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 …

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 …

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 …

An integrated biological approach to guide the development of metal-chelating inhibitors of influenza virus PA endonuclease

A Stevaert, S Nurra, N Pala, M Carcelli, D Rogolino… - Molecular …, 2015 - ASPET
The influenza virus PA endonuclease, which cleaves capped cellular pre-mRNAs to prime
viral mRNA synthesis, is a promising target for novel anti–influenza virus therapeutics. The …

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 …

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 …

Discovery and optimization of new 6, 7-dihydroxy-1, 2, 3, 4-tetrahydroisoquinoline derivatives as potent influenza virus PAN inhibitors

Z Liu, S Gu, X Zhu, M Liu, Z Cao, P Qiu, S Li… - European Journal of …, 2022 - Elsevier
Annual unpredictable efficacy of vaccines, coupled with emerging drug resistance,
underlines the development of new antiviral drugs to treat influenza infections. The N …

N-acylhydrazone inhibitors of influenza virus PA endonuclease with versatile metal binding modes

M Carcelli, D Rogolino, A Gatti, L De Luca, M Sechi… - Scientific reports, 2016 - nature.com
Influenza virus PA endonuclease has recently emerged as an attractive target for the
development of novel antiviral therapeutics. This is an enzyme with divalent metal ion …

Identification of the I38T PA substitution as a resistance marker for next-generation influenza virus endonuclease inhibitors

JC Jones, G Kumar, S Barman, I Najera, SW White… - MBio, 2018 - Am Soc Microbiol
The clinical severity and annual occurrence of influenza virus epidemics, combined with the
availability of just a single class of antivirals to treat infections, underscores the urgent need …