ArticleBiochemistry2012
Probing the peripheral site of human butyrylcholinesterase.
Article in Biochemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
26 citing papers in PubMed, 71 citations in OpenAlex.
- Structure-Based Design of New Series of Sulfonates with Potent and Specific BChE Inhibition and Anti-Inflammatory Effects.International journal of molecular sciences · 2026Article
- Fluorometric and Colorimetric Biosensors for the Assay of Cholinesterase Inhibitors.Sensors (Basel, Switzerland) · 2025Review
- Anti-Alzheimer effects of the newly synthesized cationic compounds as multi-target dual hAChE/hBuChE inhibitor: AnBioImpacts : BI · 2025Article
- Identification of AChE targeted therapeutic compounds for Alzheimer's disease: an in-silico study with DFT integration.Scientific reports · 2024Article
- Sertraline as a Multi-Target Modulator of AChE, COX-2, BACE-1, and GSK-3β: Computational and In Vivo Studies.Molecules (Basel, Switzerland) · 2024Article
- Virtual Screening, Toxicity Evaluation and Pharmacokinetics of Erythrina Alkaloids as Acetylcholinesterase Inhibitor Candidates from Natural Products.Advances and applications in bioinformatics and chemistry : AABC · 2024Article
- Investigation of the enantioselectivity of acetylcholinesterase and butyrylcholinesterase upon inhibition by tacrine-iminosugar heterodimers.Journal of enzyme inhibition and medicinal chemistry · 2023Article
- Anti-AChE and Anti-BuChE Screening of the Fermentation Broth Extracts from Twelve Aspergillus Isolates and GC-MS and Molecular Docking Studies of the Most Active Extracts.Applied biochemistry and biotechnology · 2023Article
- Correlation between total phenolic and flavonoid contents and biological activities of 12 ethanolic extracts of Iranian propolis.Food science & nutrition · 2023Article
- 8-Hydroxyquinolylnitrones as multifunctional ligands for the therapy of neurodegenerative diseases.Acta pharmaceutica Sinica. B · 2023Article
- Synthesis and biological evaluation of substituted acetamide derivatives as potential butyrylcholinestrase inhibitors.Scientific reports · 2023Article
- Article
- Exploiting butyrylcholinesterase inhibitors through a combined 3-D pharmacophore modeling, QSAR, molecular docking, and molecular dynamics investigation.RSC advances · 2023Article
- Neuroprotective Effect of Methanolic Ajwa Seed Extract on Lipopolysaccharide-Induced Memory Dysfunction and Neuroinflammation: In Vivo, Molecular Docking and Dynamics Studies.Plants (Basel, Switzerland) · 2023Article
- Tacrine-Based Hybrids: Past, Present, and Future.International journal of molecular sciences · 2023Review
- Green and four-component cyclocondensation synthesis and in silico docking of new polyfunctionalized pyrrole derivatives as the potential anticholinesterase agents.Molecular diversity · 2022Article
- A hybrid of 1-deoxynojirimycin and benzotriazole induces preferential inhibition of butyrylcholinesterase (BuChE) over acetylcholinesterase (AChE).Journal of enzyme inhibition and medicinal chemistry · 2022Article
- Evaluation of the Key Structural Features of Various Butyrylcholinesterase Inhibitors Using Simple Molecular Descriptors.Molecules (Basel, Switzerland) · 2022Article
- Chemical Synthesis and Biological Activities of Amaryllidaceae Alkaloid Norbelladine Derivatives and Precursors.Molecules (Basel, Switzerland) · 2022Article
- Novel benzimidazole-based pseudo-irreversible butyrylcholinesterase inhibitors with neuroprotective activity in an Alzheimer's disease mouse model.RSC medicinal chemistry · 2022Article
Corrections and comments
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Authors and funding
4 authors at 3 institutions in 2 countries.
Funding
Abstract
Acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) catalyze the hydrolysis of the neurotransmitter acetylcholine and, thereby, function as coregulators of cholinergic neurotransmission. For both enzymes, hydrolysis takes place near the bottom of a 20 Å deep active site gorge. A number of amino acid residues within the gorge have been identified as important in facilitating efficient catalysis and inhibitor binding. Of particular interest is the catalytic triad, consisting of serine, histidine, and glutamate residues, that mediates hydrolysis. Another site influencing the catalytic process is located above the catalytic triad toward the periphery of the active site gorge. This peripheral site (P-site) contains a number of aromatic amino acid residues as well as an aspartate residue that is able to interact with cationic substrates and guide them down the gorge to the catalytic triad. In human AChE, certain aryl residues in the vicinity of the anionic aspartate residue (D74), such as W286, have been implicated in ligand binding and have therefore been considered part of the P-site of the enzyme. The present study was undertaken to explore the P-site of human BuChE and determine whether, like AChE, aromatic side chains near the peripheral aspartate (D70) of this enzyme contribute to ligand binding. Results obtained, utilizing inhibitor competition studies and BuChE mutant species, indicate the participation of aryl residues (F329 and Y332) in the E-helix component of the BuChE active site gorge, along with the anionic aspartate residue (D70), in binding ligands to the P-site of the enzyme.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.