| dc.rights.license | CC BY | eng |
| dc.contributor.author | Valle da Silva, Jorge Alberto | cze |
| dc.contributor.author | Pereira, Ander Francisco | cze |
| dc.contributor.author | LaPlante, Steven R | cze |
| dc.contributor.author | Kuča, Kamil | cze |
| dc.contributor.author | Ramalho, Teodorico Castro | cze |
| dc.contributor.author | Costa Franca, Tanos Celmar | cze |
| dc.date.accessioned | 2025-12-05T08:42:19Z | |
| dc.date.available | 2025-12-05T08:42:19Z | |
| dc.date.issued | 2020 | eng |
| dc.identifier.issn | 2218-273X | eng |
| dc.identifier.uri | http://hdl.handle.net/20.500.12603/980 | |
| dc.description.abstract | In the present work, we performed a complementary quantum mechanical (QM) study to describe the mechanism by which deprotonated pralidoxime (2-PAM) could reactivate human (Homo sapiens sapiens) acetylcholinesterase (HssAChE) inhibited by the nerve agent VX. Such a reaction is proposed to occur in subsequent addition-elimination steps, starting with a nucleophile bimolecular substitution (S(N)2) mechanism through the formation of a trigonal bipyramidal transition state (TS). A near attack conformation (NAC), obtained in a former study using molecular mechanics (MM) calculations, was taken as a starting point for this project, where we described the possible formation of the TS. Together, this combined QM/MM study on AChE reactivation shows the feasibility of the reactivation occurring via attack of the deprotonated form of 2-PAM against the Ser203-VX adduct of HssAChE. | eng |
| dc.format | p. "Article Number: 192" | eng |
| dc.language.iso | eng | eng |
| dc.publisher | MDPI | eng |
| dc.relation.ispartof | BIOMOLECULES, volume 10, issue: 2 | eng |
| dc.subject | acetylcholinesterase | eng |
| dc.subject | VX | eng |
| dc.subject | 2-PAM | eng |
| dc.subject | QM | eng |
| dc.subject | MM method | eng |
| dc.subject | acetylcholinesteráza | cze |
| dc.subject | VX | cze |
| dc.subject | 2-PAM | cze |
| dc.subject | QM | cze |
| dc.subject | MM metoda | cze |
| dc.title | Reactivation of VX-Inhibited Human Acetylcholinesterase by Deprotonated Pralidoxime. A Complementary Quantum Mechanical Study | eng |
| dc.title.alternative | Reaktivace VX-inhibované lidské acetylcholinesterázy deprotonovaným pralidoximem. Doplňková kvantová mechanická studie | cze |
| dc.type | article | eng |
| dc.identifier.obd | 43876289 | eng |
| dc.identifier.wos | 000522138500170 | eng |
| dc.identifier.doi | 10.3390/biom10020192 | eng |
| dc.description.abstract-translated | této práci jsme provedli komplementární kvantovou mechanickou (QM) studii, která popisuje mechanismus, kterým by deprotonovaný pralidoxim (2-PAM) mohl reaktivovat lidskou (Homo sapiens sapiens) acetylcholinesterázu (HssAChE) inhibovanou nervovým činidlem VX. Navrhuje se, aby k takové reakci došlo v následných krocích eliminace, počínaje mechanismem nukleofilní bimolekulární substituce (S (N) 2) vytvořením trigonálního bipyramidálního přechodného stavu (TS). Výchozím bodem tohoto projektu byla konformace blízkého útoku (NAC), získaná v dřívější studii pomocí výpočtů molekulární mechaniky (MM), kde jsme popsali možnou tvorbu TS. Tato kombinovaná studie QM / MM o reaktivaci AChE společně ukazuje proveditelnost reaktivace, ke které dochází prostřednictvím útoku deprotonované formy 2-PAM proti aduktu HssAChE Ser203-VX. | cze |
| dc.publicationstatus | postprint | eng |
| dc.peerreviewed | yes | eng |
| dc.source.url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7072650/ | cze |
| dc.relation.publisherversion | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7072650/ | eng |
| dc.rights.access | Open Access | eng |