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Items: 17

1.

Expression of human and Porphyromonas gingivalis glutaminyl cyclases in periodontitis and rheumatoid arthritis-A pilot study.

Bender P, Egger A, Westermann M, Taudte N, Sculean A, Potempa J, Möller B, Buchholz M, Eick S.

Arch Oral Biol. 2019 Jan;97:223-230. doi: 10.1016/j.archoralbio.2018.10.022. Epub 2018 Oct 28.

PMID:
30399509
2.

Dipeptidyl-Peptidase Activity of Meprin β Links N-truncation of Aβ with Glutaminyl Cyclase-Catalyzed pGlu-Aβ Formation.

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.

J Alzheimers Dis. 2018;66(1):359-375. doi: 10.3233/JAD-171183.

PMID:
30320570
3.

Tertiary-Amine-Based Inhibitors of the Astacin Protease Meprin α.

Tan K, Jäger C, Schlenzig D, Schilling S, Buchholz M, Ramsbeck D.

ChemMedChem. 2018 Aug 20;13(16):1619-1624. doi: 10.1002/cmdc.201800300. Epub 2018 Jul 16.

PMID:
29927060
4.

Structure-Guided Design, Synthesis, and Characterization of Next-Generation Meprin β Inhibitors.

Ramsbeck D, Hamann A, Richter G, Schlenzig D, Geissler S, Nykiel V, Cynis H, Schilling S, Buchholz M.

J Med Chem. 2018 May 24;61(10):4578-4592. doi: 10.1021/acs.jmedchem.8b00330. Epub 2018 May 7.

PMID:
29694039
5.
6.

3-Hydroxy-N'-arylidenepropanehydrazonamides with Halo-Substituted Phenanthrene Scaffolds Cure P. berghei Infected Mice When Administered Perorally.

Leven M, Knaab TC, Held J, Duffy S, Meister S, Fischli C, Meitzner D, Lehmann U, Lungerich B, Kuna K, Stahlke P, Delves MJ, Buchholz M, Winzeler EA, Avery VM, Mordmüller B, Wittlin S, Kurz T.

J Med Chem. 2017 Jul 27;60(14):6036-6044. doi: 10.1021/acs.jmedchem.7b00140. Epub 2017 Jul 17.

PMID:
28653845
7.

First insight into structure-activity relationships of selective meprin β inhibitors.

Ramsbeck D, Hamann A, Schlenzig D, Schilling S, Buchholz M.

Bioorg Med Chem Lett. 2017 Jun 1;27(11):2428-2431. doi: 10.1016/j.bmcl.2017.04.012. Epub 2017 Apr 5.

PMID:
28408220
8.

Natural Products from Microalgae with Potential against Alzheimer's Disease: Sulfolipids Are Potent Glutaminyl Cyclase Inhibitors.

Hielscher-Michael S, Griehl C, Buchholz M, Demuth HU, Arnold N, Wessjohann LA.

Mar Drugs. 2016 Nov 2;14(11). pii: E203.

9.

11th German Conference on Chemoinformatics (GCC 2015) : Fulda, Germany. 8-10 November 2015.

Fechner U, de Graaf C, Torda AE, Güssregen S, Evers A, Matter H, Hessler G, Richmond NJ, Schmidtke P, Segler MHS, Waller MP, Pleik S, Shea JE, Levine Z, Mullen R, van den Broek K, Epple M, Kuhn H, Truszkowski A, Zielesny A, Fraaije JH, Gracia RS, Kast SM, Bulusu KC, Bender A, Yosipof A, Nahum O, Senderowitz H, Krotzky T, Schulz R, Wolber G, Bietz S, Rarey M, Zimmermann MO, Lange A, Ruff M, Heidrich J, Onlia I, Exner TE, Boeckler FM, Bermudez M, Firaha DS, Hollóczki O, Kirchner B, Tautermann CS, Volkamer A, Eid S, Turk S, Rippmann F, Fulle S, Saleh N, Saladino G, Gervasio FL, Haensele E, Banting L, Whitley DC, Oliveira Santos JS, Bureau R, Clark T, Sandmann A, Lanig H, Kibies P, Heil J, Hoffgaard F, Frach R, Engel J, Smith S, Basu D, Rauh D, Kohlbacher O, Boeckler FM, Essex JW, Bodnarchuk MS, Ross GA, Finkelmann AR, Göller AH, Schneider G, Husch T, Schütter C, Balducci A, Korth M, Ntie-Kang F, Günther S, Sippl W, Mbaze LM, Ntie-Kang F, Simoben CV, Lifongo LL, Ntie-Kang F, Judson P, Barilla J, Lokajíček MV, Pisaková H, Simr P, Kireeva N, Petrov A, Ostroumov D, Solovev VP, Pervov VS, Friedrich NO, Sommer K, Rarey M, Kirchmair J, Proschak E, Weber J, Moser D, Kalinowski L, Achenbach J, Mackey M, Cheeseright T, Renner G, Renner G, Schmidt TC, Schram J, Egelkraut-Holtus M, van Oeyen A, Kalliokoski T, Fourches D, Ibezim A, Mbah CJ, Adikwu UM, Nwodo NJ, Steudle A, Masek BB, Nagy S, Baker D, Soltanshahi F, Dorfman R, Dubrucq K, Patel H, Koch O, Mrugalla F, Kast SM, Ain QU, Fuchs JE, Owen RM, Omoto K, Torella R, Pryde DC, Glen R, Bender A, Hošek P, Spiwok V, Mervin LH, Barrett I, Firth M, Murray DC, McWilliams L, Cao Q, Engkvist O, Warszycki D, Śmieja M, Bojarski AJ, Aniceto N, Freitas A, Ghafourian T, Herrmann G, Eigner-Pitto V, Naß A, Kurczab R, Bojarski AJ, Lange A, Günther MB, Hennig S, Büttner FM, Schall C, Sievers-Engler A, Ansideri F, Koch P, Stehle T, Laufer S, Böckler FM, Zdrazil B, Montanari F, Ecker GF, Grebner C, Hogner A, Ulander J, Edman K, Guallar V, Tyrchan C, Ulander J, Tyrchan C, Klute W, Bergström F, Kramer C, Nguyen QD, Frach R, Kibies P, Strohfeldt S, Böttcher S, Pongratz T, Horinek D, Kast SM, Rupp B, Al-Yamori R, Lisurek M, Kühne R, Furtado F, van den Broek K, Wessjohann L, Mathea M, Baumann K, Mohamad-Zobir SZ, Fu X, Fan TP, Bender A, Kuhn MA, Sotriffer CA, Zoufir A, Li X, Mervin L, Berg E, Polokoff M, Ihlenfeldt WD, Ihlenfeldt WD, Pretzel J, Alhalabi Z, Fraczkiewicz R, Waldman M, Clark RD, Shaikh N, Garg P, Kos A, Himmler HJ, Sandmann A, Jardin C, Sticht H, Steinbrecher TB, Dahlgren M, Cappel D, Lin T, Wang L, Krilov G, Abel R, Friesner R, Sherman W, Pöhner IA, Panecka J, Wade RC, Bietz S, Schomburg KT, Hilbig M, Rarey M, Jäger C, Wieczorek V, Westerhoff LM, Borbulevych OY, Demuth HU, Buchholz M, Schmidt D, Rickmeyer T, Krotzky T, Kolb P, Mittal S, Sánchez-García E, Nogueira MS, Oliveira TB, da Costa FB, Schmidt TJ.

