{"title":"[甲型流感和SARS-CoV-2病毒的分子离子通道阻滞剂]。","authors":"Yu N Vorobjev","doi":"10.31857/S0026898424040125, EDN: IMBPHX","DOIUrl":null,"url":null,"abstract":"<p><p>Molecules were proposed to block the functional cycles of the influenza virus A and SARS-CoV- 2. The blocker molecules efficiently bind inside the M2 and E channels of influenza A and SARS-CoV-2 viruses and block diffusion of H^(+)/K^(+) ions, thus distorting the virus functional cycle. A family of positively charged (+2 e.u.) molecular blockers of H^(+)/K^(+) ion diffusion through the M2 and E channels was proposed. The blocker molecules were diazabicyclooctane (DABCO) derivatives and were investigated for affinity for the M2 and E channels. Thermal dynamics of native and mutant channel structures and blocker binding were modeled by exhaustive docking. Binding energy calculations revealed within-channel, blocking, and extrachannel binding sites in the M2 and E channel proteins. Blocker molecules with higher affinity for the blocking sites were proposed. The most probable amino acid mutations the M2 and E channels were considered, the efficiency of channel blocking was analyzed, and optimal structures were assumed for the blocker molecules.</p>","PeriodicalId":39818,"journal":{"name":"Molekulyarnaya Biologiya","volume":"58 4","pages":"665-680"},"PeriodicalIF":0.0000,"publicationDate":"2024-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"[Molecular Ion Channel Blockers of Influenza A and SARS-CoV-2 Viruses].\",\"authors\":\"Yu N Vorobjev\",\"doi\":\"10.31857/S0026898424040125, EDN: IMBPHX\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Molecules were proposed to block the functional cycles of the influenza virus A and SARS-CoV- 2. The blocker molecules efficiently bind inside the M2 and E channels of influenza A and SARS-CoV-2 viruses and block diffusion of H^(+)/K^(+) ions, thus distorting the virus functional cycle. A family of positively charged (+2 e.u.) molecular blockers of H^(+)/K^(+) ion diffusion through the M2 and E channels was proposed. The blocker molecules were diazabicyclooctane (DABCO) derivatives and were investigated for affinity for the M2 and E channels. Thermal dynamics of native and mutant channel structures and blocker binding were modeled by exhaustive docking. Binding energy calculations revealed within-channel, blocking, and extrachannel binding sites in the M2 and E channel proteins. Blocker molecules with higher affinity for the blocking sites were proposed. The most probable amino acid mutations the M2 and E channels were considered, the efficiency of channel blocking was analyzed, and optimal structures were assumed for the blocker molecules.</p>\",\"PeriodicalId\":39818,\"journal\":{\"name\":\"Molekulyarnaya Biologiya\",\"volume\":\"58 4\",\"pages\":\"665-680\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2024-07-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Molekulyarnaya Biologiya\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.31857/S0026898424040125, EDN: IMBPHX\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"Medicine\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Molekulyarnaya Biologiya","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.31857/S0026898424040125, EDN: IMBPHX","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"Medicine","Score":null,"Total":0}
[Molecular Ion Channel Blockers of Influenza A and SARS-CoV-2 Viruses].
Molecules were proposed to block the functional cycles of the influenza virus A and SARS-CoV- 2. The blocker molecules efficiently bind inside the M2 and E channels of influenza A and SARS-CoV-2 viruses and block diffusion of H^(+)/K^(+) ions, thus distorting the virus functional cycle. A family of positively charged (+2 e.u.) molecular blockers of H^(+)/K^(+) ion diffusion through the M2 and E channels was proposed. The blocker molecules were diazabicyclooctane (DABCO) derivatives and were investigated for affinity for the M2 and E channels. Thermal dynamics of native and mutant channel structures and blocker binding were modeled by exhaustive docking. Binding energy calculations revealed within-channel, blocking, and extrachannel binding sites in the M2 and E channel proteins. Blocker molecules with higher affinity for the blocking sites were proposed. The most probable amino acid mutations the M2 and E channels were considered, the efficiency of channel blocking was analyzed, and optimal structures were assumed for the blocker molecules.