Details of the Drug Therapeutic Target (DTT)
General Information of Drug Therapeutic Target (DTT) (ID: TT1RS9F)
DTT Name | Acetylcholinesterase (AChE) | ||||
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Synonyms | YT; N-ACHE; ARACHE | ||||
Gene Name | ACHE | ||||
DTT Type |
Successful target
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[1] | |||
BioChemical Class |
Carboxylic ester hydrolase
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UniProt ID | |||||
TTD ID | |||||
3D Structure | |||||
EC Number |
EC 3.1.1.7
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Sequence |
MRPPQCLLHTPSLASPLLLLLLWLLGGGVGAEGREDAELLVTVRGGRLRGIRLKTPGGPV
SAFLGIPFAEPPMGPRRFLPPEPKQPWSGVVDATTFQSVCYQYVDTLYPGFEGTEMWNPN RELSEDCLYLNVWTPYPRPTSPTPVLVWIYGGGFYSGASSLDVYDGRFLVQAERTVLVSM NYRVGAFGFLALPGSREAPGNVGLLDQRLALQWVQENVAAFGGDPTSVTLFGESAGAASV GMHLLSPPSRGLFHRAVLQSGAPNGPWATVGMGEARRRATQLAHLVGCPPGGTGGNDTEL VACLRTRPAQVLVNHEWHVLPQESVFRFSFVPVVDGDFLSDTPEALINAGDFHGLQVLVG VVKDEGSYFLVYGAPGFSKDNESLISRAEFLAGVRVGVPQVSDLAAEAVVLHYTDWLHPE DPARLREALSDVVGDHNVVCPVAQLAGRLAAQGARVYAYVFEHRASTLSWPLWMGVPHGY EIEFIFGIPLDPSRNYTAEEKIFAQRLMRYWANFARTGDPNEPRDPKAPQWPPYTAGAQQ YVSLDLRPLEVRRGLRAQACAFWNRFLPKLLSATDTLDEAERQWKAEFHRWSSYMVHWKN QFDHYSKQDRCSDL |
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Function | Role in neuronal apoptosis. Terminates signal transduction at the neuromuscular junction by rapid hydrolysis of the acetylcholine released into the synaptic cleft. | ||||
KEGG Pathway | |||||
Reactome Pathway | |||||
Molecular Interaction Atlas (MIA) of This DTT
Molecular Interaction Atlas (MIA) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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15 Approved Drug(s) Targeting This DTT
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17 Clinical Trial Drug(s) Targeting This DTT
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54 Patented Agent(s) Targeting This DTT
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20 Discontinued Drug(s) Targeting This DTT
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2 Preclinical Drug(s) Targeting This DTT
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220 Investigative Drug(s) Targeting This DTT
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Molecular Expression Atlas (MEA) of This DTT
The Drug-Metabolizing Enzyme (DME) Role of This DTT
DTT DME Name | Acetylcholinesterase (ACHE) | |||||||||||||||||||||||||||||||||
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Gene Name | ACHE | |||||||||||||||||||||||||||||||||
2 Approved Drug(s) Metabolized by This DTT
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References
1 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2465). | ||||
---|---|---|---|---|---|
2 | Alpha6-containing nicotinic acetylcholine receptors dominate the nicotine control of dopamine neurotransmission in nucleus accumbens. Neuropsychopharmacology. 2008 Aug;33(9):2158-66. | ||||
3 | The effects of topical ocular application of 0.25% demecarium bromide on serum acetylcholinesterase levels in normal dogs. Vet Ophthalmol. 2003 Mar;6(1):23-5. | ||||
4 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | ||||
5 | Screening of acetylcholinesterase inhibitors by CE after enzymatic reaction at capillary inlet. J Sep Sci. 2009 May;32(10):1748-56. | ||||
6 | [From symptomatic to disease modifying therapy Recent developments in the pharmacotherapy of Alzheimer's disease]. Fortschr Neurol Psychiatr. 2009 Jun;77(6):326-33. | ||||
