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
| 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 : 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 : |
| PubMedSearch : Radic_1995_J.Biol.Chem_270_20391 |
| PubMedID: 7657613 |