[HTML][HTML] Structural and biochemical basis for development of influenza virus inhibitors targeting the PA endonuclease

RM DuBois, PJ Slavish, BM Baughman, MK Yun… - PLoS …, 2012 - journals.plos.org
Emerging influenza viruses are a serious threat to human health because of their pandemic
potential. A promising target for the development of novel anti-influenza therapeutics is the …

Influenza A virus polymerase: an attractive target for next-generation anti-influenza therapeutics

Z Zhou, T Liu, J Zhang, P Zhan, X Liu - Drug Discovery Today, 2018 - Elsevier
Highlights•The structures of influenza polymerase allow the identification of novel anti-
influenza drugs.•The inhibitors targeting influenza polymerase are discussed.•The screening …

[HTML][HTML] A novel small-molecule inhibitor of influenza A virus acts by suppressing PA endonuclease activity of the viral polymerase

S Yuan, H Chu, K Singh, H Zhao, K Zhang, RYT Kao… - Scientific reports, 2016 - nature.com
The RNA-dependent RNA polymerase of influenza A virus comprises conserved and
independently-folded subdomains with defined functionalities. The N-terminal domain of the …

Mutational analysis of the binding pockets of the diketo acid inhibitor L-742,001 in the influenza virus PA endonuclease

A Stevaert, R Dallocchio, A Dessì, N Pala… - Journal of …, 2013 - Am Soc Microbiol
The influenza virus PA endonuclease, which cleaves capped host pre-mRNAs to initiate
synthesis of viral mRNA, is a prime target for antiviral therapy. The diketo acid compound L …

Fragment-based identification of influenza endonuclease inhibitors

CV Credille, Y Chen, SM Cohen - Journal of medicinal chemistry, 2016 - ACS Publications
The influenza virus is responsible for millions of cases of severe illness annually. Yearly
variance in the effectiveness of vaccination, coupled with emerging drug resistance …

Virtual screening and biological validation of novel influenza virus PA endonuclease inhibitors

N Pala, A Stevaert, R Dallocchio, A Dessì… - ACS Medicinal …, 2015 - ACS Publications
The influenza virus RNA-dependent RNA polymerase complex (RdRp), a heterotrimeric
protein complex responsible for viral RNA transcription and replication, represents a primary …

A Novel Endonuclease Inhibitor Exhibits Broad-Spectrum Anti-Influenza Virus Activity In Vitro

JC Jones, BM Marathe, C Lerner, L Kreis… - Antimicrobial agents …, 2016 - Am Soc Microbiol
Antiviral drugs are important in preventing and controlling influenza, particularly when
vaccines are ineffective or unavailable. A single class of antiviral drugs, the neuraminidase …

[HTML][HTML] Endonuclease substrate selectivity characterized with full-length PA of influenza A virus polymerase

E Noble, A Cox, J Deval, B Kim - Virology, 2012 - Elsevier
The influenza A polymerase is a heterotrimer which transcribes viral mRNAs and replicates
the viral genome. To initiate synthesis of mRNA, the polymerase binds a host pre-mRNA and …

Inhibitors of influenza virus polymerase acidic (PA) endonuclease: contemporary developments and perspectives

H Ju, J Zhang, B Huang, D Kang, B Huang… - Journal of Medicinal …, 2017 - ACS Publications
Influenza virus (IFV) causes periodic global influenza pandemics, resulting in substantial
socioeconomic loss and burden on medical facilities. Yearly variation in the effectiveness of …

[HTML][HTML] Structural analysis of specific metal chelating inhibitor binding to the endonuclease domain of influenza pH1N1 (2009) polymerase

E Kowalinski, C Zubieta, A Wolkerstorfer… - PLoS …, 2012 - journals.plos.org
It is generally recognised that novel antiviral drugs, less prone to resistance, would be a
desirable alternative to current drug options in order to be able to treat potentially serious …