7 | Huperzine A attenuates cognitive deficits and brain injury in neonatal rats after hypoxia-ischemia. Brain Res. 2002 Sep 13;949(1-2):162-70. | ||||
8 | Rational design of alkylene-linked bis-pyridiniumaldoximes as improved acetylcholinesterase reactivators. Chem Biol. 2003 Jun;10(6):491-502. | ||||
9 | Acetylcholinesterase activity in Corbicula fluminea Mull., as a biomarker of organophosphate pesticide pollution in Pinacanauan River, Philippines. Environ Monit Assess. 2010 Jun;165(1-4):331-40. | ||||
10 | Neuromuscular blockade, reversal agent use, and operating room time: retrospective analysis of US inpatient surgeries. Curr Med Res Opin. 2009 Apr;25(4):943-50. | ||||
11 | Evidence that the clinical effects of cholinesterase inhibitors are related to potency and targeting of action. Int J Clin Pract Suppl. 2002 Jun;(127):6-19. | ||||
12 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
13 | Long-acting anticholinesterases for myasthenia gravis: synthesis and activities of quaternary phenylcarbamates of neostigmine, pyridostigmine and physostigmine. Bioorg Med Chem. 2010 Jul 1;18(13):4687-93. | ||||
14 | Activity, mechanism of action and pharmacokinetics of 2-tert-butylbenzothiazole and CGP 6140 (amocarzine) antifilarial drugs. Acta Trop. 1992 Aug;51(3-4):195-211. | ||||
15 | Eptastigmine: ten years of pharmacology, toxicology, pharmacokinetic, and clinical studies. CNS Drug Rev. 2001 Winter;7(4):369-86. | ||||
16 | The memory ameliorating effects of INM-176, an ethanolic extract of Angelica gigas, against scopolamine- or Abeta(1-42)-induced cognitive dysfunction in mice. J Ethnopharmacol. 2012 Sep 28;143(2):611-20. | ||||
17 | Potential clinical use of an adrenergic/cholinergic agent (HP 128) in the treatment of Alzheimer's disease. Ann N Y Acad Sci. 1991;640:263-7. | ||||
18 | Multifunctional Compound AD-35 Improves Cognitive Impairment and Attenuates the Production of TNF-alpha and IL-1beta in an Abeta25-35-induced Rat Model of Alzheimer's Disease. J Alzheimers Dis. 2017;56(4):1403-1417. | ||||
19 | Ladostigil: a novel multimodal neuroprotective drug with cholinesterase and brain-selective monoamine oxidase inhibitory activities for Alzheimer's disease treatment. Curr Drug Targets. 2012 Apr;13(4):483-94. | ||||
20 | A randomized phase I study of methanesulfonyl fluoride, an irreversible cholinesterase inhibitor, for the treatment of Alzheimer's disease. Br J Clin Pharmacol. 2013 May;75(5):1231-9. | ||||
21 | An overview of phenserine tartrate, a novel acetylcholinesterase inhibitor for the treatment of Alzheimer's disease. Curr Alzheimer Res. 2005 Jul;2(3):281-90. | ||||
22 | Effects of T-82, a novel acetylcholinesterase inhibitor, on impaired learning and memory in passive avoidance task in rats. Eur J Pharmacol. 2003 Mar 28;465(1-2):97-103. | ||||
23 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | ||||
24 | Phase I clinical trial with desoxypeganine, a new cholinesterase and selective MAO-A inhibitor: tolerance and pharmacokinetics study of escalating single oral doses. Methods Find Exp Clin Pharmacol. 2008 Mar;30(2):141-7. | ||||
25 | Oral administration of KW-5092, a novel gastroprokinetic agent with acetylcholinesterase inhibitory and acetylcholine release enhancing activities, causes a dose-dependent increase in the blood acetylcholine content of beagle dogs. Neurosci Lett. 1997 Mar 28;225(1):25-8. | ||||
26 | Preclinical and first-in-human evaluation of PRX-105, a PEGylated, plant-derived, recombinant human acetylcholinesterase-R. Toxicol Appl Pharmacol. 2015 Sep 15;287(3):202-9. | ||||
