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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BMC Pharmacology & Toxicology, 2018 Background Based on in vitro and in vivo rat experiments, the newly developed acetylcholinesterase (AChE) reactivator, K203, appears to be much more effective in the treatment of tabun poisonings than currently fielded oximes.
Kamil Kuca, Kamil Musilek, Daniel Jun
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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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Two Step Synthesis of a Non-symmetric Acetylcholinesterase Reactivator
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 ...
Kamil Musilek +2 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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PK11007 Covalently Inhibits Thioredoxin Reductase 1 to Induce Oxidative Stress and Autophagy Impairment in NSCLC Cells [PDF]
AntioxidantsSelenoprotein thioredoxin reductase 1 (TXNRD1) is frequently upregulated in various cancer cells to sustain cellular redox homeostasis, and its inhibition has emerged as a promising anti-cancer strategy.
Hanziyi Zhou +10 more
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Cholesterol Oxime Olesoxime Assessed as a Potential Ligand of Human Cholinesterases [PDF]
BiomoleculesOlesoxime, a cholesterol derivative with an oxime group, possesses the ability to cross the blood–brain barrier, and has demonstrated excellent safety and tolerability properties in clinical research.
Dora Kolić +6 more
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