Gene Locus : human-BCHE
Mode of mutation : Site directed mutagenesis
Disease :
Summary : Cocaine hydrolysis 4-fold improvement in catalytic efficiency kcat\/Km Xie_1999_Mol.Pharmacol_55_83 || Binding of inhibitors smaller dimension of the active-site gorge Saxena_1999_Chem.Biol.Interact_119-120_61 || Substrate activation substrate activation Masson_2001_Biochim.Biophys.Acta_1544_166 || Aricept~Donepezil~E2020 inhibition small increase Ki vs WT Saxena_2003_Eur.J.Biochem_270_4447
AAA Change :
Allelic Variant :
Risk Factor :
Inhibitor :
Structure :
Disease by interaction :
Interact Gene Locus :
Xenobiotic sensitivity :
Modification : Acyl specificity || Substrate activation || Cocaine hydrolysis || Aricept~Donepezil~E2020 inhibition
Torpedo_number : 330
Kinetic Parameter : No kinetic parameter
News : No news
Comment :
p.A328Y Ala328Tyr (p.A356Y Ala356Tyr in primary sequence with 28 amino-acids signal peptide)Cocaine hydrolysis\;4-fold improvement in catalytic efficiency kcat\/Km Substrate activation, Aricept~Donepezil~E2020 inhibition\;small increase Ki vs WT
| Title : Probing the peripheral site of human butyrylcholinesterase - Macdonald_2012_Biochemistry_51_7046 |
| Author(s) : Macdonald IR , Martin E , Rosenberry TL , Darvesh S |
| Ref : Biochemistry , 51 :7046 , 2012 |
| Abstract : |
| PubMedSearch : Macdonald_2012_Biochemistry_51_7046 |
| PubMedID: 22901043 |
| Title : Aromatic amino-acid residues at the active and peripheral anionic sites control the binding of E2020 (Aricept) to cholinesterases - Saxena_2003_Eur.J.Biochem_270_4447 |
| Author(s) : Saxena A , Fedorko JM , Vinayaka CR , Medhekar R , Radic Z , Taylor P , Lockridge O , Doctor BP |
| Ref : European Journal of Biochemistry , 270 :4447 , 2003 |
| Abstract : |
| PubMedSearch : Saxena_2003_Eur.J.Biochem_270_4447 |
| PubMedID: 14622273 |
| Title : Concentration-dependent reversible activation-inhibition of human butyrylcholinesterase by tetraethylammonium ion - Stojan_2002_Eur.J.Biochem_269_1154 |
| Author(s) : Stojan J , Golicnik M , Froment MT , Estour F , Masson P |
| Ref : European Journal of Biochemistry , 269 :1154 , 2002 |
| Abstract : |
| PubMedSearch : Stojan_2002_Eur.J.Biochem_269_1154 |
| PubMedID: 11856351 |
| Title : Effects of mutations of active site residues and amino acids interacting with the Omega loop on substrate activation of butyrylcholinesterase - Masson_2001_Biochim.Biophys.Acta_1544_166 |
| Author(s) : Masson P , Xie W , Froment MT , Lockridge O |
| Ref : Biochimica & Biophysica Acta , 1544 :166 , 2001 |
| Abstract : |
| PubMedSearch : Masson_2001_Biochim.Biophys.Acta_1544_166 |
| PubMedID: 11341926 |
| Gene_locus related to this paper: human-BCHE |
| Title : An improved cocaine hydrolase: the A328Y mutant of human butyrylcholinesterase is 4-fold more efficient - Xie_1999_Mol.Pharmacol_55_83 |
| Author(s) : Xie W , Altamirano CV , Bartels CF , Speirs RJ , Cashman JR , Lockridge O |
| Ref : Molecular Pharmacology , 55 :83 , 1999 |
| Abstract : |
| PubMedSearch : Xie_1999_Mol.Pharmacol_55_83 |
| PubMedID: 9882701 |
| Title : Differences in active-site gorge dimensions of cholinesterases revealed by binding of inhibitors to human butyrylcholinesterase - Saxena_1999_Chem.Biol.Interact_119-120_61 |
| Author(s) : Saxena A , Redman AM , Jiang X , Lockridge O , Doctor BP |
| Ref : Chemico-Biological Interactions , 119-120 :61 , 1999 |
| Abstract : |
| PubMedSearch : Saxena_1999_Chem.Biol.Interact_119-120_61 |
| PubMedID: 10421439 |