27 | A sensitive method for the determination of the novel cholinesterase inhibitor ZT-1 and its active metabolite huperzine A in rat blood using liquid chromatography/tandem mass spectrometry. Rapid Commun Mass Spectrom. 2004;18(6):651-6. | ||||
28 | Recent advances in acetylcholinesterase Inhibitors and Reactivators: an update on the patent literature (2012-2015).Expert Opin Ther Pat. 2017 Apr;27(4):455-476. | ||||
29 | A patent review of butyrylcholinesterase inhibitors and reactivators 2010-2017.Expert Opin Ther Pat. 2018 Jun;28(6):455-465. | ||||
30 | Synthesis and biological activity of putative mono-hydroxylated metabolites of velnacrine, Bioorg. Med. Chem. Lett. 2(8):865-870 (1992). | ||||
31 | Effect of oral administration of zanapezil (TAK-147) for 21 days on acetylcholine and monoamines levels in the ventral hippocampus of freely moving rats. Br J Pharmacol. 2005 Aug;145(8):1035-44. | ||||
32 | Biochemical pharmacology of N-acetyl-N-(methylcarbamoyloxy)-N'-methylurea (caracemide; NSC-253272). Biochem Pharmacol. 1986 Aug 15;35(16):2781-7. | ||||
33 | NXX-066 in patients with Alzheimer's disease: a bridging study. Life Sci. 1999;64(14):1215-21. | ||||
34 | A docking score function for estimating ligand-protein interactions: application to acetylcholinesterase inhibition. J Med Chem. 2004 Oct 21;47(22):5492-500. | ||||
35 | The effects of physostigmine on acetylcholinesterase activity of CSF plasma and brain. A comparison of intravenous and intraventricular administration in beagle dogs. Neuropharmacology. 1986 Oct;25(10):1167-77. | ||||
36 | Xanthine derivatives IBMX and S-9977-2 potentiate transmission at an Aplysia central cholinergic synapse. Brain Res. 1992 Jul 17;586(1):78-85. | ||||
37 | Pharmacological and biochemical assessment of SM-10888, a novel cholinesterase inhibitor. Jpn J Pharmacol. 1990 Jun;53(2):145-55. | ||||
38 | Effects of TAK-802, a novel acetylcholinesterase inhibitor, on distension-induced rhythmic bladder contractions in rats and guinea pigs. Eur J Pharmacol. 2004 Feb 6;485(1-3):299-305. | ||||
39 | Acetylcholinesterase inhibition by zifrosilone: pharmacokinetics and pharmacodynamics. Clin Pharmacol Ther. 1995 Jul;58(1):54-61. | ||||
40 | Potent beta-amyloid modulators. Neurodegener Dis. 2008;5(3-4):153-6. | ||||
41 | Galantamine, a cholinesterase inhibitor that allosterically modulates nicotinic receptors: effects on the course of Alzheimer's disease. Biol Psychiatry. 2001 Feb 1;49(3):289-99. | ||||
42 | Synthesis and in vitro evaluation of N-alkyl-7-methoxytacrine hydrochlorides as potential cholinesterase inhibitors in Alzheimer disease. Bioorg Med Chem Lett. 2010 Oct 15;20(20):6093-5. | ||||
43 | Novel tacrine analogues for potential use against Alzheimer's disease: potent and selective acetylcholinesterase inhibitors and 5-HT uptake inhibitors. J Med Chem. 1997 Oct 24;40(22):3516-23. | ||||
44 | PD 142676 (CI 1002), a novel anticholinesterase and muscarinic antagonist. Mol Neurobiol. 1994 Aug-Dec;9(1-3):93-106. | ||||
45 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004498) | ||||
46 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006757) | ||||
47 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006922) | ||||
48 | The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. | ||||
49 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017551) | ||||
50 | A novel acetylcholinesterase inhibitor, Ro 46-5934, which interacts with muscarinic M2 receptors. Biochem Soc Trans. 1994 Aug;22(3):755-8. | ||||
