Gene Locus : human-ACHE
Mode of mutation : Site directed mutagenesis
Disease :
Summary : Catalysis Decrease in catalytic and bimolecular constant, identical effect on charge and uncharged substrate, affects acylation-deacylation steps and not the noncovalent complex formation 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 || H-bond network Decrease in catalytic and bimolecular constant, identical effect on charge and uncharged substrate, affects acylation-deacylation steps and not the noncovalent complex formation 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 E202 mutant not inhibited at high substrate concentration 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 || Acylation,Phosphorylation low effect on inhibition by DFP and DEFP but high for Paraoxon Ordentlich_1995_5th.ChE.Meeting.Madras__221 Ordentlich_1996_J.Biol.Chem_271_11953 Shafferman_1996_Biochem.J_318_833 || Aging E202 contributes to the aging process by stabilizing the imidazolium His447 Shafferman_1996_Biochem.J_318_833
AAA Change :
Allelic Variant :
Risk Factor :
Inhibitor :
Structure :
Disease by interaction :
Interact Gene Locus :
Xenobiotic sensitivity :
Modification : Acylation,Phosphorylation || Substrate inhibition || Aging || H-bond network
Torpedo_number : 199
Kinetic Parameter : BW284C51_E202A_human-ACHE, Decamethonium_E202A_human-ACHE, Propidium_E202A_human-ACHE, Edrophonium_E202A_human-ACHE, Acetylthiocholine_E202A_human-ACHE, Tacrine_E202A_human-ACHE, HuperzineA_E202A_human-ACHE
News : No news
Comment :
p.E202A Glu202Ala (p.E233A Glu233Ala in primary sequence with 31 amino-acids signal peptide) Catalysis\;Decrease in catalytic and bimolecular constant, identical effect on charge and uncharged substrate, affects acylation-deacylation steps and not the noncovalent complex formation\; H-bond network\; not inhibited at high substrate concentration\; Acylation,Phosphorylation\;low effect on inhibition by DFP and DEFP but high for Paraoxon\; Aging:E202 contributes to the aging process by stabilizing the imidazolium His447
| 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 : The architecture of human acetylcholinesterase active center probed by interactions with selected organophosphate inhibitors - Ordentlich_1996_J.Biol.Chem_271_11953 |
| Author(s) : Ordentlich A , Barak D , Kronman C , Ariel N , Segall Y , Velan B , Shafferman A |
| Ref : Journal of Biological Chemistry , 271 :11953 , 1996 |
| Abstract : |
| PubMedSearch : Ordentlich_1996_J.Biol.Chem_271_11953 |
| PubMedID: 8662593 |
| 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 : 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 |
| Title : Amino Acids Determining Specificity to OP-Agents and Facilitating the Aging Process in Human Acetylcholinesterase - |
| Author(s) : Ordentlich A , Kronman C , Stein D , Ariel N , Reuveny S , Marcus D , Segall Y , Barak D , Velan B , Shafferman A |
| 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. :221 , 1995 |
| PubMedID: |
| 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 : 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 |