Gene Locus : mouse-ACHE
Mode of mutation : Site directed mutagenesis
Disease :
Summary : Signal transduction responsible for the 1800 fold difference in Ki for ethopropazine AChE\/BChE Radic_1993_Biochemistry_32_12074 Radic_1994_J.Biol.Chem_269_11233 Saxena_1994_Protein.Sci_3_1770 || Aricept~Donepezil~E2020 inhibition decrease Ki vs WT Saxena_2003_Eur.J.Biochem_270_4447 || Oxime interaction enlargement of the active site of the gorge Kovarik_2006_Biochem.Biophys.Res.Commun_342_973 Kovarik_2007_Toxicology_233_79 || Oxime interaction Kovarik_2004_Biochemistry_43_3222
AAA Change :
Allelic Variant :
Risk Factor :
Inhibitor :
Structure : 2XUF || 2XUG || 2XUH || 2XUI || 2XUJ || 2XUK || 2XUP || 2XUQ || 2XUD
Disease by interaction :
Interact Gene Locus :
Xenobiotic sensitivity :
Modification : Signal transduction || Substrate inhibition || Oxime interaction || Aricept~Donepezil~E2020 inhibition
Torpedo_number : 330
Kinetic Parameter : Acetylthiocholine_Y337A_mouse-ACHE, Edrophonium_Y337A_mouse-ACHE, Acridine_Y337A_mouse-ACHE, N-Methyl-acridinium_Y337A_mouse-ACHE, 9-Aminoacridine_Y337A_mouse-ACHE, Tacrine_Y337A_mouse-ACHE, Promazine_Y337A_mouse-ACHE, Chlorpromazine_Y337A_mouse-ACHE, Promethazine_Y337A_mouse-ACHE, Ethopropazine_Y337A_mouse-ACHE, WT-fasciculin2_Y337A_mouse-ACHE
News : DECEMBER-08-2010
Comment :
enlargement of the active site of the gorge || p.Tyr337Ala
| Title : Reactivation of Tabun-inhibited Acetylcholinesterase Investigated by Two Oximes and Mutagenesis - Katalinic_2012_Croatica.Chem.Acta_85_209 |
| Author(s) : Katalinic M , Kovarik Z |
| Ref : Croatica Chemica Acta , 85 :209\ , 2012 |
| Abstract : |
| PubMedSearch : Katalinic_2012_Croatica.Chem.Acta_85_209 |
| PubMedID: |
| Title : Conformational remodeling of femtomolar inhibitor-acetylcholinesterase complexes in the crystalline state - Bourne_2010_J.Am.Chem.Soc_132_18292 |
| Author(s) : Bourne Y , Radic Z , Taylor P , Marchot P |
| Ref : Journal of the American Chemical Society , 132 :18292 , 2010 |
| Abstract : |
| PubMedSearch : Bourne_2010_J.Am.Chem.Soc_132_18292 |
| PubMedID: 21090615 |
| Gene_locus related to this paper: mouse-ACHE |
| Title : Mutation of acetylcholinesterase to enhance oxime-assisted catalytic turnover of methylphosphonates - Kovarik_2007_Toxicology_233_79 |
| Author(s) : Kovarik Z , Radic Z , Berman HA , Taylor P |
| Ref : Toxicology , 233 :79 , 2007 |
| Abstract : |
| PubMedSearch : Kovarik_2007_Toxicology_233_79 |
| PubMedID: 17046138 |
| Title : Active site mutant acetylcholinesterase interactions with 2-PAM, HI-6, and DDVP - Kovarik_2006_Biochem.Biophys.Res.Commun_342_973 |
| Author(s) : Kovarik Z , Ciban N , Radic Z , Simeon-Rudolf V , Taylor P |
| Ref : Biochemical & Biophysical Research Communications , 342 :973 , 2006 |
| Abstract : |
| PubMedSearch : Kovarik_2006_Biochem.Biophys.Res.Commun_342_973 |
| PubMedID: 16598855 |
| Title : Aromatic amino-acid residues at the active and peripheral anionic sites control the binding of E2020 (Aricept) to cholinesterases - Saxena_2003_Eur.J.Biochem_270_4447 |
| Author(s) : Saxena A , Fedorko JM , Vinayaka CR , Medhekar R , Radic Z , Taylor P , Lockridge O , Doctor BP |
| Ref : European Journal of Biochemistry , 270 :4447 , 2003 |
| Abstract : |
| PubMedSearch : Saxena_2003_Eur.J.Biochem_270_4447 |
| PubMedID: 14622273 |
| Title : Inactivation studies of acetylcholinesterase with phenylmethylsulfonyl fluoride - Kraut_2000_Mol.Pharmacol_57_1243 |
| Author(s) : Kraut D , Goff H , Pai RK , Hosea NA , Silman I , Sussman JL , Taylor P , Voet JG |
| Ref : Molecular Pharmacology , 57 :1243 , 2000 |
| Abstract : |
| PubMedSearch : Kraut_2000_Mol.Pharmacol_57_1243 |
| PubMedID: 10825396 |
| Title : Amino acid residues involved in the interaction of acetylcholinesterase and butyrylcholinesterase with the carbamates Ro 02-0683 and bambuterol, and with terbutaline - Kovarik_1999_Biochim.Biophys.Acta_1433_261 |
| Author(s) : Kovarik Z , Radic Z , Grgas B , Skrinjaric-Spoljar M , Reiner E , Simeon-Rudolf V |
| Ref : Biochimica & Biophysica Acta , 1433 :261 , 1999 |
| Abstract : |
| PubMedSearch : Kovarik_1999_Biochim.Biophys.Acta_1433_261 |
| PubMedID: 10446376 |
| Title : Site of fasciculin interaction with acetylcholinesterase - Radic_1994_J.Biol.Chem_269_11233 |
| Author(s) : Radic Z , Duran R , Vellom DC , Li Y , Cervenansky C , Taylor P |
| Ref : Journal of Biological Chemistry , 269 :11233 , 1994 |
| Abstract : |
| PubMedSearch : Radic_1994_J.Biol.Chem_269_11233 |
| PubMedID: 8157652 |
| Title : Identification of amino acid residues involved in the binding of Huperzine A to cholinesterases - Saxena_1994_Protein.Sci_3_1770 |
| Author(s) : Saxena A , Qian N , Kovach IM , Kozikowski AP , Pang YP , Vellom DC , Radic Z , Quinn DM , Taylor P , Doctor BP |
| Ref : Protein Science , 3 :1770 , 1994 |
| Abstract : |
| PubMedSearch : Saxena_1994_Protein.Sci_3_1770 |
| PubMedID: 7849595 |
| Title : Three distinct domains in the cholinesterase molecule confer selectivity for acetyl- and butyrylcholinesterase inhibitors - Radic_1993_Biochemistry_32_12074 |
| Author(s) : Radic Z , Pickering NA , Vellom DC , Camp S , Taylor P |
| Ref : Biochemistry , 32 :12074 , 1993 |
| Abstract : |
| PubMedSearch : Radic_1993_Biochemistry_32_12074 |
| PubMedID: 8218285 |