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Items: 1 to 20 of 89

1.

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
2.

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
3.

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
4.

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
5.

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
6.

Identification of human glutaminyl cyclase as a metalloenzyme. Potent inhibition by imidazole derivatives and heterocyclic chelators.

Schilling S, Niestroj AJ, Rahfeld JU, Hoffmann T, Wermann M, Zunkel K, Wasternack C, Demuth HU.

J Biol Chem. 2003 Dec 12;278(50):49773-9. Epub 2003 Sep 30.

7.

Inhibitory effect of flavonoids on human glutaminyl cyclase.

Li M, Dong Y, Yu X, Zou Y, Zheng Y, Bu X, Quan J, He Z, Wu H.

Bioorg Med Chem. 2016 May 15;24(10):2280-6. doi: 10.1016/j.bmc.2016.03.064. Epub 2016 Apr 1.

PMID:
27061673
8.

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
9.

Identification of potential glutaminyl cyclase inhibitors from lead-like libraries by in silico and in vitro fragment-based screening.

Szaszkó M, Hajdú I, Flachner B, Dobi K, Magyar C, Simon I, Lőrincz Z, Kapui Z, Pázmány T, Cseh S, Dormán G.

Mol Divers. 2017 Feb;21(1):175-186. doi: 10.1007/s11030-016-9717-4. Epub 2017 Jan 9.

PMID:
28070724
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.

Design of benzimidazole- and benzoxazole-2-thione derivatives as inhibitors of bacterial hyaluronan lyase.

Braun S, Botzki A, Salmen S, Textor C, Bernhardt G, Dove S, Buschauer A.

Eur J Med Chem. 2011 Sep;46(9):4419-29. doi: 10.1016/j.ejmech.2011.07.014. Epub 2011 Jul 19.

PMID:
21803461
12.

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.

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.

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
15.

Benzimidazole derivatives as new serotonin 5-HT6 receptor antagonists. Molecular mechanisms of receptor inactivation.

de la Fuente T, Martín-Fontecha M, Sallander J, Benhamú B, Campillo M, Medina RA, Pellissier LP, Claeysen S, Dumuis A, Pardo L, López-Rodríguez ML.

J Med Chem. 2010 Feb 11;53(3):1357-69. doi: 10.1021/jm901672k.

PMID:
20078106
16.

Identification of novel benzimidazole derivatives as inhibitors of leukotriene biosynthesis by virtual screening targeting 5-lipoxygenase-activating protein (FLAP).

Banoglu E, Çalişkan B, Luderer S, Eren G, Özkan Y, Altenhofen W, Weinigel C, Barz D, Gerstmeier J, Pergola C, Werz O.

Bioorg Med Chem. 2012 Jun 15;20(12):3728-41. doi: 10.1016/j.bmc.2012.04.048. Epub 2012 May 1.

PMID:
22607880
17.

Potent and highly selective benzimidazole inhibitors of PI3-kinase delta.

Murray JM, Sweeney ZK, Chan BK, Balazs M, Bradley E, Castanedo G, Chabot C, Chantry D, Flagella M, Goldstein DM, Kondru R, Lesnick J, Li J, Lucas MC, Nonomiya J, Pang J, Price S, Salphati L, Safina B, Savy PP, Seward EM, Ultsch M, Sutherlin DP.

J Med Chem. 2012 Sep 13;55(17):7686-95. doi: 10.1021/jm300717c. Epub 2012 Aug 21.

PMID:
22877085
18.

Design, synthesis, molecular docking and biological evaluation of new dithiocarbamates substituted benzimidazole and chalcones as possible chemotherapeutic agents.

Bacharaju K, Jambula SR, Sivan S, Jyostnatangeda S, Manga V.

Bioorg Med Chem Lett. 2012 May 1;22(9):3274-7. doi: 10.1016/j.bmcl.2012.03.018. Epub 2012 Mar 11.

PMID:
22460028
19.

New benzimidazole derivatives as antiplasmodial agents and plasmepsin inhibitors: synthesis and analysis of structure-activity relationships.

Saify ZS, Azim MK, Ahmad W, Nisa M, Goldberg DE, Hussain SA, Akhtar S, Akram A, Arayne A, Oksman A, Khan IA.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1282-6. doi: 10.1016/j.bmcl.2011.10.018. Epub 2011 Oct 20.

PMID:
22204908
20.

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

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