W86A_mouse-ACHE

General

Gene Locus : mouse-ACHE

Mode of mutation : Site directed mutagenesis

Disease :

Summary : Fasciculin inhibition Fas becomes an allosteric activator instead of an inhibitor for certain substr. Radic_1995_J.Biol.Chem_270_20391 Ashani_1995_5th.ChE.Meeting.Madras__133 || Aricept~Donepezil~E2020 inhibition 300-fold increase in 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 : Choline binding site || Aricept~Donepezil~E2020 inhibition

Torpedo_number : 84

Kinetic Parameter : No kinetic parameter

News : No news

Comment : p.W86A Trp86Ala Fasciculin becomes an allosteric activator instead of an inhibitor for certain substrates\; Aricept~Donepezil~E2020 inhibition\;300-fold increase in Ki vs WT

References (3)

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 : Saxena_2003_Eur.J.Biochem_270_4447
ESTHER : Saxena_2003_Eur.J.Biochem_270_4447
PubMedSearch : Saxena_2003_Eur.J.Biochem_270_4447
PubMedID: 14622273

Title : Amino Acid Residues that Control Mono- and Bisquaternary Oxime-Induced Reactivation of O-Ethyl Methylphosphonylated Cholinesterases -
Author(s) : Ashani Y , Radic Z , Tsigelny I , Vellom DC , Pickering NA , Quinn DM , Doctor BP , Taylor P
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. :133 , 1995
PubMedID:

Title : Allosteric control of acetylcholinesterase catalysis by fasciculin - Radic_1995_J.Biol.Chem_270_20391
Author(s) : Radic Z , Quinn DM , Vellom DC , Camp S , Taylor P
Ref : Journal of Biological Chemistry , 270 :20391 , 1995
Abstract : Radic_1995_J.Biol.Chem_270_20391
ESTHER : Radic_1995_J.Biol.Chem_270_20391
PubMedSearch : Radic_1995_J.Biol.Chem_270_20391
PubMedID: 7657613