Homo sapiens (Human) acetylcholinesterase
Acetylcholinesterase (ACHE\; EC 3.1.1.7) controls synaptic and neurohumoral cholinergic activity by hydrolyzing the neurotransmitter acetylcholine. ACHE function relies on precise regulation of its expression and localization. In particular, alternative splicing of the 3-prime region of ACHE results in ACHE isoforms with distinct C-terminal peptides that determine posttranslational maturation and oligomeric assembly. Acetylcholinesterase is also found on the red blood cell membranes, where it constitutes the Yt blood group antigen. (H322N)
Family : ACHE
Block : C
Position in NCBI Life Tree : Homo sapiens
(Below N is a link to NCBI taxonomic web page and E link to ESTHER at designed phylum.)
> cellular organisms N E > Eukaryota N E > Opisthokonta N E > Metazoa N E > Eumetazoa N E > Bilateria N E > Deuterostomia N E > Chordata N E > Craniata N E > Vertebrata N E > Gnathostomata N E > Teleostomi N E > Euteleostomi N E > Sarcopterygii N E > Dipnotetrapodomorpha N E > Tetrapoda N E > Amniota N E > Mammalia N E > Theria N E > Eutheria N E > Boreoeutheria N E > Euarchontoglires N E > Primates N E > Haplorrhini N E > Simiiformes N E > Catarrhini N E > Hominoidea N E > Hominidae N E > Homininae N E > Homo N E > Homo sapiens N EMRPPQCLLHT PSLASPLLLL LLWLLGGGVG AEGREDAELL VTVRGGRLRG IRLKTPGGPV SAFLGIPFAE PPMGPRRFLP PEPKQPWSGV VDATTFQSVC YQYVDTLYPG FEGTEMWNPN RELSEDCLYL NVWTPYPRPT SPTPVLVWIY GGGFYSGASS LDVYDGRFLV QAERTVLVSM NYRVGAFGFL ALPGSREAPG NVGLLDQRLA LQWVQENVAA FGGDPTSVTL FGESAGAASV GMHLLSPPSR GLFHRAVLQS GAPNGPWATV GMGEARRRAT QLAHLVGCPP GGTGGNDTEL VACLRTRPAQ VLVNHEWHVL PQESVFRFSF VPVVDGDFLS DTPEALINAG DFHGLQVLVG VVKDEGSYFL VYGAPGFSKD NESLISRAEF LAGVRVGVPQ VSDLAAEAVV LHYTDWLHPE DPARLREALS DVVGDHNVVC PVAQLAGRLA AQGARVYAYV FEHRASTLSW PLWMGVPHGY EIEFIFGIPL DPSRNYTAEE KIFAQRLMRY WANFARTGDP NEPRDPKAPQ WPPYTAGAQQ YVSLDLRPLE VRRGLRAQAC AFWNRFLPKL LSATDTLDEA ERQWKAEFHR WSSYMVHWKN QFDHYSKQDR CSDL
Title : A New Class of Bi- and Trifunctional Sugar Oximes as Antidotes against Organophosphorus Poisoning - Da Silva_2022_J.Med.Chem_65_4649 |
Author(s) : Da Silva O , Probst N , Landry C , Hanak AS , Warnault P , Coisne C , Calas AG , Gosselet F , Courageux C , Gastellier AJ , Trancart M , Baati R , Dehouck MP , Jean L , Nachon F , Renard PY , Dias J |
Ref : Journal of Medicinal Chemistry , 65 :4649 , 2022 |
Abstract : |
PubMedSearch : Da Silva_2022_J.Med.Chem_65_4649 |
PubMedID: 35255209 |
Gene_locus related to this paper: human-ACHE |
Title : Crystal structure of human acetylcholinesterase in complex with tacrine: Implications for drug discovery - Dileep_2022_Int.J.Biol.Macromol_210_172 |
Author(s) : Dileep KV , Ihara K , Mishima-Tsumagari C , Kukimoto-Niino M , Yonemochi M , Hanada K , Shirouzu M , Zhang KYJ |
Ref : Int J Biol Macromol , 210 :172 , 2022 |
Abstract : |
PubMedSearch : Dileep_2022_Int.J.Biol.Macromol_210_172 |
PubMedID: 35526766 |
Gene_locus related to this paper: human-ACHE |
Title : Structural and dynamic effects of paraoxon binding to human acetylcholinesterase by X-ray crystallography and inelastic neutron scattering - Gerlits_2022_Structure_30_1538 |
Author(s) : Gerlits O , Fajer M , Cheng X , Blumenthal DK , Radic Z , Kovalevsky A |
Ref : Structure , 30 :1538 , 2022 |
Abstract : |
PubMedSearch : Gerlits_2022_Structure_30_1538 |
PubMedID: 36265484 |
Gene_locus related to this paper: human-ACHE |
