Gene Locus : human-ACHE
Mode of mutation : Site directed mutagenesis
Disease :
Summary : Signal transduction reduced kcat, marginal effect on inhibition by edrophonium 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 Barak_1994_J.Biol.Chem_269_6296 Shafferman_1995_5th.ChE.Meeting.Madras__189 Shafferman_1996_Biochem.J_318_833 || Acyl specificity Acyl pocket decreased catalytic activity, orientation of His 447 Barak_2002_Biochemistry_41_8245 Shafferman_2005_Chem.Biol.Interact_157-158_123 || Oxime interaction Cochran_2011_J.Biol.Chem_286_29718
AAA Change :
Allelic Variant :
Risk Factor :
Inhibitor :
Structure :
Disease by interaction :
Interact Gene Locus :
Xenobiotic sensitivity :
Modification : Hydrophobic subsite || Acyl specificity || Signal transduction
Torpedo_number : 331
Kinetic Parameter : Edrophonium_F338A_human-ACHE, Paranitrophenylacetate_F338A_human-ACHE, S-N-Propylthioacetate_F338A_human-ACHE, 3,3-dimethylbutylthioacetate_F338A_human-ACHE, Acetylthiocholine_F338A_human-ACHE, Hexamethonium_F338A_human-ACHE, BW284C51_F338A_human-ACHE, Propidium_F338A_human-ACHE, Decamethonium_F338A_human-ACHE, Tacrine_F338A_human-ACHE, HuperzineA_F338A_human-ACHE
News : No news
Comment :
p.F338A Phe338Ala (p.F369A Phe369Ala in primary sequence with 31 amino-acids signal peptide) Signal transduction: reduced kcat, marginal effect on inhibition by edrophonium\; Acyl pocket decreased catalytic activity, orientation of His 447
| Title : Oxime-assisted acetylcholinesterase catalytic scavengers of organophosphates that resist aging - Cochran_2011_J.Biol.Chem_286_29718 |
| Author(s) : Cochran R , Kalisiak J , Tuylu Kucukkilinc T , Radic Z , Garcia E , Zhang L , Ho KY , Amitai G , Kovarik Z , Fokin VV , Sharpless KB , Taylor P |
| Ref : Journal of Biological Chemistry , 286 :29718 , 2011 |
| Abstract : |
| PubMedSearch : Cochran_2011_J.Biol.Chem_286_29718 |
| PubMedID: 21730071 |
| Title : Next generation OP-bioscavengers: a circulatory long-lived 4-PEG hypolysine mutant of F338A-HuAChE with optimal pharmacokinetics and pseudo-catalytic characteristics - Kronman_2010_Chem.Biol.Interact_187_253 |
| Author(s) : Kronman C , Cohen O , Mazor O , Ordentlich A , Raveh L , Velan B , Shafferman A |
| Ref : Chemico-Biological Interactions , 187 :253 , 2010 |
| Abstract : |
| PubMedSearch : Kronman_2010_Chem.Biol.Interact_187_253 |
| PubMedID: 20005217 |
| Title : Functional requirements for the optimal catalytic configuration of the AChE active center - Shafferman_2005_Chem.Biol.Interact_157-158_123 |
| Author(s) : Shafferman A , Barak D , Kaplan D , Ordentlich A , Kronman C , Velan B |
| Ref : Chemico-Biological Interactions , 157-158 :123 , 2005 |
| Abstract : |
| PubMedSearch : Shafferman_2005_Chem.Biol.Interact_157-158_123 |
| PubMedID: 16256968 |
| Title : The aromatic trapping of the catalytic histidine is essential for efficient catalysis in acetylcholinesterase - Barak_2002_Biochemistry_41_8245 |
| Author(s) : Barak D , Kaplan D , Ordentlich A , Ariel N , Velan B , Shafferman A |
| Ref : Biochemistry , 41 :8245 , 2002 |
| Abstract : |
| PubMedSearch : Barak_2002_Biochemistry_41_8245 |
| PubMedID: 12081473 |
| 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 : 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 : |
| PubMedSearch : Barak_1994_J.Biol.Chem_269_6296 |
| PubMedID: 8119978 |
| 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 : |
| PubMedSearch : Ordentlich_1993_J.Biol.Chem_268_17083 |
| PubMedID: 8349597 |
| Gene_locus related to this paper: human-ACHE , human-BCHE |
| 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 : 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 : |
| 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: |