Discovery of highly potent human glutaminyl cyclase (QC) inhibitors as anti-Alzheimer's agents by the combination of pharmacophore-based and structure-based design.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113819
Abstract: The inhibition of glutaminyl cyclase (QC) may provide a promising strategy for the treatment of early Alzheimer's disease (AD) by reducing the amount of the toxic pyroform of β-amyloid (AβΝ3pE) in the brains of AD… read more here.
Keywords: glutaminyl cyclase; highly potent; potent human; cyclase ... See more keywords
Piperidine-4-carboxamide as a new scaffold for designing secretory glutaminyl cyclase inhibitors.
Sign Up to like & getrecommendations! Published in 2020 at "International journal of biological macromolecules"
DOI: 10.1016/j.ijbiomac.2020.12.118
Abstract: Alzheimer's disease (AD), a common chronic neurodegenerative disease, has become a major public health concern. Despite years of research, therapeutics for AD are limited. Overexpression of secretory glutaminyl cyclase (sQC) in AD brain leads to… read more here.
Keywords: glutaminyl cyclase; carboxamide new; new scaffold; piperidine carboxamide ... See more keywords
Concerted action of dipeptidyl peptidase IV and glutaminyl cyclase results in formation of pyroglutamate-modified amyloid peptides in vitro
Sign Up to like & getrecommendations! Published in 2018 at "Neurochemistry International"
DOI: 10.1016/j.neuint.2017.12.001
Abstract: &NA; Compelling evidence suggests a crucial role of amyloid beta peptides (A&bgr;(1‐40/42)) in the etiology of Alzheimer's disease (AD). The N‐terminal truncation of A&bgr;(1‐40/42) and their modification, e.g. by glutaminyl cyclase (QC), is expected to… read more here.
Keywords: glutaminyl cyclase; dipeptidyl peptidase; bgr; formation ... See more keywords
Human Glutaminyl Cyclase: Structure, Function, Inhibitors and Involvement in Alzheimer's Disease.
Sign Up to like & getrecommendations! Published in 2019 at "Pharmacological research"
DOI: 10.1016/j.phrs.2019.104342
Abstract: Human glutaminyl cyclase (hQC) is an important enzyme for post-translational modification by converting the N-terminal glutaminyl and glutamyl into its pyroglutamate (pGlu) through cyclization. The two isoforms of hQC, secretory glutaminyl cyclase (sQC) and golgi… read more here.
Keywords: glutaminyl cyclase; function inhibitors; alzheimer disease; human glutaminyl ... See more keywords
Glutaminyl Cyclase, Diseases, and Development of Glutaminyl Cyclase Inhibitors.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00325
Abstract: Pyroglutamate (pE) modification, catalyzed mainly by glutaminyl cyclase (QC), is prevalent throughout nature and is particularly important in mammals including humans for the maturation of hormones, peptides, and proteins. In humans, the upregulation of QC… read more here.
Keywords: glutaminyl cyclase; diseases development; cyclase diseases; cyclase ... See more keywords
Discovery of Conformationally Restricted Human Glutaminyl Cyclase Inhibitors as Potent Anti-Alzheimer's Agents by Structure-Based Design.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b00751
Abstract: Alzheimer's disease (AD) is an incurable, progressive neurodegenerative disease whose pathogenesis cannot be defined by one single element but consist of various factors; thus, there is a call for alternative approaches to tackle the multifaceted… read more here.
Keywords: glutaminyl cyclase; discovery conformationally; conformationally restricted; restricted human ... See more keywords
Enhancement of EGFR antibody tumor immunotherapy by glutaminyl cyclase inhibition to interfere with CD47/SIRPα interactions.
Sign Up to like & getrecommendations! Published in 2021 at "Cancer science"
DOI: 10.1111/cas.14999
Abstract: Integrin associated protein (CD47) is an important target in immunotherapy, as it is expressed as a 'don't eat me' signal on many tumor cells. Interference with its counter molecule signal regulatory protein alpha (SIRPα), expressed… read more here.
Keywords: glutaminyl cyclase; egfr; antibody; inhibition ... See more keywords
2D- and 3D-QSAR Modeling of Imidazole-Based Glutaminyl Cyclase Inhibitors.
Sign Up to like & getrecommendations! Published in 2019 at "Current computer-aided drug design"
DOI: 10.2174/1573409915666190918150136
Abstract: BACKGROUND Glutaminyl cyclase (QC) is a novel target in the battle against Alzheimer's disease, a highly prevalent neurodegenerative disorder. QC inhibitors have the potential to be developed as therapeutically useful anti-Alzheimer's disease agents. METHODS Linear… read more here.
Keywords: glutaminyl cyclase; alzheimer disease; imidazole based; qsar modeling ... See more keywords
Can small molecule inhibitors of glutaminyl cyclase be used as a therapeutic for Alzheimer's disease?
Sign Up to like & getrecommendations! Published in 2017 at "Future medicinal chemistry"
DOI: 10.4155/fmc-2017-0190
Abstract: Alzheimer's disease (AD) is a multifactorial and socioeconomically burdensome disease. In view of the failures of anti-AD candidates, we should try to rethink what we did before and what we should do next, in part… read more here.
Keywords: glutaminyl cyclase; alzheimer disease; small molecule; disease ... See more keywords