J Cheminform. 2016 Apr 26;8(Suppl 1):18. doi: 10.1186/s13321-016-0119-5. No abstract available.

10.

Structure-activity relationships of benzimidazole-based glutaminyl cyclase inhibitors featuring a heteroaryl scaffold.

Ramsbeck D, Buchholz M, Koch B, Böhme L, Hoffmann T, Demuth HU, Heiser U.

J Med Chem. 2013 Sep 12;56(17):6613-25. doi: 10.1021/jm4001709. Epub 2013 Aug 19.

PMID:
23886302
11.

Probing secondary glutaminyl cyclase (QC) inhibitor interactions applying an in silico-modeling/site-directed mutagenesis approach: implications for drug development.

Koch B, Buchholz M, Wermann M, Heiser U, Schilling S, Demuth HU.

Chem Biol Drug Des. 2012 Dec;80(6):937-46. doi: 10.1111/cbdd.12046. Epub 2012 Oct 11.

PMID:
22967026
12.

Crystal structures of glutaminyl cyclases (QCs) from Drosophila melanogaster reveal active site conservation between insect and mammalian QCs.

Koch B, Kolenko P, Buchholz M, Carrillo DR, Parthier C, Wermann M, Rahfeld JU, Reuter G, Schilling S, Stubbs MT, Demuth HU.

Biochemistry. 2012 Sep 18;51(37):7383-92. doi: 10.1021/bi300687g. Epub 2012 Sep 5.

PMID:
22897232
13.

Structures of glycosylated mammalian glutaminyl cyclases reveal conformational variability near the active center.

Ruiz-Carrillo D, Koch B, Parthier C, Wermann M, Dambe T, Buchholz M, Ludwig HH, Heiser U, Rahfeld JU, Stubbs MT, Schilling S, Demuth HU.

Biochemistry. 2011 Jul 19;50(28):6280-8. doi: 10.1021/bi200249h. Epub 2011 Jun 27.

PMID:
21671571
14.

Inhibitors for human glutaminyl cyclase by structure based design and bioisosteric replacement.

Buchholz M, Hamann A, Aust S, Brandt W, Böhme L, Hoffmann T, Schilling S, Demuth HU, Heiser U.

J Med Chem. 2009 Nov 26;52(22):7069-80. doi: 10.1021/jm900969p.

PMID:
19863057
15.

Inhibition of glutaminyl cyclase prevents pGlu-Abeta formation after intracortical/hippocampal microinjection in vivo/in situ.

Schilling S, Appl T, Hoffmann T, Cynis H, Schulz K, Jagla W, Friedrich D, Wermann M, Buchholz M, Heiser U, von Hörsten S, Demuth HU.

J Neurochem. 2008 Aug;106(3):1225-36. doi: 10.1111/j.1471-4159.2008.05471.x. Epub 2008 Jul 8.

16.

The first potent inhibitors for human glutaminyl cyclase: synthesis and structure-activity relationship.

Buchholz M, Heiser U, Schilling S, Niestroj AJ, Zunkel K, Demuth HU.

J Med Chem. 2006 Jan 26;49(2):664-77.

PMID:
16420052
17.

Isolation, catalytic properties, and competitive inhibitors of the zinc-dependent murine glutaminyl cyclase.

Schilling S, Cynis H, von Bohlen A, Hoffmann T, Wermann M, Heiser U, Buchholz M, Zunkel K, Demuth HU.

Biochemistry. 2005 Oct 11;44(40):13415-24.

PMID:
16201766

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