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Items: 31

1.

Glutaminyl Cyclase Inhibitor PQ912 Improves Cognition in Mouse Models of Alzheimer's Disease-Studies on Relation to Effective Target Occupancy.

Hoffmann T, Meyer A, Heiser U, Kurat S, Böhme L, Kleinschmidt M, Bühring KU, Hutter-Paier B, Farcher M, Demuth HU, Lues I, Schilling S.

J Pharmacol Exp Ther. 2017 Jul;362(1):119-130. doi: 10.1124/jpet.117.240614. Epub 2017 Apr 26.

PMID:
28446518
2.

Inhibition of CDK9 as a therapeutic strategy for inflammatory arthritis.

Hellvard A, Zeitlmann L, Heiser U, Kehlen A, Niestroj A, Demuth HU, Koziel J, Delaleu N, Jan Potempa, Mydel P.

Sci Rep. 2016 Aug 11;6:31441. doi: 10.1038/srep31441.

3.

Identifying neuropeptide Y (NPY) as the main stress-related substrate of dipeptidyl peptidase 4 (DPP4) in blood circulation.

Wagner L, Kaestner F, Wolf R, Stiller H, Heiser U, Manhart S, Hoffmann T, Rahfeld JU, Demuth HU, Rothermundt M, von Hörsten S.

Neuropeptides. 2016 Jun;57:21-34. doi: 10.1016/j.npep.2016.02.007. Epub 2016 Feb 27.

PMID:
26988064
4.

A phase 1 study to evaluate the safety and pharmacokinetics of PQ912, a glutaminyl cyclase inhibitor, in healthy subjects.

Lues I, Weber F, Meyer A, Bühring U, Hoffmann T, Kühn-Wache K, Manhart S, Heiser U, Pokorny R, Chiesa J, Glund K.

Alzheimers Dement (N Y). 2015 Oct 3;1(3):182-195. doi: 10.1016/j.trci.2015.08.002. eCollection 2015 Nov.

5.

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
6.

Inhibition of Glutaminyl Cyclases alleviates CCL2-mediated inflammation of non-alcoholic fatty liver disease in mice.

Cynis H, Kehlen A, Haegele M, Hoffmann T, Heiser U, Fujii M, Shibazaki Y, Yoneyama H, Schilling S, Demuth HU.

Int J Exp Pathol. 2013 Jun;94(3):217-25. doi: 10.1111/iep.12020. Epub 2013 Apr 8.

7.

Glutaminyl cyclases as novel targets for the treatment of septic arthritis.

Hellvard A, Maresz K, Schilling S, Graubner S, Heiser U, Jonsson R, Cynis H, Demuth HU, Potempa J, Mydel P.

J Infect Dis. 2013 Mar 1;207(5):768-77. doi: 10.1093/infdis/jis729. Epub 2012 Nov 29.

8.

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
9.

The isoenzyme of glutaminyl cyclase is an important regulator of monocyte infiltration under inflammatory conditions.

Cynis H, Hoffmann T, Friedrich D, Kehlen A, Gans K, Kleinschmidt M, Rahfeld JU, Wolf R, Wermann M, Stephan A, Haegele M, Sedlmeier R, Graubner S, Jagla W, Müller A, Eichentopf R, Heiser U, Seifert F, Quax PH, de Vries MR, Hesse I, Trautwein D, Wollert U, Berg S, Freyse EJ, Schilling S, Demuth HU.

EMBO Mol Med. 2011 Sep;3(9):545-58. doi: 10.1002/emmm.201100158. Epub 2011 Jul 20.

10.

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
11.

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
12.

Glutaminyl cyclase inhibition attenuates pyroglutamate Abeta and Alzheimer's disease-like pathology.

Schilling S, Zeitschel U, Hoffmann T, Heiser U, Francke M, Kehlen A, Holzer M, Hutter-Paier B, Prokesch M, Windisch M, Jagla W, Schlenzig D, Lindner C, Rudolph T, Reuter G, Cynis H, Montag D, Demuth HU, Rossner S.

Nat Med. 2008 Oct;14(10):1106-11. doi: 10.1038/nm.1872. Epub 2008 Sep 28.

PMID:
18836460
13.

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.

14.

Novel inhibitor for prolyl tripeptidyl aminopeptidase from Porphyromonas gingivalis and details of substrate-recognition mechanism.

Xu Y, Nakajima Y, Ito K, Zheng H, Oyama H, Heiser U, Hoffmann T, Gärtner UT, Demuth HU, Yoshimoto T.

J Mol Biol. 2008 Jan 18;375(3):708-19. Epub 2007 Oct 3.

PMID:
18042490
15.

Does human attractin have DP4 activity?

Friedrich D, Hoffmann T, Bär J, Wermann M, Manhart S, Heiser U, Demuth HU.

