Gene Locus : human-ACHE
Mode of mutation : Site directed mutagenesis
Disease :
Summary : Acyl specificity Acyl pocket, OP-specificity.inhanced affinity for BTC 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 Ordentlich_1995_5th.ChE.Meeting.Madras__221 Shafferman_1995_5th.ChE.Meeting.Madras__189 || OP-specificity increased reactivity to DFP DEFP and paraoxon Shafferman_1993_Proc.Med.Def.Biosci.Rev_3_1097 Ashani_1994_Mol.Pharmacol_45_555 Barak_1994_J.Biol.Chem_269_6296 Ordentlich_1995_5th.ChE.Meeting.Madras__221 Shafferman_1995_5th.ChE.Meeting.Madras__189 Ordentlich_1996_J.Biol.Chem_271_11953 || Acyl specificity Acyl pocket, decreased catalytic activity, orientation of His 447 Barak_2002_Biochemistry_41_8245 || VX stereospecificity decrease in stereoselectivity Ordentlich_2004_Biochemistry_43_11255 Ordentlich_2005_Chem.Biol.Interact_157-158_191
AAA Change :
Allelic Variant :
Risk Factor :
Inhibitor :
Structure :
Disease by interaction :
Interact Gene Locus :
Xenobiotic sensitivity :
Modification : Acyl specificity
Torpedo_number : 288
Kinetic Parameter : Acetylthiocholine_F295A_human-ACHE, Edrophonium_F295A_human-ACHE, Hexamethonium_F295A_human-ACHE, BW284C51_F295A_human-ACHE, Propidium_F295A_human-ACHE, Decamethonium_F295A_human-ACHE, Tacrine_F295A_human-ACHE, HuperzineA_F295A_human-ACHE
News : No news
Comment : p.F295A Phe295Ala (p.F326A Phe326Ala in primary sequence with 31 amino-acids signal peptide) Acyl specificity\;Acyl pocket, OP-specificity.inhanced affinity for BTC\; increased reactivity to DFP DEFP and paraoxon, decreased catalytic activity, orientation of His 447
| 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 : 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 : Barak_2002_Biochemistry_41_8245 |
| ESTHER : Barak_2002_Biochemistry_41_8245 |
| 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 : Ariel_1998_Biochem.J_335_95 |
| ESTHER : Ariel_1998_Biochem.J_335_95 |
| 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 : Ordentlich_1996_J.Biol.Chem_271_11953 |
| ESTHER : Ordentlich_1996_J.Biol.Chem_271_11953 |
| PubMedSearch : Ordentlich_1996_J.Biol.Chem_271_11953 |
| PubMedID: 8662593 |
| 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 : 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 : 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 |