Title : Fine-Tuning the Biological Profile of Multitarget Mitochondriotropic Antioxidants for Neurodegenerative Diseases - Chavarria_2021_Antioxidants.(Basel)_10_329 |
Author(s) : Chavarria D , Da Silva O , Benfeito S , Barreiro S , Garrido J , Cagide F , Soares P , Remiao F , Brazzolotto X , Nachon F , Oliveira PJ , Dias J , Borges F |
Ref : Antioxidants (Basel) , 10 :329 , 2021 |
Abstract : |
PubMedSearch : Chavarria_2021_Antioxidants.(Basel)_10_329 |
PubMedID: 33672269 |
Gene_locus related to this paper: human-ACHE , human-BCHE |
Title : Structural and Biochemical Insights into the Inhibition of Human Acetylcholinesterase by G-Series Nerve Agents and Subsequent Reactivation by HI-6 - McGuire_2021_Chem.Res.Toxicol_34_804 |
Author(s) : McGuire JR , Bester SM , Guelta MA , Cheung J , Langley C , Winemiller MD , Bae SY , Funk V , Myslinski JM , Pegan SD , Height JJ |
Ref : Chemical Research in Toxicology , 34 :804 , 2021 |
Abstract : |
PubMedSearch : McGuire_2021_Chem.Res.Toxicol_34_804 |
PubMedID: 33538594 |
Gene_locus related to this paper: human-ACHE |
Title : Covalent inhibition of hAChE by organophosphates causes homodimer dissociation through long-range allosteric effects - Blumenthal_2021_J.Biol.Chem__ |
Author(s) : Blumenthal DK , Cheng X , Fajer M , Ho KY , Rohrer J , Gerlits O , Taylor P , Juneja P , Kovalevsky A , Radic Z |
Ref : Journal of Biological Chemistry , :101007 , 2021 |
Abstract : |
PubMedSearch : Blumenthal_2021_J.Biol.Chem__ |
PubMedID: 34324828 |
Gene_locus related to this paper: human-ACHE |
Title : Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate - Zhou_2021_J.Med.Chem_64_1844 |
Author(s) : Zhou Y , Fu Y , Yin W , Li J , Wang W , Bai F , Xu S , Gong Q , Peng T , Hong Y , Zhang D , Liu Q , Xu Y , Xu HE , Zhang H , Jiang H , Liu H |
Ref : Journal of Medicinal Chemistry , 64 :1844 , 2021 |
Abstract : |
PubMedSearch : Zhou_2021_J.Med.Chem_64_1844 |
PubMedID: 33570950 |
Gene_locus related to this paper: human-ACHE |
Title : Room temperature crystallography of human acetylcholinesterase bound to a substrate analogue 4K-TMA: Towards a neutron structure - Gerlits_2021_Curr.Res.Struct.Biol_3_206 |
Author(s) : Gerlits O , Blakeley MP , Keen DA , Radic Z , Kovalevsky A |
Ref : Current Research in Structural Biology , 3 :206 , 2021 |
Abstract : |
PubMedSearch : Gerlits_2021_Curr.Res.Struct.Biol_3_206 |
PubMedID: 34541552 |
Gene_locus related to this paper: human-ACHE |
Title : Discovery of a Potent Dual Inhibitor of Acetylcholinesterase and Butyrylcholinesterase with Antioxidant Activity that Alleviates Alzheimer-like Pathology in Old APP\/PS1 Mice - Viayna_2021_J.Med.Chem_64_812 |
Author(s) : Viayna E , Coquelle N , Cieslikiewicz-Bouet M , Cisternas P , Oliva CA , Sanchez-Lopez E , Ettcheto M , Bartolini M , De Simone A , Ricchini M , Rendina M , Pons M , Firuzi O , Perez B , Saso L , Andrisano V , Nachon F , Brazzolotto X , Garcia ML , Camins A , Silman I , Jean L , Inestrosa NC , Colletier JP , Renard PY , Munoz-Torrero D |
Ref : Journal of Medicinal Chemistry , 64 :812 , 2021 |
Abstract : |
PubMedSearch : Viayna_2021_J.Med.Chem_64_812 |
PubMedID: 33356266 |
Gene_locus related to this paper: human-ACHE |
Title : Rational design, synthesis and evaluation of uncharged, smart bis-oxime antidotes of organophosphate-inhibited human acetylcholinesterase - Gorecki_2020_J.Biol.Chem_295_4079 |
Author(s) : Gorecki L , Gerlits O , Kong X , Cheng X , Blumenthal DK , Taylor P , Ballatore C , Kovalevsky A , Radic Z |