Biol Chem. 2007 Feb;388(2):155-62.

PMID:
17261078
16.

Neuropeptide Y (NPY) cleaving enzymes: structural and functional homologues of dipeptidyl peptidase 4.

Frerker N, Wagner L, Wolf R, Heiser U, Hoffmann T, Rahfeld JU, Schade J, Karl T, Naim HY, Alfalah M, Demuth HU, von Hörsten S.

Peptides. 2007 Feb;28(2):257-68. Epub 2007 Jan 16.

PMID:
17223229
17.

Inhibition of glutaminyl cyclase alters pyroglutamate formation in mammalian cells.

Cynis H, Schilling S, Bodnár M, Hoffmann T, Heiser U, Saido TC, Demuth HU.

Biochim Biophys Acta. 2006 Oct;1764(10):1618-25. Epub 2006 Aug 16.

PMID:
17005457
18.

Effects of dipeptidyl peptidase IV on the satiety actions of peptide YY.

Unniappan S, McIntosh CH, Demuth HU, Heiser U, Wolf R, Kieffer TJ.

Diabetologia. 2006 Aug;49(8):1915-23. Epub 2006 Jun 27.

PMID:
16802131
19.

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
20.

Rigidity and flexibility of dipeptidyl peptidase IV: crystal structures of and docking experiments with DPIV.

Engel M, Hoffmann T, Manhart S, Heiser U, Chambre S, Huber R, Demuth HU, Bode W.

J Mol Biol. 2006 Jan 27;355(4):768-83. Epub 2005 Nov 22.

PMID:
16330047
21.

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
22.

Temperature-dependent behavior of a symmetric long-chain bolaamphiphile with phosphocholine headgroups in water: from hydrogel to nanoparticles.

Köhler K, Förster G, Hauser A, Dobner B, Heiser UF, Ziethe F, Richter W, Steiniger F, Drechsler M, Stettin H, Blume A.

J Am Chem Soc. 2004 Dec 29;126(51):16804-13.

PMID:
15612719
23.

Self-assembly in a bipolar phosphocholine-water system: the formation of nanofibers and hydrogels.

Köhler K, Förster G, Hauser A, Dobner B, Heiser UF, Ziethe F, Richter W, Steiniger F, Drechsler M, Stettin H, Blume A.

Angew Chem Int Ed Engl. 2004 Jan;43(2):245-7. No abstract available.

PMID:
14695621
24.

The crystal structure of dipeptidyl peptidase IV (CD26) reveals its functional regulation and enzymatic mechanism.

Engel M, Hoffmann T, Wagner L, Wermann M, Heiser U, Kiefersauer R, Huber R, Bode W, Demuth HU, Brandstetter H.

Proc Natl Acad Sci U S A. 2003 Apr 29;100(9):5063-8. Epub 2003 Apr 10.

25.

Acylated hydroxamates as selective and highly potent inhibitors of dipeptidyl peptidase I.

Niestroj AJ, Schlenzig D, Heiser U, Kühn-Wache K, Cigic B, Werman M, Hoffmann T, Gerhartz B, Demuth HU.

Adv Exp Med Biol. 2003;524:339-43. No abstract available.

PMID:
12675256
26.
27.

Modulation of inositol 1,4,5-triphosphate concentration by prolyl endopeptidase inhibition.

Schulz I, Gerhartz B, Neubauer A, Holloschi A, Heiser U, Hafner M, Demuth HU.

Eur J Biochem. 2002 Dec;269(23):5813-20.

28.

Inhibition of mammalian legumain by Michael acceptors and AzaAsn-halomethylketones.

Niestroj AJ, Feussner K, Heiser U, Dando PM, Barrett A, Gerhartz B, Demuth HU.

Biol Chem. 2002 Jul-Aug;383(7-8):1205-14.

PMID:
12437107
29.

Continuous spectrometric assays for glutaminyl cyclase activity.

Schilling S, Hoffmann T, Wermann M, Heiser U, Wasternack C, Demuth HU.

Anal Biochem. 2002 Apr 1;303(1):49-56.

PMID:
11906150
30.

Phase transitions and hydrogen bonding in a bipolar phosphocholine evidenced by calorimetry and vibrational spectroscopy.

Pohle W, Selle C, Rettig W, Heiser U, Dobner B, Wartewig S.

Arch Biochem Biophys. 2001 Dec 15;396(2):151-61.

PMID:
11747292
31.

Metabolism of glucagon by dipeptidyl peptidase IV (CD26).

Pospisilik JA, Hinke SA, Pederson RA, Hoffmann T, Rosche F, Schlenzig D, Glund K, Heiser U, McIntosh CH, Demuth H.

Regul Pept. 2001 Jan 12;96(3):133-41.

PMID:
11111019

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