51 | Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely... J Med Chem. 2008 Jun 12;51(11):3154-70. | ||||
52 | Structure-based alignment and comparative molecular field analysis of acetylcholinesterase inhibitors. J Med Chem. 1996 Dec 20;39(26):5064-71. | ||||
53 | Isolation and cholinesterase-inhibition studies of sterols from Haloxylon recurvum. Bioorg Med Chem Lett. 2006 Feb;16(3):573-80. | ||||
54 | Synthesis and AChE inhibitory activity of new chiral tetrahydroacridine analogues from terpenic cyclanones. Eur J Med Chem. 2010 Feb;45(2):526-35. | ||||
55 | Preparation and in vitro screening of symmetrical bispyridinium cholinesterase inhibitors bearing different connecting linkage-initial study for My... Bioorg Med Chem Lett. 2010 Mar 1;20(5):1763-6. | ||||
56 | Synthesis and biological evaluation of a new series of berberine derivatives as dual inhibitors of acetylcholinesterase and butyrylcholinesterase. Bioorg Med Chem. 2010 Jun 15;18(12):4475-84. | ||||
57 | Planarity and constraint of the carbonyl groups in 1,2-diones are determinants for selective inhibition of human carboxylesterase 1. J Med Chem. 2007 Nov 15;50(23):5727-34. | ||||
58 | Efficient method for high-throughput virtual screening based on flexible docking: discovery of novel acetylcholinesterase inhibitors. J Med Chem. 2004 Sep 23;47(20):4818-28. | ||||
59 | A structure-based design approach to the development of novel, reversible AChE inhibitors. J Med Chem. 2001 Sep 27;44(20):3203-15. | ||||
60 | Active site directed docking studies: synthesis and pharmacological evaluation of cis-2,6-dimethyl piperidine sulfonamides as inhibitors of acetylc... Eur J Med Chem. 2009 Oct;44(10):4057-62. | ||||
61 | Acetylcholinesterase inhibitors from the toadstool Cortinarius infractus. Bioorg Med Chem. 2010 Mar 15;18(6):2173-2177. | ||||
62 | Homobivalent quinazolinimines as novel nanomolar inhibitors of cholinesterases with dirigible selectivity toward butyrylcholinesterase. J Med Chem. 2006 Sep 7;49(18):5411-3. | ||||
63 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | ||||
64 | Acetylcholinesterase inhibition by alkaloids of the ant's venom Monomorium minutum, Bioorg. Med. Chem. Lett. 5(11):1131-1132 (1995). | ||||
65 | Design, synthesis and evaluation of 2,4-disubstituted pyrimidines as cholinesterase inhibitors. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3606-9. | ||||
66 | Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents. J Med Chem. 2010 May 13;53(9):3611-7. | ||||
67 | Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases. J Med Chem. 2005 Apr 21;48(8):2906-15. | ||||
68 | Synthesis, anticholinesterase activity and structure-activity relationships of m-Aminobenzoic acid derivatives. Bioorg Med Chem Lett. 2003 May 19;13(10):1825-7. | ||||
69 | Synthesis and evaluation of novel rutaecarpine derivatives and related alkaloids derivatives as selective acetylcholinesterase inhibitors. Eur J Med Chem. 2010 Apr;45(4):1415-23. | ||||
70 | Design, synthesis, and acetylcholinesterase inhibitory activity of novel coumarin analogues. Bioorg Med Chem. 2008 Sep 1;16(17):8011-21. | ||||
71 | Homo- and hetero-bivalent edrophonium-like ammonium salts as highly potent, dual binding site AChE inhibitors. Bioorg Med Chem. 2008 Aug 1;16(15):7450-6. | ||||
72 | Cholinesterase inhibitors: SAR and enzyme inhibitory activity of 3-[omega-(benzylmethylamino)alkoxy]xanthen-9-ones. Bioorg Med Chem. 2007 Jan 1;15(1):575-85. | ||||
73 | Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97. | ||||
