Gene Locus : human-ACHE
Mode of mutation : Site directed mutagenesis
Disease :
Summary : Peripheral Anionic Site Substrate inhibition 10 fold increase of inhibition K for PAS ligands Shafferman_1992_EMBO.J_11_3561 Shafferman_1992_4th.ChE.Meeting.Eilat__165 Ordentlich_1993_J.Biol.Chem_268_17083 Shafferman_1993_Proc.Med.Def.Biosci.Rev_3_1097 Ashani_1994_Mol.Pharmacol_45_555 Barak_1994_J.Biol.Chem_269_6296 Shafferman_1995_5th.ChE.Meeting.Madras__189 || Acyl specificity replacement of aromatic active center residues in human-ACHE by the corresponding residues in human-BCHE Kaplan_2001_Biochemistry_40_7433
AAA Change :
Allelic Variant :
Risk Factor :
Inhibitor :
Structure :
Disease by interaction :
Interact Gene Locus :
Xenobiotic sensitivity :
Modification : Peripheral Anionic Site || Substrate inhibition || Acyl specificity
Torpedo_number : 279
Kinetic Parameter : Edrophonium_W286A_human-ACHE, Paranitrophenylacetate_W286A_human-ACHE, S-N-Propylthioacetate_W286A_human-ACHE, 3,3-dimethylbutylthioacetate_W286A_human-ACHE, Acetylthiocholine_W286A_human-ACHE, Hexamethonium_W286A_human-ACHE, BW284C51_W286A_human-ACHE, Propidium_W286A_human-ACHE, Decamethonium_W286A_human-ACHE, Tacrine_W286A_human-ACHE, HuperzineA_W286A_human-ACHE, Butyrylthiocholine_W286A_human-ACHE
News : No news
Comment : p.W286A Trp286Ala (p.W317A Trp317Ala in primary sequence with 31 amino-acids signal peptide) Peripheral Anionic Site Substrate inhibition\;10 fold increase of inhibition K for PAS ligands\; Acyl specificity\;replacement of aromatic active center residues in human-ACHE by the corresponding residues in human-BCHE
| Title : Oxime-assisted reactivation of tabun-inhibited acetylcholinesterase analysed by active site mutations - Katalinic_2018_Toxicology_406-407_104 |
| Author(s) : Katalinic M , Sinko G , Macek Hrvat N , Zorbaz T , Bosak A , Kovarik Z |
| Ref : Toxicology , 406-407 :104 , 2018 |
| Abstract : Katalinic_2018_Toxicology_406-407_104 |
| ESTHER : Katalinic_2018_Toxicology_406-407_104 |
| PubMedSearch : Katalinic_2018_Toxicology_406-407_104 |
| PubMedID: 29772260 |
| Title : Does butyrylization of acetylcholinesterase through substitution of the six divergent aromatic amino acids in the active center gorge generate an enzyme mimic of butyrylcholinesterase? - Kaplan_2001_Biochemistry_40_7433 |
| Author(s) : Kaplan D , Ordentlich A , Barak D , Ariel N , Kronman C , Velan B , Shafferman A |
| Ref : Biochemistry , 40 :7433 , 2001 |
| Abstract : Kaplan_2001_Biochemistry_40_7433 |
| ESTHER : Kaplan_2001_Biochemistry_40_7433 |
| PubMedSearch : Kaplan_2001_Biochemistry_40_7433 |
| PubMedID: 11412096 |
| 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 : Ariel_1998_Biochem.J_335_95 |
| ESTHER : Ariel_1998_Biochem.J_335_95 |
| PubMedSearch : Ariel_1998_Biochem.J_335_95 |
| PubMedID: 9742217 |
| 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 : Acetylcholinesterase peripheral anionic site degeneracy conferred by amino acid arrays sharing a common core - Barak_1994_J.Biol.Chem_269_6296 |
| Author(s) : Barak D , Kronman C , Ordentlich A , Ariel N , Bromberg A , Marcus D , Lazar A , Velan B , Shafferman A |
| Ref : Journal of Biological Chemistry , 269 :6296 , 1994 |
| Abstract : Barak_1994_J.Biol.Chem_269_6296 |
| ESTHER : Barak_1994_J.Biol.Chem_269_6296 |
| PubMedSearch : Barak_1994_J.Biol.Chem_269_6296 |
| PubMedID: 8119978 |
| Title : Role of tyrosine 337 in the binding of huperzine A to the active site of human acetylcholinesterase - Ashani_1994_Mol.Pharmacol_45_555 |
| Author(s) : Ashani Y , Grunwald J , Kronman C , Velan B , Shafferman A |
| Ref : Molecular Pharmacology , 45 :555 , 1994 |
| Abstract : Ashani_1994_Mol.Pharmacol_45_555 |
| ESTHER : Ashani_1994_Mol.Pharmacol_45_555 |
| PubMedSearch : Ashani_1994_Mol.Pharmacol_45_555 |
| PubMedID: 8145739 |
| Gene_locus related to this paper: human-ACHE |
| Title : Recombinant human acetylcholinesterase - Enzyme engineering - |
| Author(s) : Shafferman A , Velan B , Barak D , Kronman C , Ordentlich A , Flashner Y , Leitner M , Segal Y , Grosfeld H , Stein D , Ariel N |
| Ref : Medical Defense Bioscience Review , 3 :1097 , 1993 |
| PubMedID: |
| Title : Dissection of the human acetylcholinesterase active center determinants of substrate specificity. Identification of residues constituting the anionic site, the hydrophobic site, and the acyl pocket - Ordentlich_1993_J.Biol.Chem_268_17083 |
| Author(s) : Ordentlich A , Barak D , Kronman C , Flashner Y , Leitner M , Segall Y , Ariel N , Cohen S , Velan B , Shafferman A |
| Ref : Journal of Biological Chemistry , 268 :17083 , 1993 |
| Abstract : Ordentlich_1993_J.Biol.Chem_268_17083 |
| ESTHER : Ordentlich_1993_J.Biol.Chem_268_17083 |
| PubMedSearch : Ordentlich_1993_J.Biol.Chem_268_17083 |
| PubMedID: 8349597 |
| Gene_locus related to this paper: human-ACHE , human-BCHE |
| Title : Substrate inhibition of acetylcholinesterase: residues affecting signal transduction from the surface to the catalytic center - Shafferman_1992_EMBO.J_11_3561 |
| Author(s) : Shafferman A , Velan B , Ordentlich A , Kronman C , Grosfeld H , Leitner M , Flashner Y , Cohen S , Barak D , Ariel N |
| Ref : EMBO Journal , 11 :3561 , 1992 |
| Abstract : Shafferman_1992_EMBO.J_11_3561 |
| ESTHER : Shafferman_1992_EMBO.J_11_3561 |
| PubMedSearch : Shafferman_1992_EMBO.J_11_3561 |
| PubMedID: 1396557 |
| Title : Acetylcholinesterase Catalysis - Protein Engineering Studies - |
| Author(s) : Shafferman A , Velan B |
| Ref : In Multidisciplinary approaches to cholinesterase functions - Proceedings of Fourth International Meeting on Cholinesterases , (Shafferman, A. and Velan, B., Eds) Plenum Press, New York :165 , 1992 |
| PubMedID: |