Gene Locus : human-ACHE
Mode of mutation : Site directed mutagenesis
Disease :
Summary : Omega loop No effect Velan_1996_FEBS.Lett_395_22 || Peripheral Anionic Site Affects conformation of active site and PAS Shafferman_1992_EMBO.J_11_3561 Shafferman_1992_4th.ChE.Meeting.Eilat__165 Shafferman_1993_Proc.Med.Def.Biosci.Rev_3_1097 Shafferman_1995_5th.ChE.Meeting.Madras__189 Shafferman_1996_Biochem.J_318_833 || Substrate inhibition Signal transduction Affects conformation of active site and PAS Shafferman_1992_EMBO.J_11_3561 Shafferman_1992_4th.ChE.Meeting.Eilat__165 Shafferman_1993_Proc.Med.Def.Biosci.Rev_3_1097 Shafferman_1995_5th.ChE.Meeting.Madras__189 Shafferman_1996_Biochem.J_318_833 || Heat and pressure stability strengthened heat or pressure stability Clery-Barraud_2002_Eur.J.Biochem_269_4297 || VX stereospecificity decrease in stereoselectivity Ordentlich_2004_Biochemistry_43_11255 Ordentlich_2005_Chem.Biol.Interact_157-158_191 || oxime interaction reactivation of tabun-inhibited human AChE. Rate constant 20-fold decreased for K027 and HLo-7. Unable to facilitate HI-6-mediated reactivation of tabun-hAChE Artursson_2009_Toxicology_265_108
AAA Change :
Allelic Variant :
Risk Factor :
Inhibitor :
Structure :
Disease by interaction :
Interact Gene Locus :
Xenobiotic sensitivity :
Modification : Omega loop || Peripheral Anionic Site || Substrate inhibition || Heat and pressure stability || Stability || Oxime interaction
Torpedo_number : 72
Kinetic Parameter : Acetylthiocholine_D74N_human-ACHE, Edrophonium_D74N_human-ACHE, Hexamethonium_D74N_human-ACHE, BW284C51_D74N_human-ACHE, Propidium_D74N_human-ACHE, Decamethonium_D74N_human-ACHE, Tacrine_D74N_human-ACHE, HuperzineA_D74N_human-ACHE
News : No news
Comment : p.D74N Asp74Asn (p.D105N Asp105Asn in primary sequence with 31 amino-acids signal peptide) Substrate inhibition\;Signal transduction Affects conformation of active site and PAS\; strengthened heat or pressure stability \;decrease in VX stereoselectivity\; reactivation of tabun-inhibited human AChE. Rate constant 20-fold decreased for K027 and HLo-7. Unable to facilitate HI-6-mediated reactivation of tabun-hAChE
| Title : Reactivation of tabun-hAChE investigated by structurally analogous oximes and mutagenesis - Artursson_2009_Toxicology_265_108 |
| Author(s) : Artursson E , Akfur C , Hornberg A , Worek F , Ekstrom F |
| Ref : Toxicology , 265 :108 , 2009 |
| Abstract : Artursson_2009_Toxicology_265_108 |
| ESTHER : Artursson_2009_Toxicology_265_108 |
| PubMedSearch : Artursson_2009_Toxicology_265_108 |
| PubMedID: 19761810 |
| Title : The role of AChE active site gorge in determining stereoselectivity of charged and noncharged VX enantiomers - Ordentlich_2005_Chem.Biol.Interact_157-158_191 |
| Author(s) : Ordentlich A , Barak D , Sod-Moriah G , Kaplan D , Mizrahi D , Segall Y , Kronman C , Karton Y , Lazar A , Marcus D , Velan B , Shafferman A |
| Ref : Chemico-Biological Interactions , 157-158 :191 , 2005 |
| Abstract : Ordentlich_2005_Chem.Biol.Interact_157-158_191 |
| ESTHER : Ordentlich_2005_Chem.Biol.Interact_157-158_191 |
| PubMedSearch : Ordentlich_2005_Chem.Biol.Interact_157-158_191 |
| PubMedID: 16289014 |
| Title : Stereoselectivity toward VX is determined by interactions with residues of the acyl pocket as well as of the peripheral anionic site of AChE - Ordentlich_2004_Biochemistry_43_11255 |
| Author(s) : Ordentlich A , Barak D , Sod-Moriah G , Kaplan D , Mizrahi D , Segall Y , Kronman C , Karton Y , Lazar A , Marcus D , Velan B , Shafferman A |
| Ref : Biochemistry , 43 :11255 , 2004 |
| Abstract : Ordentlich_2004_Biochemistry_43_11255 |
| ESTHER : Ordentlich_2004_Biochemistry_43_11255 |
| PubMedSearch : Ordentlich_2004_Biochemistry_43_11255 |
| PubMedID: 15366935 |
| Title : Pressure and heat inactivation of recombinant human acetylcholinesterase. Importance of residue E202 for enzyme stability - Clery-Barraud_2002_Eur.J.Biochem_269_4297 |
| Author(s) : Clery-Barraud C , Ordentlich A , Grosfeld H , Shafferman A , Masson P |
| Ref : European Journal of Biochemistry , 269 :4297 , 2002 |
| Abstract : Clery-Barraud_2002_Eur.J.Biochem_269_4297 |
| ESTHER : Clery-Barraud_2002_Eur.J.Biochem_269_4297 |
| PubMedSearch : Clery-Barraud_2002_Eur.J.Biochem_269_4297 |
| PubMedID: 12199708 |
| 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 : Structural modifications of the omega loop in human acetylcholinesterase - Velan_1996_FEBS.Lett_395_22 |
| Author(s) : Velan B , Barak D , Ariel N , Leitner M , Bino T , Ordentlich A , Shafferman A |
| Ref : FEBS Letters , 395 :22 , 1996 |
| Abstract : Velan_1996_FEBS.Lett_395_22 |
| ESTHER : Velan_1996_FEBS.Lett_395_22 |
| PubMedSearch : Velan_1996_FEBS.Lett_395_22 |
| PubMedID: 8849682 |
| 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 : Shafferman_1996_Biochem.J_318_833 |
| ESTHER : Shafferman_1996_Biochem.J_318_833 |
| 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 : 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 : 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 : 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: |