Results 11 to 20 of about 1,554 (191)

Targeted Synthesis of 1-(4-Hydroxyiminomethylpyridinium)-3-pyridiniumpropane Dibromide – A New Nerve Agent Reactivator

Molecules, 2007
Preparation of 1-(4-hydroxy-iminomethylpyridinium)-3-pyridiniumpropane dibromide is described. This compound represents a new acetylcholinesterase (AChE) reactivator, which has no substituents on the second pyridinium ring as found in other commonly used
Jan Marek, Martina Hrabinova, Petr Stodulka, Daniel Jun, Martin Paar, Kamil Musilek, Kamil Kuca   +6 more
doaj   +2 more sources

Effects of the Mutant TP53 Reactivator APR-246 on Therapeutic Sensitivity of Pancreatic Cancer Cells in the Presence and Absence of WT-TP53 [PDF]

Cells, 2022
The TP53 tumor suppressor is mutated in ~75% of pancreatic cancers. The mutant TP53 protein in pancreatic ductal adenocarcinomas (PDAC) promotes tumor growth and metastasis.
Stephen L. Abrams, Przemysław Duda, Shaw M. Akula, Linda S. Steelman, Matilde L. Follo, Lucio Cocco, Stefano Ratti, Alberto M. Martelli, Giuseppe Montalto, Maria Rita Emma, Melchiorre Cervello, Dariusz Rakus, Agnieszka Gizak, James A. McCubrey   +13 more
doaj   +3 more sources

A newly developed oxime K203 is the most effective reactivator of tabun-inhibited acetylcholinesterase

BMC Pharmacology and 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, Jana Zdarova-Karasova, Eugenie Nepovimova, Ondrej Soukup, Martina Hrabinova, John Mikler, Tanos C. C. Franca, Elaine F. F. Da Cunha, Alexandre A. De Castro, Martin Valis, Teodorico C. Ramalho   +12 more
doaj   +2 more sources

Molecular Modeling and In Vitro Studies of a Neutral Oxime as a Potential Reactivator for Acetylcholinesterase Inhibited by Paraoxon

Molecules, 2018
The present work aimed to compare the small, neutral and monoaromatic oxime, isatin-3-oxime (isatin-O), to the commercial ones, pralidoxime (2-PAM) and obidoxime, in a search for a new potential reactivator for acetylcholinesterase (AChE) inhibited by ...
Reuel L. de Paula, Joyce S. F. D. de Almeida, Samir F. A. Cavalcante, Arlan S. Gonçalves, Alessandro B. C. Simas, Tanos C. C. Franca, Martin Valis, Kamil Kuca, Eugenie Nepovimova, José M. Granjeiro   +9 more
doaj   +2 more sources

Optimal Choice of Acetylcholinesterase Reactivators for Antidoral Treatment of Nerve Agent Intoxication

Acta Medica, 2010
The studies dealing with mechanism of organophosphates (OP)/nerve agent action, prophylaxis and treatment of intoxications is a very hot topic at present.
Jiří Bajgar
doaj   +2 more sources

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, Andreas Hörnberg, Elisabet Artursson, Lars-Gunnar Hammarström, Gunter Schneider, Yuan-Ping Pang   +5 more
doaj   +2 more sources

A rapid in vitro assay for evaluating the effects of acetylcholinesterase inhibitors and reactivators in the rat basolateral amygdala

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, Scott W. Harden, Michael A. King, James D. Talton, Charles J. Frazier   +4 more
doaj   +1 more source

AI-powered discovery of a novel p53-Y220C reactivator

Frontiers in Oncology, 2023
IntroductionThe p53-Y220C mutation is one of the most common mutations that play a major role in cancer progression.MethodsIn this study, we applied artificial intelligence (AI)-powered virtual screening to identify small-molecule compounds that ...
Shan Zhou, Dafei Chai, Xu Wang, Praveen Neeli, Xinfang Yu, Aram Davtyan, Ken Young, Yong Li   +7 more
doaj   +1 more source

Discovery of Rezatapopt (PC14586), a First-in-Class, Small-Molecule Reactivator of p53 Y220C Mutant in Development [PDF]

ACS Medicinal Chemistry Letters
David C Fry
exaly   +2 more sources

A Reactivator of Organophosphorus Nerve Agent-Inhibited Human Acetylcholinesterase: Characterization, Mechanistic Insights and Design

, 2022
Koh, John T.Organophosphorus nerve agents are highly toxic compounds which pose a threat worldwide. These compounds induce toxicity by covalently binding to the active site serine of acetylcholinesterase, which results in inhibition of the enzyme ...
Cadieux, C. Linn
core   +1 more source