Ref : Journal of Biological Chemistry , 295 :4079 , 2020 |
Abstract : |
PubMedSearch : Gorecki_2020_J.Biol.Chem_295_4079 |
PubMedID: 32019865 |
Gene_locus related to this paper: human-ACHE |
Title : New evidence for dual binding site inhibitors of acetylcholinesterase as improved drugs for treatment of Alzheimer's disease - Zueva_2019_Neuropharmacol_155_131 |
Author(s) : Zueva IV , Dias J , Lushchekina SV , Semenov VE , Mukhamedyarov MA , Pashirova TN , Babaev VM , Nachon F , Petrova N , Nurullin LF , Zakharova LY , Ilyin VI , Masson P , Petrov KA |
Ref : Neuropharmacology , 155 :131 , 2019 |
Abstract : |
PubMedSearch : Zueva_2019_Neuropharmacol_155_131 |
PubMedID: 31132435 |
Gene_locus related to this paper: human-ACHE |
Title : The structural and biochemical impacts of monomerizing human acetylcholinesterase - Bester_2019_Protein.Sci_28_1106 |
Author(s) : Bester SM , Adipietro KA , Funk VL , Myslinski JM , Keul ND , Cheung J , Wilder PT , Wood ZA , Weber DJ , Height JJ , Pegan SD |
Ref : Protein Science , 28 :1106 , 2019 |
Abstract : |
PubMedSearch : Bester_2019_Protein.Sci_28_1106 |
PubMedID: 30993792 |
Gene_locus related to this paper: human-ACHE |
Title : A new crystal form of human acetylcholinesterase for exploratory room-temperature crystallography studies - Gerlits_2019_Chem.Biol.Interact_13ChEPon_ |
Author(s) : Gerlits O , Ho KY , Cheng X , Blumenthal D , Taylor P , Kovalevsky A , Radic Z |
Ref : Chemico-Biological Interactions , : , 2019 |
Abstract : |
PubMedSearch : Gerlits_2019_Chem.Biol.Interact_13ChEPon_ |
PubMedID: 31176713 |
Gene_locus related to this paper: human-ACHE |
Title : Productive reorientation of a bound oxime reactivator revealed in room temperature X-ray structures of native and VX-inhibited human acetylcholinesterase - Gerlits_2019_J.Biol.Chem_294_10607 |
Author(s) : Gerlits O , Kong X , Cheng X , Wymore T , Blumenthal DK , Taylor P , Radic Z , Kovalevsky A |
Ref : Journal of Biological Chemistry , 294 :10607 , 2019 |
Abstract : |
PubMedSearch : Gerlits_2019_J.Biol.Chem_294_10607 |
PubMedID: 31138650 |
Gene_locus related to this paper: human-ACHE |
Title : Synthesis and Molecular Properties of Nerve Agent Reactivator HLo-7 Dimethanesulfonate - Hsu_2019_ACS.Med.Chem.Lett_10_761 |
Author(s) : Hsu FL , Bae SY , McGuire J , Anderson DR , Bester SM , Height JJ , Pegan SD , Walz AJ |
Ref : ACS Med Chem Lett , 10 :761 , 2019 |
Abstract : |
PubMedSearch : Hsu_2019_ACS.Med.Chem.Lett_10_761 |
PubMedID: 31097996 |
Gene_locus related to this paper: human-ACHE |
Title : Counteracting tabun inhibition by reactivation by pyridinium aldoximes that interact with active center gorge mutants of acetylcholinesterase - Kovarik_2019_Toxicol.Appl.Pharmacol_372_40 |
Author(s) : Kovarik Z , Macek Hrvat N , Kalisiak J , Katalinic M , Sit RK , Zorbaz T , Radic Z , Fokin VV , Sharpless KB , Taylor P |
Ref : Toxicol Appl Pharmacol , 372 :40 , 2019 |
Abstract : |
PubMedSearch : Kovarik_2019_Toxicol.Appl.Pharmacol_372_40 |
PubMedID: 30978400 |
Gene_locus related to this paper: human-ACHE |
Title : Structural Insights of Stereospecific Inhibition of Human Acetylcholinesterase by VX and Subsequent Reactivation by HI-6 - Bester_2018_Chem.Res.Toxicol_31_1405 |
Author(s) : Bester SM , Guelta MA , Cheung J , Winemiller MD , Bae SY , Myslinski J , Pegan SD , Height JJ |
Ref : Chemical Research in Toxicology , 31 :1405 , 2018 |
Abstract : |
PubMedSearch : Bester_2018_Chem.Res.Toxicol_31_1405 |
PubMedID: 30462502 |
