Two Step Synthesis of a Non-symmetric Acetylcholinesterase Reactivator [PDF]
Molecules, 2007 The newly developed and very promising acetylcholinesterase reactivator (E)-1- (2-hydroxyiminomethylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide was prepared using two different pathways via a two-step synthesis involving the ...
Vit Koleckar +5 more
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Molecular modeling studies on the multistep reactivation process of organophosphate-inhibited acetylcholinesterase and butyrylcholinesterase [PDF]
, 2021 Poisoning with organophosphorus compounds used as pesticides or misused as chemical weapons remains a serious threat to human health and life.
Bajda, Marek +6 more
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Pyridinium-2-carbaldoximes with quinolinium carboxamide moiety are simultaneous reactivators of acetylcholinesterase and butyrylcholinesterase inhibited by nerve agent surrogates [PDF]
Journal of Enzyme Inhibition and Medicinal Chemistry, 2021 The pyridinium-2-carbaldoximes with quinolinium carboxamide moiety were designed and synthesised as cholinesterase reactivators. The prepared compounds showed intermediate-to-high inhibition of both cholinesterases when compared to standard oximes. Their
Hyun Myung Lee +13 more
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A rapid in vitro assay for evaluating the effects of acetylcholinesterase inhibitors and reactivators in the rat basolateral amygdala [PDF]
Frontiers in Cellular Neuroscience, 2022 We established a novel brain slice assay to test the ability of acetylcholinesterase (AChE) reactivators to prevent ACh-induced M1 muscarinic acetylcholine receptor (mAChR) dependent hyperexcitability observed after exposure to the organophosphate (OP ...
Jeffrey S. Thinschmidt +4 more
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Rezatapopt: A promising small-molecule “refolder” specific for TP53Y220C mutant tumors [PDF]
Neoplasia: An International Journal for Oncology ResearchInactivation of p53 due to mutation is observed in approximately half of all human cancer cases, therefore, restoration of the tumor suppressor function of oncogenic p53 mutants represents an attractive and rational therapeutic approach.
Kostas A. Papavassiliou +2 more
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Deep learning untangles the resistance mechanism of p53 reactivator in lung cancer cells [PDF]
iScience, 2023 Summary: Tumor suppressor p53 plays a pivotal role in suppressing cancer, so various drugs has been suggested to upregulate its function. However, drug resistance is still the biggest hurdle to be overcome.
Soo Min Lee +2 more
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Reactivation of Human Acetylcholinesterase and Butyrylcholinesterase Inhibited by Leptophos-Oxon with Different Oxime Reactivators in Vitro [PDF]
, 2010 We have evaluated in vitro the potency of 23 oximes to reactivate human erythrocyte acetylcholinesterase (AChE) and plasma butyrylcholinesterase (BChE) inhibited by racemic leptophos-oxon (O-[4-bromo-2,5-dichlorophenyl]-O-methyl phenyl-phosphonate), a ...
Bajgar +20 more
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In-silico drug repositioning studies of Candida albicans Nitrogen permease reactivator 1 (Npr1) kinase [PDF]
Scientific ReportsNpr1 is an essential protein in C. albicans, maintains ion homeostasis and nutrient transportation at cell membrane, and regulates the activity of ammonium transporter protein Mep2.
Sanjib Das +12 more
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Tannic acid reactivates HIV-1 latency by mediating CBX4 degradation [PDF]
Journal of VirologyHIV-1 can integrate viral DNA into host cell chromosomes and establish a long-term stable latent viral reservoir, a major obstacle in curing HIV-1 infection. The reactivation of latent proviruses with latency-reversing agents (LRAs) is a prerequisite for
Cancan Chen +11 more
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Structure of HI-6*sarin-acetylcholinesterase determined by X-ray crystallography and molecular dynamics simulation: reactivator mechanism and design. [PDF]
PLoS ONE, 2009 Organophosphonates such as isopropyl metylphosphonofluoridate (sarin) are extremely toxic as they phosphonylate the catalytic serine residue of acetylcholinesterase (AChE), an enzyme essential to humans and other species.
Fredrik Ekström +5 more
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