Results 11 to 20 of about 821 (130)

Repurposing FDA-Approved Compounds for the Discovery of Glutaminyl Cyclase Inhibitors as Drugs Against Alzheimer's Disease. [PDF]

ChemistryOpen, 2021
Alzheimer's disease (AD) is one of the most common neurodegenerative causes of dementia, the pathology of which is still not much clear. It′s challenging to discover the disease modifying agents for the prevention and treatment of AD over the years ...
Xu C, Zou H, Yu X, Xie Y, Cai J, Shang Q, Ouyang N, Wang Y, Xu P, He Z, Wu H.   +10 more
europepmc   +2 more sources

Functions of glutaminyl cyclase and its isoform in diseases

Visualized Cancer Medicine, 2023
Glutaminyl cyclase (QC; isoform: isoQC) is a zinc-dependent enzyme that catalyzes the intramolecular cyclization of N-terminal glutamine and glutamic acid residues into a pyroglutamate residue (pGlu).
Liu Yu’e, Shi Yufeng, Wang Ping
doaj   +2 more sources

Focal Cerebral Ischemia Induces Expression of Glutaminyl Cyclase along with Downstream Molecular and Cellular Inflammatory Responses. [PDF]

Cells
Glutaminyl cyclase (QC) and its isoenzyme (isoQC) catalyze the formation of N-terminal pyroglutamate (pGlu) from glutamine on a number of neuropeptides, peptide hormones and chemokines.
Höfling C, Ulrich L, Burghardt S, Donkersloot P, Opitz M, Geissler S, Schilling S, Cynis H, Michalski D, Roßner S.   +9 more
europepmc   +2 more sources

Pyroglutamation of cell surface proteins CD47 and TRP1 by glutaminyl cyclase modulates therapeutic antibody binding. [PDF]

Commun Biol
Monoclonal antibodies are important modalities in the treatment of cancer. Post-translational modifications of proteins, such as glycosylation, can affect the binding affinity of therapeutic antibodies.
van der Plas-van Duijn A, Winkelman LMT, Lensen C, van Duivendijk M, Derksen I, van Veenendaal JMF, Schaap G, Sluijter M, van Groningen TJB, van Doorn R, van Hall T, Slieker RC, Sharp TH, Beltman JB, Bresser K, Scheeren FA.   +15 more
europepmc   +2 more sources

Safety, tolerability and efficacy of the glutaminyl cyclase inhibitor PQ912 in Alzheimer's disease: results of a randomized, double-blind, placebo-controlled phase 2a study. [PDF]

Alzheimers Res Ther, 2018
Background PQ912 is an inhibitor of the glutaminyl cyclase enzyme that plays a central role in the formation of synaptotoxic pyroglutamate-A-beta oligomers.
Scheltens P, Hallikainen M, Grimmer T, Duning T, Gouw AA, Teunissen CE, Wink AM, Maruff P, Harrison J, van Baal CM, Bruins S, Lues I, Prins ND.   +12 more
europepmc   +2 more sources

Upregulation of Glutaminyl Cyclase Contributes to ERS-Induced Apoptosis in PC12 Cells. [PDF]

Biomed Res Int, 2022
Glutaminyl cyclase (QC) is responsible for converting the N‐terminal glutaminyl and glutamyl of the proteins into pyroglutamate (pE) through cyclization. It has been confirmed that QC catalyzes the formation of neurotoxic pE‐modified Aβ in the brain of AD patients.
Shang Q, Yu X, Ouyang N, Xu P, Chen X, Wang Y, Li C, Wang X, Lu X, Xu C, Wu H.   +10 more
europepmc   +3 more sources

Metal Ion Binding to Human Glutaminyl Cyclase: A Structural Perspective. [PDF]

Int J Mol Sci
Glutaminyl-peptide cyclotransferases (QCs) convert the N-terminal glutamine or glutamate residues of protein and peptide substrates into pyroglutamate (pE) by releasing ammonia or a water molecule. The N-terminal pE modification protects peptides/proteins against proteolytic degradation by amino- or exopeptidases, increasing their stability.
Tassone G, Pozzi C, Mangani S.
europepmc   +4 more sources

Rationale and study design of a randomized, placebo-controlled, double-blind phase 2b trial to evaluate efficacy, safety, and tolerability of an oral glutaminyl cyclase inhibitor varoglutamstat (PQ912) in study participants with MCI and mild AD-VIVIAD. [PDF]

Alzheimers Res Ther, 2021
Background Varoglutamstat (formerly PQ912) is a small molecule that inhibits the activity of the glutaminyl cyclase to reduce the level of pyroglutamate-A-beta (pGluAB42).
Vijverberg EGB, Axelsen TM, Bihlet AR, Henriksen K, Weber F, Fuchs K, Harrison JE, Kühn-Wache K, Alexandersen P, Prins ND, Scheltens P.   +10 more
europepmc   +2 more sources

Identification of Glutaminyl Cyclase Genes Involved in Pyroglutamate Modification of Fungal Lignocellulolytic Enzymes. [PDF]

mBio, 2017
The breakdown of plant biomass to simple sugars is essential for the production of second-generation biofuels and high-value bioproducts. Currently, enzymes produced from filamentous fungi are used for deconstructing plant cell wall polysaccharides into ...
Wu VW, Dana CM, Iavarone AT, Clark DS, Glass NL.   +4 more
europepmc   +2 more sources

Glutaminyl cyclases unfold glutamyl cyclase activity under mild acid conditions [PDF]

FEBS Letters, 2004
N‐terminal pyroglutamate (pGlu) formation from glutaminyl precursors is a posttranslational event in the processing of bioactive neuropeptides such as thyrotropin‐releasing hormone and neurotensin during their maturation in the secretory pathway. The reaction is facilitated by glutaminyl cyclase (QC), an enzyme highly abundant in mammalian brain. Here,
Stephan Schilling, Hans-Ulrich Demuth
exaly   +3 more sources