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Items: 1 to 20 of 106

1.

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
2.

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
3.

Structures of human Golgi-resident glutaminyl cyclase and its complexes with inhibitors reveal a large loop movement upon inhibitor binding.

Huang KF, Liaw SS, Huang WL, Chia CY, Lo YC, Chen YL, Wang AH.

J Biol Chem. 2011 Apr 8;286(14):12439-49. doi: 10.1074/jbc.M110.208595. Epub 2011 Feb 1.

4.

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
5.

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
6.

Structural and functional analyses of a glutaminyl cyclase from Ixodes scapularis reveal metal-independent catalysis and inhibitor binding.

Huang KF, Hsu HL, Karim S, Wang AH.

Acta Crystallogr D Biol Crystallogr. 2014 Mar;70(Pt 3):789-801. doi: 10.1107/S1399004713033488. Epub 2014 Feb 22.

PMID:
24598748
7.

Crystal structure and functional analysis of the glutaminyl cyclase from Xanthomonas campestris.

Huang WL, Wang YR, Ko TP, Chia CY, Huang KF, Wang AH.

J Mol Biol. 2010 Aug 20;401(3):374-88. doi: 10.1016/j.jmb.2010.06.012. Epub 2010 Jun 15.

PMID:
20558177
8.

Mammalian glutaminyl cyclases and their isoenzymes have identical enzymatic characteristics.

Stephan A, Wermann M, von Bohlen A, Koch B, Cynis H, Demuth HU, Schilling S.

FEBS J. 2009 Nov;276(22):6522-36. doi: 10.1111/j.1742-4658.2009.07337.x. Epub 2009 Oct 5.

9.

Crystal structures of human glutaminyl cyclase, an enzyme responsible for protein N-terminal pyroglutamate formation.

Huang KF, Liu YL, Cheng WJ, Ko TP, Wang AH.

Proc Natl Acad Sci U S A. 2005 Sep 13;102(37):13117-22. Epub 2005 Aug 31.

10.

The soluble Y115E-Y117E variant of human glutaminyl cyclase is a valid target for X-ray and NMR screening of inhibitors against Alzheimer disease.

DiPisa F, Pozzi C, Benvenuti M, Andreini M, Marconi G, Mangani S.

Acta Crystallogr F Struct Biol Commun. 2015 Aug;71(Pt 8):986-92. doi: 10.1107/S2053230X15010389. Epub 2015 Jul 28.

PMID:
26249687
11.

Inhibition of glutaminyl cyclase attenuates cell migration modulated by monocyte chemoattractant proteins.

Chen YL, Huang KF, Kuo WC, Lo YC, Lee YM, Wang AH.

Biochem J. 2012 Mar 1;442(2):403-12. doi: 10.1042/BJ20110535.

PMID:
22060158
12.

Glutaminyl cyclase knock-out mice exhibit slight hypothyroidism but no hypogonadism: implications for enzyme function and drug development.

Schilling S, Kohlmann S, Bäuscher C, Sedlmeier R, Koch B, Eichentopf R, Becker A, Cynis H, Hoffmann T, Berg S, Freyse EJ, von Hörsten S, Rossner S, Graubner S, Demuth HU.

J Biol Chem. 2011 Apr 22;286(16):14199-208. doi: 10.1074/jbc.M111.229385. Epub 2011 Feb 17.

13.

Amyloidogenic processing of amyloid precursor protein: evidence of a pivotal role of glutaminyl cyclase in generation of pyroglutamate-modified amyloid-beta.

Cynis H, Scheel E, Saido TC, Schilling S, Demuth HU.

Biochemistry. 2008 Jul 15;47(28):7405-13. doi: 10.1021/bi800250p. Epub 2008 Jun 21.

PMID:
18570439
14.

Crystal structure of human ABAD/HSD10 with a bound inhibitor: implications for design of Alzheimer's disease therapeutics.

Kissinger CR, Rejto PA, Pelletier LA, Thomson JA, Showalter RE, Abreo MA, Agree CS, Margosiak S, Meng JJ, Aust RM, Vanderpool D, Li B, Tempczyk-Russell A, Villafranca JE.

J Mol Biol. 2004 Sep 17;342(3):943-52.

PMID:
15342248
15.

Overexpression of glutaminyl cyclase, the enzyme responsible for pyroglutamate A{beta} formation, induces behavioral deficits, and glutaminyl cyclase knock-out rescues the behavioral phenotype in 5XFAD mice.

Jawhar S, Wirths O, Schilling S, Graubner S, Demuth HU, Bayer TA.

J Biol Chem. 2011 Feb 11;286(6):4454-60. doi: 10.1074/jbc.M110.185819. Epub 2010 Dec 10.

16.

Structure-activity relationship of human glutaminyl cyclase inhibitors having an N-(5-methyl-1H-imidazol-1-yl)propyl thiourea template.

Tran PT, Hoang VH, Thorat SA, Kim SE, Ann J, Chang YJ, Nam DW, Song H, Mook-Jung I, Lee J, Lee J.

Bioorg Med Chem. 2013 Jul 1;21(13):3821-30. doi: 10.1016/j.bmc.2013.04.005. Epub 2013 Apr 17.

PMID:
23643900
17.

A conserved hydrogen-bond network in the catalytic centre of animal glutaminyl cyclases is critical for catalysis.

Huang KF, Wang YR, Chang EC, Chou TL, Wang AH.

Biochem J. 2008 Apr 1;411(1):181-90.

PMID:
18072935
18.

Heterologous expression and characterization of human glutaminyl cyclase: evidence for a disulfide bond with importance for catalytic activity.

Schilling S, Hoffmann T, Rosche F, Manhart S, Wasternack C, Demuth HU.

Biochemistry. 2002 Sep 3;41(35):10849-57.

PMID:
12196024
19.

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
20.

Thermodynamic cycle analysis and inhibitor design against beta-lactamase.

Roth TA, Minasov G, Morandi S, Prati F, Shoichet BK.

Biochemistry. 2003 Dec 16;42(49):14483-91.

PMID:
14661960
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