W86F_human-ACHE

General

Gene Locus : human-ACHE

Mode of mutation : Site directed mutagenesis

Disease :

Summary : Choline binding site cation-aromatic interaction, 660 fold decrease affinity for ACTh no effect on uncharged substrate Ordentlich_1995_J.Biol.Chem_270_2082 || Signal transduction Y133 maintains the correct orientation of W86 Shafferman_1995_5th.ChE.Meeting.Madras__189 Ordentlich_1995_J.Biol.Chem_270_2082

AAA Change :

Allelic Variant :

Risk Factor :

Inhibitor :

Structure :

Disease by interaction :

Interact Gene Locus :

Xenobiotic sensitivity :

Modification : Choline binding site || Signal transduction

Torpedo_number : 84

Kinetic Parameter : Acetylthiocholine_W86F_human-ACHE, 3,3-dimethylbutylthioacetate_W86F_human-ACHE, Edrophonium_W86F_human-ACHE, Propidium_W86F_human-ACHE, Decamethonium_W86F_human-ACHE, Tacrine_W86F_human-ACHE, HuperzineA_W86F_human-ACHE

News : No news

Comment :
p.W86F Trp86Phe (p.W117F Trp117Phe in primary sequence with 31 amino-acids signal peptide) Choline binding site\;cation-aromatic interaction, 660 fold decrease affinity for ACTh no effect on uncharged substrate\; Y133 maintains the correct orientation of W86

References (4)

Title : The 'aromatic patch' of three proximal residues in the human acetylcholinesterase active centre allows for versatile interaction modes with inhibitors - Ariel_1998_Biochem.J_335_95
Author(s) : Ariel N , Ordentlich A , Barak D , Bino T , Velan B , Shafferman A
Ref : Biochemical Journal , 335 :95 , 1998
Abstract :
PubMedSearch : Ariel_1998_Biochem.J_335_95
PubMedID: 9742217

Title : Aging of phosphylated human acetylcholinesterase: catalytic processes mediated by aromatic and polar residues of the active centre - Shafferman_1996_Biochem.J_318_833
Author(s) : Shafferman A , Ordentlich A , Barak D , Stein D , Ariel N , Velan B
Ref : Biochemical Journal , 318 :833 , 1996
Abstract :
PubMedSearch : Shafferman_1996_Biochem.J_318_833
PubMedID: 8836126

Title : Molecular Aspects of Catalysis and of Allosteric Regulation of Aceytlcholinesterases -
Author(s) : Shafferman A , Ordentlich A , Barak D , Kronman C , Ariel N , Leitner M , Segall Y , Bromberg A , Reuveny S , Marcus D , Bino T , Lazar A , Cohen S , Velan B
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. :189 , 1995
PubMedID:

Title : Contribution of aromatic moieties of tyrosine 133 and of the anionic subsite tryptophan 86 to catalytic efficiency and allosteric modulation of acetylcholinesterase - Ordentlich_1995_J.Biol.Chem_270_2082
Author(s) : Ordentlich A , Barak D , Kronman C , Ariel N , Segall Y , Velan B , Shafferman A
Ref : Journal of Biological Chemistry , 270 :2082 , 1995
Abstract :
PubMedSearch : Ordentlich_1995_J.Biol.Chem_270_2082
PubMedID: 7836436