Gene_locus related to this paper: human-ACHE |
Title : Structure of a prereaction complex between the nerve agent sarin, its biological target acetylcholinesterase, and the antidote HI-6 - Allgardsson_2016_Proc.Natl.Acad.Sci.U.S.A_113_5514 |
Author(s) : Allgardsson A , Berg L , Akfur C , Hornberg A , Worek F , Linusson A , Ekstrom F |
Ref : Proc Natl Acad Sci U S A , 113 :5514 , 2016 |
Abstract : |
PubMedSearch : Allgardsson_2016_Proc.Natl.Acad.Sci.U.S.A_113_5514 |
PubMedID: 27140636 |
Gene_locus related to this paper: human-ACHE |
Title : Automated Structure- and Sequence-Based Design of Proteins for High Bacterial Expression and Stability - Goldenzweig_2016_Mol.Cell_63_337 |
Author(s) : Goldenzweig A , Goldsmith M , Hill SE , Gertman O , Laurino P , Ashani Y , Dym O , Unger T , Albeck S , Prilusky J , Lieberman RL , Aharoni A , Silman I , Sussman JL , Tawfik DS , Fleishman SJ |
Ref : Mol Cell , 63 :337 , 2016 |
Abstract : |
PubMedSearch : Goldenzweig_2016_Mol.Cell_63_337 |
PubMedID: 27425410 |
Gene_locus related to this paper: human-ACHE |
Title : HI-6 assisted catalytic scavenging of VX by acetylcholinesterase choline binding site mutants - Macek Hrvat_2016_Chem.Biol.Interact_259_148 |
Author(s) : Macek Hrvat N , Zunec S , Taylor P , Radic Z , Kovarik Z |
Ref : Chemico-Biological Interactions , 259 :148 , 2016 |
Abstract : |
PubMedSearch : Macek Hrvat_2016_Chem.Biol.Interact_259_148 |
PubMedID: 27083141 |
Gene_locus related to this paper: human-ACHE |
Title : Structures of paraoxon-inhibited human acetylcholinesterase reveal perturbations of the acyl loop and the dimer interface - Franklin_2016_Proteins_84_1246 |
Author(s) : Franklin MC , Rudolph MJ , Ginter C , Cassidy MS , Cheung J |
Ref : Proteins , 84 :1246 , 2016 |
Abstract : |
PubMedSearch : Franklin_2016_Proteins_84_1246 |
PubMedID: 27191504 |
Gene_locus related to this paper: human-ACHE |
Title : Crystal structures of human cholinesterases in complex with huprine W and tacrine: elements of specificity for anti-Alzheimer's drugs targeting acetyl- and butyryl-cholinesterase - Nachon_2013_Biochem.J_453_393 |
Author(s) : Nachon F , Carletti E , Ronco C , Trovaslet M , Nicolet Y , Jean L , Renard PY |
Ref : Biochemical Journal , 453 :393 , 2013 |
Abstract : |
PubMedSearch : Nachon_2013_Biochem.J_453_393 |
PubMedID: 23679855 |
Gene_locus related to this paper: human-ACHE , human-BCHE |
Title : Structures of Human Acetylcholinesterase Bound to Dihydrotanshinone I and Territrem B Show Peripheral Site Flexibility - Cheung_2013_ACS.Med.Chem.Lett_4_1091 |
Author(s) : Cheung J , Gary EN , Shiomi K , Rosenberry TL |
Ref : ACS Med Chem Lett , 4 :1091 , 2013 |
Abstract : |
PubMedSearch : Cheung_2013_ACS.Med.Chem.Lett_4_1091 |
PubMedID: 24900610 |
Gene_locus related to this paper: human-ACHE |
Title : Structures of human acetylcholinesterase in complex with pharmacologically important ligands - Cheung_2012_J.Med.Chem_55_10282 |
Author(s) : Cheung J , Rudolph MJ , Burshteyn F , Cassidy MS , Gary EN , Love J , Franklin MC , Height JJ |
Ref : Journal of Medicinal Chemistry , 55 :10282 , 2012 |
Abstract : |
PubMedSearch : Cheung_2012_J.Med.Chem_55_10282 |
PubMedID: 23035744 |
Gene_locus related to this paper: human-ACHE |
Title : Acetylcholinesterase: from 3D structure to function - Dvir_2010_Chem.Biol.Interact_187_10 |
Author(s) : Dvir H , Silman I , Harel M , Rosenberry TL , Sussman JL |
Ref : Chemico-Biological Interactions , 187 :10 , 2010 |
