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Select item 66156921.

Productive reorientation of a bound oxime reactivator revealed in room temperature X-ray structures of native and VX-inhibited human acetylcholinesterase

Oksana Gerlits, Xiaotian Kong, Xiaolin Cheng, Troy Wymore, Donald K. Blumenthal, Palmer Taylor, Zoran Radić, Andrey Kovalevsky

J Biol Chem. 2019 Jul 5; 294(27): 10607–10618. Published online 2019 May 28. doi: 10.1074/jbc.RA119.008725

PMCID:: PMC6615692

Article PDF–2.0M

Select item 89616092.

APR-246—The Mutant TP53 Reactivator—Increases the Effectiveness of Berberine and Modified Berberines to Inhibit the Proliferation of Pancreatic Cancer Cells

James Andrew McCubrey, Stephen L. Abrams, Linda S. Steelman, Lucio Cocco, Stefano Ratti, Alberto M. Martelli, Paolo Lombardi, Agnieszka Gizak, Przemysław Duda

Biomolecules. 2022 Feb; 12(2): 276. Published online 2022 Feb 8. doi: 10.3390/biom12020276

PMCID:: PMC8961609

Article PDF–3.6M

Select item 83249133.

Development of a CNS-permeable reactivator for nerve agent exposure: an iterative, multi-disciplinary approach

Brian J. Bennion, Michael A. Malfatti, Nicholas A. Be, Heather A. Enright, Saphon Hok, C. Linn Cadieux, Timothy S. Carpenter, Victoria Lao, Edward A. Kuhn, M. Windy McNerney, Felice C. Lightstone, Tuan H. Nguyen, Carlos A. Valdez

Sci Rep. 2021; 11: 15567. Published online 2021 Jul 30. doi: 10.1038/s41598-021-94963-2

PMCID:: PMC8324913

Article PDF–2.7M

Select item 61491094.

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

Kamil Kuca, Kamil Musilek, Martin Paar, Daniel Jun, Petr Stodulka, Martina Hrabinova, Jan Marek

Molecules. 2007 Aug; 12(8): 1964–1972. Published online 2007 Aug 20. doi: 10.3390/12081964

PMCID:: PMC6149109

Article PDF–64K

Select item 58225995.

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

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

BMC Pharmacol Toxicol. 2018; 19: 8. Published online 2018 Feb 21. doi: 10.1186/s40360-018-0196-3

PMCID:: PMC5822599

Article PDF–1.1M

Select item 73556336.

Efficacy Assessment of an Uncharged Reactivator of NOP-Inhibited Acetylcholinesterase Based on Tetrahydroacridine Pyridine-Aldoxime Hybrid in Mouse Compared to Pralidoxime

André-Guilhem Calas, Anne-Sophie Hanak, Nina Jaffré, Aurélie Nervo, José Dias, Catherine Rousseau, Charlotte Courageux, Xavier Brazzolotto, Pascal Villa, Adeline Obrecht, Jean-François Goossens, Christophe Landry, Johan Hachani, Fabien Gosselet, Marie-Pierre Dehouck, Jagadeesh Yerri, Maria Kliachyna, Rachid Baati, Florian Nachon

Biomolecules. 2020 Jun; 10(6): 858. Published online 2020 Jun 4. doi: 10.3390/biom10060858

PMCID:: PMC7355633

Article PDF–4.3M

Select item 61491697.

Two Step Synthesis of a Non-symmetric Acetylcholinesterase Reactivator

Kamil Musilek, Kamil Kuca, Vlastimil Dohnal, Daniel Jun, Jan Marek, Vit Koleckar

Molecules. 2007 Aug; 12(8): 1755–1761. Published online 2007 Aug 7. doi: 10.3390/12081755

PMCID:: PMC6149169

Article PDF–58K

Select item 65119458.

Synthesis and Molecular Properties of Nerve Agent Reactivator HLö-7 Dimethanesulfonate

Fu-Lian Hsu, Su Y. Bae, Jack McGuire, Dana R Anderson, Stephanie M. Bester, Jude J. Height, Scott D. Pegan, Andrew J. Walz

ACS Med Chem Lett. 2019 May 9; 10(5): 761–766. Published online 2019 Mar 28. doi: 10.1021/acsmedchemlett.9b00021

PMCID:: PMC6511945

Article PDF–1.2M

Select item 26939269.

