acetylcholinesterase (Cartwright blood group)

Target id: 2465

Nomenclature: acetylcholinesterase (Cartwright blood group)

Abbreviated Name: AChE

Family: Hydrolases, Acetylcholine turnover

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for acetylcholinesterase (Cartwright blood group) in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 614 7q22 ACHE acetylcholinesterase (Cartwright blood group)
Mouse - 614 5 G2 Ache acetylcholinesterase
Rat - 614 12 Ache acetylcholinesterase
Previous and Unofficial Names
Yt blood group | acetylcholinesterase | acetylcholinesterase (Yt blood group)
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of Recombinant Human Acetylcholinesterase in Complex with Donepezil
PDB Id:  4EY7
Ligand:  donepezil
Resolution:  2.35Å
Species:  Human
References:  4
Enzyme Reaction
EC Number: 3.1.1.7 Acetylcholine + H2O = acetic acid + choline + H+

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
tacrine Hs Inhibition 7.5 pKi 2
pKi 7.5 (Ki 3x10-8 M) [2]
edrophonium Hs Inhibition 6.7 pKi 1
pKi 6.7 (Ki 2x10-7 M) [1]
Description: Using the chloride salt
donepezil Hs Inhibition 7.7 – 8.3 pIC50 3,6,9
pIC50 7.7 – 8.3 [3,6,9]
physostigmine Hs Inhibition 7.6 – 7.8 pIC50 9
pIC50 7.6 – 7.8 [9]
BW284C51 Hs Inhibition 7.7 pIC50 7
pIC50 7.7 [7]
neostigmine Hs Inhibition 7.3 pIC50 8
pIC50 7.3 (IC50 4.5x10-8 M) [8]
Description: Inhibition of ACHE activity in human serum.
pyridostigmine Hs Inhibition 6.4 pIC50 11
pIC50 6.4 (IC50 3.6x10-7 M) [11]
Description: Inhibition of human erythrocyte ACHE activity by a modified Ellman assay.
galantamine Hs Inhibition 6.3 pIC50 5
pIC50 6.3 (IC50 5x10-7 M) [5]
rivastigmine Hs Inhibition 5.4 pIC50 9
pIC50 5.4 (IC50 4.15x10-6 M) [9]
pralidoxime Hs Inhibition 3.1 pIC50 10
pIC50 3.1 (IC50 8.78x10-4 M) [10]
Description: Inhibition of human recombinant AChE by modified Ellman's method.
echothiophate Hs Inhibition - -
General Comments
It has been shown that ACHE corresponds to the Yt blood group antigen. For more details see the OMIM entry 112100.

References

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1. Boyle NA, Talesa V, Giovannini E, Rosi G, Norton SJ. (1997) Synthesis and study of thiocarbonate derivatives of choline as potential inhibitors of acetylcholinesterase. J. Med. Chem.40 (19): 3009-13. [PMID:9301662]

2. 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]

3. Cardozo MG, Iimura Y, Sugimoto H, Yamanishi Y, Hopfinger AJ. (1992) QSAR analyses of the substituted indanone and benzylpiperidine rings of a series of indanone-benzylpiperidine inhibitors of acetylcholinesterase. J. Med. Chem.35 (3): 584-9. [PMID:1738151]

4. Cheung J, Rudolph MJ, Burshteyn F, Cassidy MS, Gary EN, Love J, Franklin MC, Height JJ. (2012) Structures of human acetylcholinesterase in complex with pharmacologically important ligands. J. Med. Chem.55 (22): 10282-6. [PMID:23035744]

5. Clark JK, Cowley P, Muir AW, Palin R, Pow E, Prosser AB, Taylor R, Zhang MQ. (2002) Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block. Bioorg. Med. Chem. Lett.12 (18): 2565-8. [PMID:12182861]

6. Galli A, Mori F, Benini L, Cacciarelli N. (1994) Acetylcholinesterase protection and the anti-diisopropylfluorophosphate efficacy of E2020. Eur. J. Pharmacol.270 (2-3): 189-93. [PMID:8039548]

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

8. Kavitha CV, Gaonkar SL, Narendra Sharath Chandra JN, Sadashiva CT, Rangappa KS. (2007) Synthesis and screening for acetylcholinesterase inhibitor activity of some novel 2-butyl-1,3-diaza-spiro[4,4]non-1-en-4-ones: derivatives of irbesartan key intermediate. Bioorg. Med. Chem.15 (23): 7391-8. [PMID:17888667]

9. 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]

10. Musilek K, Komloova M, Holas O, Horova A, Pohanka M, Gunn-Moore F, Dohnal V, Dolezal M, Kuca K. (2011) Mono-oxime bisquaternary acetylcholinesterase reactivators with prop-1,3-diyl linkage-Preparation, in vitro screening and molecular docking. Bioorg. Med. Chem.19 (2): 754-62. [PMID:21215642]

11. 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]

How to cite this page

Acetylcholine turnover: acetylcholinesterase (Cartwright blood group). Last modified on 21/03/2016. Accessed on 17/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2465.