Abstract : |
PubMedSearch : Dvir_2010_Chem.Biol.Interact_187_10 |
PubMedID: 20138030 |
Gene_locus related to this paper: human-ACHE |
Title : Structural evidence that human acetylcholinesterase inhibited by tabun ages through O-dealkylation - Carletti_2010_J.Med.Chem_53_4002 |
Author(s) : Carletti E , Colletier JP , Dupeux F , Trovaslet M , Masson P , Nachon F |
Ref : Journal of Medicinal Chemistry , 53 :4002 , 2010 |
Abstract : |
PubMedSearch : Carletti_2010_J.Med.Chem_53_4002 |
PubMedID: 20408548 |
Gene_locus related to this paper: human-ACHE |
Title : Comparative analysis of the gene-dense ACHE\/TFR2 region on human chromosome 7q22 with the orthologous region on mouse chromosome 5 - Wilson_2001_Nucleic.Acids.Res_29_1352 |
Author(s) : Wilson MD , Riemer C , Martindale DW , Schnupf P , Boright AP , Cheung TL , Hardy DM , Schwartz S , Scherer SW , Tsui LC , Miller W , Koop BF |
Ref : Nucleic Acids Research , 29 :1352 , 2001 |
Abstract : |
PubMedSearch : Wilson_2001_Nucleic.Acids.Res_29_1352 |
PubMedID: 11239002 |
Gene_locus related to this paper: human-ACHE , mouse-ACHE |
Title : Structures of recombinant native and E202Q mutant human acetylcholinesterase complexed with the snake-venom toxin fasciculin-II - Kryger_2000_Acta.Crystallogr.D.Biol.Crystallogr_56_1385 |
Author(s) : Kryger G , Harel M , Giles K , Toker L , Velan B , Lazar A , Kronman C , Barak D , Ariel N , Shafferman A , Silman I , Sussman JL |
Ref : Acta Crystallographica D Biol Crystallogr , 56 :1385 , 2000 |
Abstract : |
PubMedSearch : Kryger_2000_Acta.Crystallogr.D.Biol.Crystallogr_56_1385 |
PubMedID: 11053835 |
Gene_locus related to this paper: human-ACHE |
Title : A transcription-activating polymorphism in the ACHE promoter associated with acute sensitivity to anti-acetylcholinesterases - Shapira_2000_Hum.Mol.Genet_9_1273 |
Author(s) : Shapira M , Tur-Kaspa I , Bosgraaf L , Livni N , Grant AD , Grisaru D , Korner M , Ebstein RP , Soreq H |
Ref : Hum Mol Genet , 9 :1273 , 2000 |
Abstract : |
PubMedSearch : Shapira_2000_Hum.Mol.Genet_9_1273 |
PubMedID: 10814709 |
Gene_locus related to this paper: human-ACHE |
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 : |
PubMedSearch : Ashani_1994_Mol.Pharmacol_45_555 |
PubMedID: 8145739 |
Gene_locus related to this paper: human-ACHE |
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 : |
PubMedSearch : Ordentlich_1993_J.Biol.Chem_268_17083 |
PubMedID: 8349597 |
Gene_locus related to this paper: human-ACHE , human-BCHE |
Title : Molecular cloning and construction of the coding region for human acetylcholinesterase reveals a G + C-rich attenuating structure - Soreq_1990_Proc.Natl.Acad.Sci.U.S.A_87_9688 |
Author(s) : Soreq H , Ben-Aziz R , Prody CA , Seidman S , Gnatt A , Neville LF , Lieman-Hurwitz J , Lev-Lehman E , Ginzberg D , Lipidot-Lifson Y |
Ref : Proceedings of the National Academy of Sciences of the United States of America , 87 :9688 , 1990 |
Abstract : |
PubMedSearch : Soreq_1990_Proc.Natl.Acad.Sci.U.S.A_87_9688 |
PubMedID: 2263619 |
Gene_locus related to this paper: human-ACHE |
Title : Purification and partial amino acid sequence analysis of human erythrocyte acetylcholinesterase - Chhajlani_1989_FEBS.Lett_247_279 |
Author(s) : Chhajlani V , Derr D , Earles B , Schmell ED , August T |
Ref : FEBS Letters , 247 :279 , 1989 |
Abstract : |
PubMedSearch : Chhajlani_1989_FEBS.Lett_247_279 |
PubMedID: 2714437 |
Gene_locus related to this paper: human-ACHE |