74 | Synthesis and biological evaluation of helicid analogues as novel acetylcholinesterase inhibitors. Eur J Med Chem. 2008 Jan;43(1):166-73. | ||||
75 | Design, synthesis, evaluation and QSAR analysis of N(1)-substituted norcymserine derivatives as selective butyrylcholinesterase inhibitors. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1718-20. | ||||
76 | Synthesis, in vitro assay, and molecular modeling of new piperidine derivatives having dual inhibitory potency against acetylcholinesterase and Abe... Bioorg Med Chem. 2007 Oct 15;15(20):6596-607. | ||||
77 | Structure and anti-acetylcholinesterase activity of 4 alpha-(hydroxymethyl)-4 alpha-demethylterritrem B. J Nat Prod. 1997 Aug;60(8):842-3. | ||||
78 | The synthesis and in vitro acetylcholinesterase and butyrylcholinesterase inhibitory activity of tacrine (Cognex ) derivaties, Bioorg. Med. Chem. Lett. 2(8):861-864 (1992). | ||||
79 | Novel and potent tacrine-related hetero- and homobivalent ligands for acetylcholinesterase and butyrylcholinesterase. Bioorg Med Chem Lett. 2001 Jul 9;11(13):1779-82. | ||||
80 | Pyrano[3,2-c]quinoline-6-chlorotacrine hybrids as a novel family of acetylcholinesterase- and beta-amyloid-directed anti-Alzheimer compounds. J Med Chem. 2009 Sep 10;52(17):5365-79. | ||||
81 | 6-Hydroxy- and 6-methoxy-beta-carbolines as acetyl- and butyrylcholinesterase inhibitors. Bioorg Med Chem Lett. 2006 Nov 15;16(22):5840-3. | ||||
82 | Synthesis, biological evaluation and molecular modeling of oxoisoaporphine and oxoaporphine derivatives as new dual inhibitors of acetylcholinester... Eur J Med Chem. 2009 Jun;44(6):2523-32. | ||||
83 | Novel heterobivalent tacrine derivatives as cholinesterase inhibitors with notable selectivity toward butyrylcholinesterase. J Med Chem. 2006 Dec 14;49(25):7540-4. | ||||
84 | Synthesis, biological evaluation, and molecular modeling of berberine derivatives as potent acetylcholinesterase inhibitors. Bioorg Med Chem. 2010 Feb;18(3):1244-51. | ||||
85 | Targeting Alzheimer's disease: Novel indanone hybrids bearing a pharmacophoric fragment of AP2238. Bioorg Med Chem. 2010 Mar 1;18(5):1749-60. | ||||
86 | Multi-target-directed coumarin derivatives: hAChE and BACE1 inhibitors as potential anti-Alzheimer compounds. Bioorg Med Chem Lett. 2008 Jan 1;18(1):423-6. | ||||
87 | DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-41. | ||||
88 | Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors. J Med Chem. 2005 Feb 10;48(3):655-7. | ||||
89 | Cholinesterases: new roles in brain function and in Alzheimer's disease. Neurochem Res. 2003 Apr;28(3-4):515-22. | ||||
90 | Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inne... J Med Chem. 2008 Nov 27;51(22):7308-12. | ||||
91 | Carinatumins A-C, new alkaloids from Lycopodium carinatum inhibiting acetylcholinesterase. Bioorg Med Chem. 2007 Feb 15;15(4):1703-7. | ||||
92 | Structural determinants of Torpedo californica acetylcholinesterase inhibition by the novel and orally active carbamate based anti-alzheimer drug g... J Med Chem. 2006 Aug 24;49(17):5051-8. | ||||
93 | Activation of the endocannabinoid system by organophosphorus nerve agents. Nat Chem Biol. 2008 Jun;4(6):373-8. | ||||
94 | Synthesis of the novel series of bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against chlorpy... Bioorg Med Chem Lett. 2006 Feb;16(3):622-7. | ||||
95 | Indole alkaloids from Ervatamia hainanensis with potent acetylcholinesterase inhibition activities. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6185-7. | ||||
