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butyrylcholinesterase

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Target id: 2471

Nomenclature: butyrylcholinesterase

Abbreviated Name: BChE

Family: Hydrolases & Lipases, Acetylcholine turnover

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 602 3q26.1 BCHE butyrylcholinesterase
Mouse - 603 3 E3 Bche butyrylcholinesterase
Rat - - 2q32 Bche butyrylcholinesterase
Previous and Unofficial Names Click here for help
Acylcholine acylhydrolase | Butyrylcholine esterase | CHE1 | Choline esterase II | cholinesterase
Database Links Click here for help
Alphafold P06276 (Hs), Q03311 (Mm)
BRENDA 3.1.1.7
CATH/Gene3D 3.40.50.1820
ChEMBL Target CHEMBL1914 (Hs), CHEMBL2528 (Mm)
DrugBank Target P06276 (Hs)
Ensembl Gene ENSG00000114200 (Hs), ENSMUSG00000027792 (Mm), ENSRNOG00000009826 (Rn)
Entrez Gene 590 (Hs), 12038 (Mm)
Human Protein Atlas ENSG00000114200 (Hs)
KEGG Enzyme 3.1.1.7
KEGG Gene hsa:590 (Hs), mmu:12038 (Mm)
OMIM 177400 (Hs)
Orphanet ORPHA118998 (Hs)
Pharos P06276 (Hs)
RefSeq Nucleotide NM_000055 (Hs), NM_009738 (Mm), NM_022942 (Rn)
RefSeq Protein NP_000046 (Hs), NP_033868 (Mm), NP_075231 (Rn)
SynPHARM 78671 (in complex with tacrine)
UniProtKB P06276 (Hs), Q03311 (Mm)
Wikipedia BCHE (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human butyryl cholinesterase
PDB Id:  1P0I
Resolution:  2.0Å
Species:  Human
References:  4
Enzyme Reaction Click here for help
EC Number: 3.1.1.7 Acetylcholine + H2O = acetic acid + choline + H+

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
tacrine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.2 pKi 1
⤷ pKi 7.2 (Ki 7x10-8 M) [1]
bambuterol Small molecule or natural product Approved drug Hs Inhibition 8.5 pIC50 2
⤷ pIC50 8.5 [2]
physostigmine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 7.6 – 7.8 pIC50 3
⤷ pIC50 7.6 – 7.8 [3]
rivastigmine Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.4 pIC50 3
⤷ pIC50 7.4 (IC50 3.7x10-8 M) [3]
pyridostigmine Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 6.1 pIC50 5
⤷ pIC50 6.1 (IC50 9x10-7 M) [5]
Description: Inhibition of human plasma BCHE activity by a modified Ellman assay.
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Butyrylcholinesterase deficiency
Orphanet: ORPHA132

References

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1. Butini S, Campiani G, Borriello M, Gemma S, Panico A, Persico M, Catalanotti B, Ros S, Brindisi M, Agnusdei M et al.. (2008) Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors. J Med Chem, 51 (11): 3154-70. [PMID:18479118]

2. Giacobini E. (2003) Cholinesterases: new roles in brain function and in Alzheimer's disease. Neurochem Res, 28 (3-4): 515-22. [PMID:12675140]

3. Luo W, Yu QS, Kulkarni SS, Parrish DA, Holloway HW, Tweedie D, Shafferman A, Lahiri DK, Brossi A, Greig NH. (2006) Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine. J Med Chem, 49 (7): 2174-85. [PMID:16570913]

4. Nicolet Y, Lockridge O, Masson P, Fontecilla-Camps JC, Nachon F. (2003) Crystal structure of human butyrylcholinesterase and of its complexes with substrate and products. J Biol Chem, 278 (42): 41141-7. [PMID:12869558]

5. Yu QS, Holloway HW, Luo W, Lahiri DK, Brossi A, Greig NH. (2010) Long-acting anticholinesterases for myasthenia gravis: synthesis and activities of quaternary phenylcarbamates of neostigmine, pyridostigmine and physostigmine. Bioorg Med Chem, 18 (13): 4687-93. [PMID:20627738]

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