Crystallographic fragment screening and structure-based optimization yields a new class of influenza endonuclease inhibitors

JD Bauman, D Patel, SF Baker, RSK Vijayan… - ACS chemical …, 2013 - ACS Publications
Seasonal and pandemic influenza viruses continue to be a leading global health concern.
Emerging resistance to the current drugs and the variable efficacy of vaccines underscore …

Computation-guided discovery of influenza endonuclease inhibitors

E Chen, RV Swift, N Alderson, VA Feher… - ACS medicinal …, 2014 - ACS Publications
Influenza is a global human health threat, and there is an immediate need for new antiviral
therapies to circumvent the limitations of vaccination and current small molecule therapies …

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 …

Protein-structure assisted optimization of 4, 5-dihydroxypyrimidine-6-carboxamide inhibitors of influenza virus endonuclease

D Beylkin, G Kumar, W Zhou, J Park, T Jeevan… - Scientific reports, 2017 - nature.com
Influenza is a serious hazard to human health that causes hundreds of thousands of deaths
annually. Though vaccines and current therapeutics can blunt some of the perilous impact of …

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 …

Phenyl substituted 3-hydroxypyridin-2 (1H)-ones: inhibitors of influenza A endonuclease

AK Parhi, A Xiang, JD Bauman, D Patel… - Bioorganic & medicinal …, 2013 - Elsevier
Inhibition of the endonuclease activity of influenza RNA-dependent RNA polymerase is
recognized as an attractive target for the development of new agents for the treatment of …

SAR exploration of tight-binding inhibitors of influenza virus PA endonuclease

CV Credille, CN Morrison, RW Stokes… - Journal of medicinal …, 2019 - ACS Publications
Significant efforts have been reported on the development of influenza antivirals including
inhibitors of the RNA-dependent RNA polymerase PA N-terminal (PAN) endonuclease …

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 …

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 …

Inhibitors of influenza A virus polymerase

S Yuan, L Wen, J Zhou - ACS Infectious Diseases, 2018 - ACS Publications
The propensity of influenza virus to develop resistance to commonly prescribed drugs
highlights the need for continuing development of new therapeutics. Biological and …