96 | PET imaging of brain acetylcholinesterase using [11C]CP-126,998, a brain selective enzyme inhibitor. Synapse. 2002 Jul;45(1):1-9. | ||||
97 | Cryptadines A and B, novel C27N3-type pentacyclic alkaloids from Lycopodium cryptomerinum. Bioorg Med Chem. 2007 Dec 15;15(24):7803-8. | ||||
98 | Novel carbamates as orally active acetylcholinesterase inhibitors found to improve scopolamine-induced cognition impairment: pharmacophore-based vi... J Med Chem. 2010 Sep 9;53(17):6490-505. | ||||
99 | Synthesis and structure-activity relationship of Huprine derivatives as human acetylcholinesterase inhibitors. Bioorg Med Chem. 2009 Jul 1;17(13):4523-36. | ||||
100 | Synthesis and pharmacological evaluation of huprine-tacrine heterodimers: subnanomolar dual binding site acetylcholinesterase inhibitors. J Med Chem. 2005 Mar 24;48(6):1701-4. | ||||
101 | Isosorbide-2-carbamate esters: potent and selective butyrylcholinesterase inhibitors. J Med Chem. 2008 Oct 23;51(20):6400-9. | ||||
102 | Isosorbide-based cholinesterase inhibitors; replacement of 5-ester groups leading to increased stability. Bioorg Med Chem. 2010 Feb;18(3):1045-53. | ||||
103 | Toward a rational design of multitarget-directed antioxidants: merging memoquin and lipoic acid molecular frameworks. J Med Chem. 2009 Dec 10;52(23):7883-6. | ||||
104 | Characterization of Acetylcholinesterase Inhibitory Constituents from Annona glabra Assisted by HPLC Microfractionation. J Nat Prod. 2010 Oct 22;73(10):1632-5. | ||||
105 | 4-Phenylcoumarins from Mesua elegans with acetylcholinesterase inhibitory activity. Bioorg Med Chem. 2010 Nov 15;18(22):7873-7. | ||||
106 | Bis-(-)-nor-meptazinols as novel nanomolar cholinesterase inhibitors with high inhibitory potency on amyloid-beta aggregation. J Med Chem. 2008 Apr 10;51(7):2027-36. | ||||
107 | N-Alkylated galanthamine derivatives: Potent acetylcholinesterase inhibitors from Leucojum aestivum. Bioorg Med Chem Lett. 2008 Apr 1;18(7):2263-6. | ||||
108 | Litebamine N-homologues: preparation and anti-acetylcholinesterase activity. J Nat Prod. 1998 Jan;61(1):46-50. | ||||
109 | Differential binding of phenothiazine urea derivatives to wild-type human cholinesterases and butyrylcholinesterase mutants. Bioorg Med Chem. 2010 Mar 15;18(6):2232-2244. | ||||
110 | Petrosamine, a potent anticholinesterase pyridoacridine alkaloid from a Thai marine sponge Petrosia n. sp. Bioorg Med Chem. 2008 Jul 1;16(13):6560-7. | ||||
111 | Taspine: bioactivity-guided isolation and molecular ligand-target insight of a potent acetylcholinesterase inhibitor from Magnolia x soulangiana. J Nat Prod. 2006 Sep;69(9):1341-6. | ||||
112 | Acetylcholinesterase inhibition by territrem B derivatives. J Nat Prod. 1995 Jun;58(6):857-62. | ||||
113 | Multi-target-directed ligands to combat neurodegenerative diseases. J Med Chem. 2008 Feb 14;51(3):347-72. | ||||
114 | Indole glucoalkaloids from Chimarrhis turbinata and their evaluation as antioxidant agents and acetylcholinesterase inhibitors. J Nat Prod. 2004 Nov;67(11):1882-5. | ||||
115 | Acetylcholinesterase inhibitors: synthesis and structure-activity relationships of omega-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)- methyl]aminoalkox... J Med Chem. 1998 Oct 8;41(21):3976-86. | ||||
116 | How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | ||||
117 | Kinetic characterization of cholinesterases and a therapeutically valuable cocaine hydrolase for their catalytic activities against heroin and its metabolite 6-monoacetylmorphine. Chem Biol Interact. 2018 Sep 25;293:107-114. | ||||