Structure of HI-6•Sarin-Acetylcholinesterase Determined by X-Ray Crystallography and Molecular Dynamics Simulation: Reactivator Mechanism and Design

Fredrik Ekström, Andreas Hörnberg, Elisabet Artursson, Lars-Gunnar Hammarström, Gunter Schneider, Yuan-Ping Pang

PLoS One. 2009; 4(6): e5957. Published online 2009 Jun 18. doi: 10.1371/journal.pone.0005957

PMCID:: PMC2693926

Article PDF–1.5M

Select item 972134410.

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

Jeffrey S. Thinschmidt, Scott W. Harden, Michael A. King, James D. Talton, Charles J. Frazier

Front Cell Neurosci. 2022; 16: 1066312. Published online 2022 Nov 21. doi: 10.3389/fncel.2022.1066312

PMCID:: PMC9721344

Article PDF–935K

Select item 710531811.

Rational design, synthesis, and evaluation of uncharged, “smart” bis-oxime antidotes of organophosphate-inhibited human acetylcholinesterase

Lukas Gorecki, Oksana Gerlits, Xiaotian Kong, Xiaolin Cheng, Donald K. Blumenthal, Palmer Taylor, Carlo Ballatore, Andrey Kovalevsky, Zoran Radić

J Biol Chem. 2020 Mar 27; 295(13): 4079–4092. Published online 2020 Feb 4. doi: 10.1074/jbc.RA119.012400

Correction in:: J Biol Chem. 2020 May 8; 295(19): 6784.

PMCID:: PMC7105318

Article PDF–4.6M

Select item 627841712.

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

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

Molecules. 2018 Nov; 23(11): 2954. Published online 2018 Nov 12. doi: 10.3390/molecules23112954

PMCID:: PMC6278417

Article PDF–4.6M

Select item 890975613.

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

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

Cells. 2022 Mar; 11(5): 794. Published online 2022 Feb 24. doi: 10.3390/cells11050794

PMCID:: PMC8909756

Article PDF–2.9M

Select item 940088914.

Broad‐Spectrum Antidote Discovery by Untangling the Reactivation Mechanism of Nerve‐Agent‐Inhibited Acetylcholinesterase

Dr. Cecilia Lindgren, Dr. Nina Forsgren, Norman Hoster, Christine Akfur, Elisabet Artursson, Dr. Lotta Edvinsson, Dr. Richard Svensson, Dr. Franz Worek, Dr. Fredrik Ekström, Prof. Anna Linusson

Chemistry. 2022 Jul 15; 28(40): e202200678. Published online 2022 Jun 7. doi: 10.1002/chem.202200678

PMCID:: PMC9400889

Article PDF–1.8M

Select item 581056015.

The biodistribution and pharmacokinetics of the oxime acetylcholinesterase reactivator RS194B in guinea pigs

Michael A. Malfatti, Heather A. Enright, Nicholas A. Be, Edward A. Kuhn, Saphon Hok, M. Windy McNerney, Victoria Lao, Tuan H. Nguyen, Felice C. Lightstone, Timothy S. Carpenter, Brian J. Bennion, Carlos A. Valdez

Chem Biol Interact. Author manuscript; available in PMC 2018 Feb 13.

Published in final edited form as: Chem Biol Interact. 2017 Nov 1; 277: 159–167. Published online 2017 Sep 21. doi: 10.1016/j.cbi.2017.09.016

PMCID:: PMC5810560

Article PDF–1.1M

Select item 310332116.

New Structural Scaffolds for Centrally Acting Oxime Reactivators of Phosphylated Cholinesterases

Rakesh K. Sit, Zoran Radić, Valeria Gerardi, Limin Zhang, Edzna Garcia, Maja Katalinić, Gabriel Amitai, Zrinka Kovarik, Valery V. Fokin, K. Barry Sharpless, Palmer Taylor

J Biol Chem. 2011 Jun 3; 286(22): 19422–19430. Published online 2011 Apr 4. doi: 10.1074/jbc.M111.230656

PMCID:: PMC3103321

Article PDF–2.4M

Select item 467004017.

Small molecule reactivation of mutant p53 to wt-like p53 through the p53-Hsp40 regulatory axis

Masatsugu Hiraki, So-Young Hwang, Shugeng Cao, Timothy R. Ramadhar, Sanguine Byun, Kyoung Wan Yoon, Jung Hyun Lee, Kiki Chu, Aditi U. Gurkar, Vihren Kolev, Jianming Zhang, Takushi Namba, Maureen E. Murphy, David J. Newman, Anna Mandinova, Jon Clardy, Sam W. Lee

Chem Biol. Author manuscript; available in PMC 2016 Sep 17.

Published in final edited form as: Chem Biol. 2015 Sep 17; 22(9): 1206–1216. Published online 2015 Aug 27. doi: 10.1016/j.chembiol.2015.07.016