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
Mycobacterium tuberculosis CRISPR/Cas system Csm1 holds clues to the evolutionary relationship between DNA polymerase and cyclase activity.
Sign Up to like & getrecommendations! Published in 2020 at "International journal of biological macromolecules"
DOI: 10.1016/j.ijbiomac.2020.12.014
Abstract: Prokaryotic CRISPR/Cas systems confer immunity against invading nucleic acids through effector complexes. Csm1, the signature protein of Type III effector complexes, catalyses cyclic oligoadenylate synthesis when in the effector complex, but not when alone, activating… read more here.
Keywords: crispr cas; dna polymerase; polymerase; cyclase ... See more keywords
Expression pattern of type 3 adenylyl cyclase in rodent dorsal root ganglion and its primary afferent terminals
Sign Up to like & getrecommendations! Published in 2019 at "Neuroscience Letters"
DOI: 10.1016/j.neulet.2018.10.049
Abstract: cAMP (Cyclic Adenosine monophosphate), one of the most highly studied second messengers, is regulated by a family of adenylyl cyclase (AC) enzymes. Type 3 adenylyl cyclase (abbreviated as AC3), a subtype of adenylyl cyclase, is… read more here.
Keywords: adenylyl cyclase; type adenylyl; root ganglion; dorsal root ... 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
Transient Prenyltransferase-Cyclase Association in Fusicoccadiene Synthase, an Assembly-Line Terpene Synthase.
Sign Up to like & getrecommendations! Published in 2022 at "Biochemistry"
DOI: 10.1021/acs.biochem.2c00509
Abstract: Fusicoccadiene synthase from the fungus Phomopsis amygdali (PaFS) is an assembly-line terpene synthase that catalyzes the first two steps in the biosynthesis of Fusiccocin A, a diterpene glycoside. The C-terminal prenyltransferase domain of PaFS catalyzes… read more here.
Keywords: prenyltransferase; prenyltransferase cyclase; cyclase; fusicoccadiene synthase ... See more keywords
Cryo-EM Structure of the Cyclase Domain and Evaluation of Substrate Channeling in a Bifunctional Class II Terpene Synthase
Sign Up to like & getrecommendations! Published in 2025 at "Biochemistry"
DOI: 10.1021/acs.biochem.5c00509
Abstract: Copalyl diphosphate synthase from Penicillium verruculosum (PvCPS) is a bifunctional class II terpene synthase containing a prenyltransferase that produces geranylgeranyl diphosphate (GGPP) and a class II cyclase that utilizes GGPP as a substrate to generate… read more here.
Keywords: class; class terpene; bifunctional class; substrate channeling ... 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
A Multifunctional Cytochrome P450 and a Meroterpenoid Cyclase in the Biosynthesis of Fungal Meroterpenoid Atlantinone B.
Sign Up to like & getrecommendations! Published in 2022 at "Organic letters"
DOI: 10.1021/acs.orglett.2c00684
Abstract: The biosynthetic gene cluster of atlantinone B (10) was discovered in Penicillium chrysogenum MT-40. A multifunctional cytochrome P450 (AtlD) encoded by the cluster is responsible for the formation of the unique lactone-bridged ring and the… read more here.
Keywords: cyclase; cytochrome p450; atlantinone; multifunctional cytochrome ... See more keywords
Multidomain P450 Epoxidase and a Terpene Cyclase from the Ascochlorin Biosynthetic Pathway in Fusarium sp.
Sign Up to like & getrecommendations! Published in 2019 at "Organic letters"
DOI: 10.1021/acs.orglett.9b00616
Abstract: Ascochlorin is a medicinally important fungal meroterpenoid. Its biosynthetic pathway in Fusarium sp. was identified, and the stereoselective epoxidation of the farnesyl group by the multidomain, soluble P450 monooxygenase AscE and the subsequent formation of… read more here.
Keywords: cyclase; biosynthetic pathway; multidomain p450; pathway fusarium ... See more keywords
Characterization of a Dual Function Peptide Cyclase in Graspetide Biosynthesis.
Sign Up to like & getrecommendations! Published in 2024 at "ACS chemical biology"
DOI: 10.1021/acschembio.4c00626
Abstract: Graspetides are a diverse family of ribosomally synthesized and post-translationally modified peptides with unique macrocyclic structures formed by ATP-grasp enzymes. Group 11 graspetides, including prunipeptin, feature both macrolactone and macrolactam cross-links. Despite the known involvement… read more here.
Keywords: atp grasp; graspetide biosynthesis; prub; characterization dual ... See more keywords