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 Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.16 | - |
butyrylthiocholine | pH 7.5, 37°C | Equus caballus |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
neuromuscular junction | - |
Equus caballus | 31594 | - |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
butyrylcholine + H2O | Equus caballus | - |
choline + butyrate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Equus caballus | - |
- |
- |
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 | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
butyrylcholine + H2O | - |
Equus caballus | choline + butyrate | - |
? | |
butyrylthiocholine + H2O | - |
Equus caballus | thiocholine + butyrate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
BChE | - |
Equus caballus |
butyrylcholinesterase | - |
Equus caballus |
plasma cholinesterase | - |
Equus caballus |
pseudocholinesterase | - |
Equus caballus |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Equus caballus |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
assay at | Equus caballus |
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 Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0106 | - |
pH 7.5, 37°C | Equus caballus | abamectin |
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 |