Torpedo_number Report for: 84

caeel-ACHE1

Mutation	Kin.	Type	Evaluation system	Effect	Reference
W99X		Random	Silent variant	Random ace-1(p1000) TGG to TGA	Talesa_1995_FEBS.Lett_357_265

drome-ACHE

Mutation	Type	Evaluation system	Effect	Reference
W121E	sdm	Back door hypothesis	enlarge back channel	Nachon_2008_Febs.J_275_2659
W121A/ W359A	sdm	Insecticide sensitivity		Stojan_2016_Chem.Biol.Interact_259_110
W121Y	sdm	Insecticide sensitivity		Boublik_2002_Protein.Eng_15_43
W121A	sdm	Binding of Triton X-100 studies	no effect on Triton X-100 binding	Marcel_2000_J.Biol.Chem_275_11603
W121A	sdm	Insecticide sensitivity		Boublik_2002_Protein.Eng_15_43
W121A	sdm	Back door hypothesis	enlarge back channel	Nachon_2008_Febs.J_275_2659

human-ACHE : (kinetic parameters)

Mutation	Kin.	Type	Evaluation system	Effect	Reference
W86A	kin	sdm	Choline binding site	Choline binding site/signal transductioncation-aromatic interaction, 660 fold decrease affinity for ACTh no effect on uncharged substrate,	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, Kronman_1994_J.Biol.Chem_269_27819
W86A	kin	sdm	Signal transduction	Y133 maintains the correct orientation of W86	Shafferman_1995_5th.ChE.Meeting.Madras__189, Ordentlich_1995_J.Biol.Chem_270_2082, Shafferman_1996_Biochem.J_318_833
W86F	kin	sdm	Choline binding site	cation-aromatic interaction, 660 fold decrease affinity for ACTh no effect on uncharged substrate	Ordentlich_1995_J.Biol.Chem_270_2082
W86F	kin	sdm	Signal transduction	Y133 maintains the correct orientation of W86	Shafferman_1995_5th.ChE.Meeting.Madras__189, Ordentlich_1995_J.Biol.Chem_270_2082
W86E	kin	sdm	Choline binding site	cation-aromatic interaction, 660 fold decrease affinity for ACTh no effect on uncharged substrate	Ordentlich_1995_J.Biol.Chem_270_2082, Shafferman_1995_5th.ChE.Meeting.Madras__189
W86E	kin	sdm	Signal transduction	Y133 maintains the correct orientation of W86	Ordentlich_1995_J.Biol.Chem_270_2082, Shafferman_1995_5th.ChE.Meeting.Madras__189

human-BCHE : (kinetic parameters)

Mutation	Kin.	Type	Evaluation system	Effect	Reference
W82A		sdm	Succinylthiocholine binding	No binding of succinylthiocholine	Masson_1997_Biochemistry_36_2266
W82A		sdm	Substrate activation	substrate activation	Masson_2001_Biochim.Biophys.Acta_1544_166
W82A		sdm	Aging	W82A increases half-life of aging by DFP 13 times	Masson_1997_Biochem.J_327_601
W82A		sdm	Aricept~Donepezil~E2020 inhibition	no inhibition at >120uM	Saxena_2003_Eur.J.Biochem_270_4447
W82Y	kin	sdm	Choline binding site	increase of Km for BTCh and Ki for inhibitors tested	Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_142
W82F	kin	sdm	Choline binding site	increase of Km for BTCh and Ki for inhibitors tested	Loewenstein-Lichtenstein_1996_Mol.Pharmacol_50_1423

mouse-ACHE

Mutation	Type	Evaluation system	Effect	Reference
W86A	sdm	Fasciculin inhibition	Fas becomes an allosteric activator instead of an inhibitor for certain substr.	Radic_1995_J.Biol.Chem_270_20391, Ashani_1995_5th.ChE.Meeting.Madras__133
W86A	sdm	Aricept~Donepezil~E2020 inhibition	300-fold increase in Ki vs WT	Saxena_2003_Eur.J.Biochem_270_4447
W86F	sdm	Fasciculin inhibition	allosteric control of AChE catalysis by Fasciculin	Radic_1995_J.Biol.Chem_270_20391, Ashani_1995_5th.ChE.Meeting.Madras__133
W86Y	sdm	Fasciculin inhibition	allosteric control of AChE catalysis by Fasciculin	Radic_1995_J.Biol.Chem_270_20391
W86Y	sdm	Choline binding site	allosteric control of AChE catalysis by Fasciculin	Ashani_1995_5th.ChE.Meeting.Madras__133

Send your questions or comments to :Mail to: Nicolas Lenfant, Thierry Hotelier, Yves Bourne, Pascale Marchot and Arnaud Chatonnet.Please cite: Lenfant 2013 Nucleic.Acids.Res. or Marchot Chatonnet 2012 Prot.Pept Lett.

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