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Literature summary extracted from

  • Hielscher-Michael, S.; Griehl, C.; Buchholz, M.; Demuth, H.U.; Arnold, N.; Wessjohann, L.A.
    Natural products from microalgae with potential against Alzheimers disease sulfolipids are potent glutaminyl cyclase inhibitors (2016), Mar. Drugs, 14, 203 .
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.2.5 1,2-di-O-palmitoyl-3-O-(6'-deoxy-6'-sulfo-D-glycopyranosyl)-glycerol
-
 Homo sapiens
2.3.2.5 1-O-linolyl-2-O-palmitoyl-3-O-(6'-deoxy-6'-sulfo-D-glucopyranosyl)-glycerol
-
 Homo sapiens
2.3.2.5 1-O-palmitoyl-2-O-linolenyl-3-O-(6'-deoxy-6'-sulfo-D-glucopyranosyl)-glycerol
-
 Homo sapiens
2.3.2.5 additional information natural products from microalgae, such as Scenedesmus rubescens strain SAG 5.95, Scenedesmus producto-capitatus strain SAG 21.81, Scenedesmus accuminatus strain SAG 38.81, Scenedesmus pectinatus strain SAG 2003, Tetradesmus wisconsinensis strain SAG 3.99, and Eustigmatos magnus strain SAG 36.89, show potential against Alzheimers disease, sulfolipids are potent glutaminyl cyclase inhibitors. Mass spectrometric identification and analysis (high resolution ESI-FTIC-MS and UPLC-MS, UPLC/ESI-MSn measurements). The sulfolipids share common, necessary substructures with pharmacophore characteristics of known QC inhibitors Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.3.2.5 L-glutaminyl-peptide Homo sapiens
-
 5-oxoprolyl-peptide + NH3
-
 ?
2.3.2.5 additional information Homo sapiens orexin A, gastrin, gonadotropin, TRH, MCP-1 to 4, FPP, fibronectin, and neurotensin are substrates of the enzyme ?
-
-

Organism

EC Number Organism UniProt Comment Textmining
2.3.2.5 Homo sapiens Q16769
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.3.2.5 central nervous system
-
 Homo sapiens
-
2.3.2.5 corpus striatum
-
 Homo sapiens
-
2.3.2.5 hippocampus
-
 Homo sapiens
-
2.3.2.5 hypophysis
-
 Homo sapiens
-
2.3.2.5 hypothalamus
-
 Homo sapiens
-
2.3.2.5 thymus
-
 Homo sapiens
-
2.3.2.5 thyroid gland
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.3.2.5 L-glutaminyl-7-amido-4-methylcoumarin
-
 Homo sapiens pGlu-7-amido-4-methylcoumarin + NH3
-
 ?
2.3.2.5 L-glutaminyl-peptide
-
 Homo sapiens 5-oxoprolyl-peptide + NH3
-
 ?
2.3.2.5 additional information orexin A, gastrin, gonadotropin, TRH, MCP-1 to 4, FPP, fibronectin, and neurotensin are substrates of the enzyme Homo sapiens ?
-
-

Synonyms

EC Number Synonyms Comment Organism
2.3.2.5 glutaminyl cyclase
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.3.2.5 30
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.3.2.5 8
-
 assay at Homo sapiens

General Information

EC Number General Information Comment Organism
2.3.2.5 evolution glutaminyl cyclases (QCs) belong to the class of acyl transferases. Different types of QCs are identified in bacteria, plants and animals, including mammalian tissues Homo sapiens
2.3.2.5 physiological function glutaminyl cyclases (QCs) catalyze the intramolecular cyclization of N-terminal L-glutamine residues of peptides and proteins into pyroglutamic acid (5-oxo-prolyl, pGlu, pE) releasing ammonia, as well as the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid. Such a type of post-translational modification stabilizes the peptides and proteins, protects them from proteolytic degradation, and can be important for their biological activity Homo sapiens