F295L_mouse-ACHE

General

Gene Locus : mouse-ACHE

Mode of mutation : Site directed mutagenesis

Disease :

Summary : Acyl specificity Acyl pocket, confers butyrylcholinesterase activity Vellom_1993_Biochemistry_32_12 Pickering_1995_5th.ChE.Meeting.Madras__227 || Fasciculin inhibition low effect Radic_1994_J.Biol.Chem_269_11233 || Aricept~Donepezil~E2020 inhibition increase Ki vs WT Saxena_2003_Eur.J.Biochem_270_4447 || Oxime interaction enlargement of the active site of the gorge Kovarik_2006_Biochem.Biophys.Res.Commun_342_973 Kovarik_2007_Toxicology_233_79

AAA Change :

Allelic Variant :

Risk Factor :

Inhibitor :

Structure :

Disease by interaction :

Interact Gene Locus :

Xenobiotic sensitivity :

Modification : Acyl specificity || Aricept~Donepezil~E2020 inhibition || Oxime interaction || Fasciculin inhibition

Torpedo_number : 288

Kinetic Parameter : Acetylthiocholine_F295L_mouse-ACHE, WT-fasciculin2_F295L_mouse-ACHE, Butyrylthiocholine_F295L_mouse-ACHE, Benzoylthiocholine_F295L_mouse-ACHE

News : No news

Comment :
enlargement of the active site of the gorge || p.Phe295Leu

References (9)

Title : Mutation of acetylcholinesterase to enhance oxime-assisted catalytic turnover of methylphosphonates - Kovarik_2007_Toxicology_233_79
Author(s) : Kovarik Z , Radic Z , Berman HA , Taylor P
Ref : Toxicology , 233 :79 , 2007
Abstract :
PubMedSearch : Kovarik_2007_Toxicology_233_79
PubMedID: 17046138

Title : Active site mutant acetylcholinesterase interactions with 2-PAM, HI-6, and DDVP - Kovarik_2006_Biochem.Biophys.Res.Commun_342_973
Author(s) : Kovarik Z , Ciban N , Radic Z , Simeon-Rudolf V , Taylor P
Ref : Biochemical & Biophysical Research Communications , 342 :973 , 2006
Abstract :
PubMedSearch : Kovarik_2006_Biochem.Biophys.Res.Commun_342_973
PubMedID: 16598855

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 : Inactivation studies of acetylcholinesterase with phenylmethylsulfonyl fluoride - Kraut_2000_Mol.Pharmacol_57_1243
Author(s) : Kraut D , Goff H , Pai RK , Hosea NA , Silman I , Sussman JL , Taylor P , Voet JG
Ref : Molecular Pharmacology , 57 :1243 , 2000
Abstract :
PubMedSearch : Kraut_2000_Mol.Pharmacol_57_1243
PubMedID: 10825396

Title : Organophosphate Specificity of Acyl Pocket Cholinesterase Mutants -
Author(s) : Pickering NA , Taylor P , Berman HA
Ref : In Enzyme of the Cholinesterase Family - Proceedings of Fifth International Meeting on Cholinesterases , (Quinn, D.M., Balasubramanian, A.S., Doctor, B.P., Taylor, P., Eds) Plenum Publishing Corp. :227 , 1995
PubMedID:

Title : Specificity and orientation of trigonal carboxyl esters and tetrahedral alkylphosphonyl esters in cholinesterases - Hosea_1995_Biochemistry_34_11528
Author(s) : Hosea NA , Berman HA , Taylor P
Ref : Biochemistry , 34 :11528 , 1995
Abstract :
PubMedSearch : Hosea_1995_Biochemistry_34_11528
PubMedID: 7547883

Title : Site of fasciculin interaction with acetylcholinesterase - Radic_1994_J.Biol.Chem_269_11233
Author(s) : Radic Z , Duran R , Vellom DC , Li Y , Cervenansky C , Taylor P
Ref : Journal of Biological Chemistry , 269 :11233 , 1994
Abstract :
PubMedSearch : Radic_1994_J.Biol.Chem_269_11233
PubMedID: 8157652

Title : Amino acid residues controlling acetylcholinesterase and butyrylcholinesterase specificity - Vellom_1993_Biochemistry_32_12
Author(s) : Vellom DC , Radic Z , Li Y , Pickering NA , Camp S , Taylor P
Ref : Biochemistry , 32 :12 , 1993
Abstract :
PubMedSearch : Vellom_1993_Biochemistry_32_12
PubMedID: 8418833

Title : Three distinct domains in the cholinesterase molecule confer selectivity for acetyl- and butyrylcholinesterase inhibitors - Radic_1993_Biochemistry_32_12074
Author(s) : Radic Z , Pickering NA , Vellom DC , Camp S , Taylor P
Ref : Biochemistry , 32 :12074 , 1993
Abstract :
PubMedSearch : Radic_1993_Biochemistry_32_12074
PubMedID: 8218285