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Literature summary for 3.1.1.8 extracted from

  • Terali, K.; Dalmizrak, O.; Hoti, Q.; Ozer, N.
    Evaluation of the inhibitory effect of abamectin on mammalian butyrylcholinesterase enzyme kinetic and molecular docking studies (2018), J. Environ. Sci. Health B, 8, 1-6 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
abamectin is a potent inhibitor of horse serum butyrylcholinesterase which interacts with the enzyme in a reversible, competitive manner predictively to block the mouth of the active-site gorge of the enzyme and to bind to several critical residues that normally bind/hydrolyze choline esters. Abamectin is a blend of natural avermectins B1a and B1b. Avermectins potentiate the ability of certain neurotransmitters (GABA and/or glutamate) to trigger an influx of Cl- ions carried by neurotransmitter-gated chloride channels in target organisms. Competitive versus butyrylthiocholine. Docking study, BChE-avermectin docking and interaction profiling, overview Equus caballus
avermectin B1a engagement of avermectin B1a in a hydrogen-bonding interaction with the catalytic serine Equus caballus
avermectin B1b
-
Equus caballus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.16
-
butyrylthiocholine pH 7.5, 37°C Equus caballus

Localization

Localization Comment Organism GeneOntology No. Textmining
neuromuscular junction
-
Equus caballus 31594
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
butyrylcholine + H2O Equus caballus
-
choline + butyrate
-
?

Organism

Organism UniProt Comment Textmining
Equus caballus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
Equus caballus
-
central nervous system
-
Equus caballus
-
commercial preparation highly-purified formulation of BChE from equine serum Equus caballus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
butyrylcholine + H2O
-
Equus caballus choline + butyrate
-
?
butyrylthiocholine + H2O
-
Equus caballus thiocholine + butyrate
-
?

Synonyms

Synonyms Comment Organism
BChE
-
Equus caballus
butyrylcholinesterase
-
Equus caballus
plasma cholinesterase
-
Equus caballus
pseudocholinesterase
-
Equus caballus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Equus caballus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Equus caballus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information kinetics of BChE inhibition Equus caballus
0.00226
-
abamectin pH 7.5, 37°C Equus caballus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0106
-
pH 7.5, 37°C Equus caballus abamectin

General Information

General Information Comment Organism
physiological function butyrylcholinesterase is a serine hydrolase loosely related to the mammalian cholinergic system. It shows a nearly ubiquitous distribution among tissues and is abundant in plasma. In plasma, BChE protects the neurotransmitter function of its sister enzyme acetylcholinesterase (AChE, EC 3.1.1.7) by neutralizing toxins (including neuroactive pesticides, drugs, and a few other chemicals like food additives) before they reach AChE, while in the central nervous system as well as at the neuromuscular junction it serves as a backup to AChE by breaking down acetylcholine that has diffused out of the synaptic cleft Equus caballus