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10.1016/j.bbrc.2020.04.034

http://scihub22266oqcxt.onion/10.1016/j.bbrc.2020.04.034
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32327257!7152910!32327257
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suck abstract from ncbi


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pmid32327257      Biochem+Biophys+Res+Commun 2020 ; 526 (4): 1143-1149
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  • Kinase inhibitor roscovitine as a PB2 cap-binding inhibitor against influenza a virus replication #MMPMID32327257
  • Huang Q; Zhong Y; Li J; Ye Y; Wu W; Chen L; Feng M; Yang J; Liu S
  • Biochem Biophys Res Commun 2020[Jun]; 526 (4): 1143-1149 PMID32327257show ga
  • In this study, we examined the impact of roscovitine, a cyclin-dependent kinase inhibitor (CDKI) that has entered phase I and II clinical trials, on influenza A viruses (IAVs) and its antiviral mechanism. The results illustrated that roscovitine inhibited multiple subtypes of influenza strains dose-dependently, including A/WSN/1933(H1N1), A/Aichi/2/68 (H3N2) and A/FM1/47 (H1N1) with IC(50) value of 3.35 +/- 0.39, 7.01 +/- 1.84 and 5.99 +/- 1.89 muM, respectively. Moreover, roscovitine suppressed the gene transcription and genome replication steps in the viral life cycle. Further mechanistic studies indicated that roscovitine reduced viral polymerase activity and bound specifically to the viral PB2cap protein by fluorescence polarization assay (FP) and surface plasmon resonance (SPR). Therefore, we believed roscovitine, as a PB2cap inhibitor, was a prospective antiviral agent to be developed as therapeutic treatment against influenza A virus infection.
  • |Animals[MESH]
  • |Antiviral Agents/*pharmacology[MESH]
  • |DNA-Directed RNA Polymerases/metabolism[MESH]
  • |Dogs[MESH]
  • |Genome, Viral[MESH]
  • |Humans[MESH]
  • |Influenza A virus/drug effects/genetics/*physiology[MESH]
  • |Madin Darby Canine Kidney Cells[MESH]
  • |Protein Kinase Inhibitors/chemistry/*pharmacology[MESH]
  • |RNA Cap-Binding Proteins/*metabolism[MESH]
  • |RNA-Dependent RNA Polymerase/*metabolism[MESH]
  • |Roscovitine/chemistry/*pharmacology[MESH]
  • |Transcription, Genetic/drug effects[MESH]
  • |Viral Proteins/*metabolism[MESH]
  • |Virus Internalization/drug effects[MESH]


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