, Funk L-M, Sautner V, Seifert F, Worbs B, Ramsbeck D, Meyer F, Diederichsen U, Buchholz M, Schilling S, Demuth H-U, Tittmann K. Hydrazides Are Potent Transition-State Analogues for Glutaminyl Cyclase Implicated in the Pathogenesis of Alzheimer's Disease. Biochemistry, 2020, 59(28): 2585-2591.
  • Tan K, Jäger C, Körschgen H, Geissler S, Schlenzig D, Buchholz M, Stöcker W, Ramsbeck D. Heteroaromatic Inhibitors of the Astacin Proteinases Meprin α, Meprin β and Ovastacin Discovered by a Scaffold-Hopping Approach. ChemMedChem 2020 Dec 23.
  • Schlenzig D, Cynis H, Hartlage-Rübsamen M, Zeitschel U, Menge K, Fothe A, Ramsbeck D, Spahn C, Wermann M, Roßner S, Buchholz M, Schilling S, Demuth HU. Dipeptidyl-Peptidase Activity of Meprin β Links N-truncation of Aβ With Glutaminyl Cyclase-Catalyzed pGlu-Aβ Formation. J Alzheimers Dis. 2018;66(1):359-375.
  • Schulze A, Wermann M, Demuth HU, Yoshimoto T, Ramsbeck D, Schlenzig D, Schilling S. Continuous Assays for Meprin Alpha and Beta Using Prolyl Tripeptidyl Aminopeptidase (PtP) From Porphyromonas Gingivalis. Anal Biochem. 2018 Oct 15;559:11-16. Epub 2018 Aug 9.
  • Tan K, Jäger C, Schlenzig D, Schilling S, Buchholz M, Ramsbeck D. Tertiary-Amine-Based Inhibitors of the Astacin Protease Meprin α. ChemMedChem. 2018 Aug 20;13(16):1619-1624. Epub 2018 Jul 16.
  • Ramsbeck D, Hamann A, Richter G, Schlenzig D, Geissler S, Nykiel V, Cynis H, Schilling S, Buchholz M. Structure-Guided Design, Synthesis, and Characterization of Next-Generation Meprin β Inhibitors. J Med Chem. 2018 May 24;61(10):4578-4592. Epub 2018 May 7.
  • Lindner S, Gruhle K, Schmidt R, Garamus VM, Ramsbeck D, Hause G, Meister A, Sinz A, Drescher S. Azide-Modified Membrane Lipids: Synthesis, Properties, and Reactivity. Langmuir. 2017 May 23;33(20):4960-4973. Epub 2017 May 10.
  • Ramsbeck D, Hamann A, Schlenzig D, Schilling S, Buchholz M. First Insight Into Structure-Activity Relationships of Selective Meprin β Inhibitors. Bioorg Med Chem Lett. 2017 Jun 1;27(11):2428-2431. Epub 2017 Apr 5.
  • Schlenzig D, Wermann M, Ramsbeck D, Moenke-Wedler T, Schilling S. Expression, Purification and Initial Characterization of Human Meprin β From Pichia Pastoris. Protein Expr Purif. 2015 Dec;116:75-81. Epub 2015 Aug 6.
  • Ramsbeck D, Buchholz M, Koch B, Böhme L, Hoffmann T, Demuth HU, Heiser U. Structure-activity Relationships of Benzimidazole-Based Glutaminyl Cyclase Inhibitors Featuring a Heteroaryl Scaffold. J Med Chem. 2013 Sep 12;56(17):6613-25. Epub 2013 Aug 19.
  • Drescher S, Ramsbeck D, Dobner B, Briel D. Selective Nucleophilic Substitution Reactions in 2,4,6-Trisulfanyl-Substituted Pyrimidine-5-carbonitriles by Secondary Amines. Journal of Heterocyclic Chemistry 44(4):757-763.