Bioisosteres of the phenyl ring: recent strategic applications in lead optimization and drug design

MAM Subbaiah, NA Meanwell - Journal of Medicinal Chemistry, 2021 - ACS Publications
The benzene moiety is the most prevalent ring system in marketed drugs, underscoring its
historic popularity in drug design either as a pharmacophore or as a scaffold that projects …

Influenza virus RNA polymerase: insights into the mechanisms of viral RNA synthesis

AJW Te Velthuis, E Fodor - Nature Reviews Microbiology, 2016 - nature.com
The genomes of influenza viruses consist of multiple segments of single-stranded negative-
sense RNA. Each of these segments is bound by the heterotrimeric viral RNA-dependent …

Characterization of influenza virus variants induced by treatment with the endonuclease inhibitor baloxavir marboxil

S Omoto, V Speranzini, T Hashimoto, T Noshi… - Scientific reports, 2018 - nature.com
Baloxavir acid (BXA), derived from the prodrug baloxavir marboxil (BXM), potently and
selectively inhibits the cap-dependent endonuclease within the polymerase PA subunit of …

Targeting metalloenzymes for therapeutic intervention

AY Chen, RN Adamek, BL Dick, CV Credille… - Chemical …, 2018 - ACS Publications
Metalloenzymes are central to a wide range of essential biological activities, including
nucleic acid modification, protein degradation, and many others. The role of metalloenzymes …

Structure of influenza A polymerase bound to the viral RNA promoter

A Pflug, D Guilligay, S Reich, S Cusack - Nature, 2014 - nature.com
The influenza virus polymerase transcribes or replicates the segmented RNA genome (viral
RNA) into viral messenger RNA or full-length copies. To initiate RNA synthesis, the …

Bat-derived influenza-like viruses H17N10 and H18N11

Y Wu, Y Wu, B Tefsen, Y Shi, GF Gao - Trends in microbiology, 2014 - cell.com
Shorebirds and waterfowls are believed to be the reservoir hosts for influenza viruses,
whereas swine putatively act as mixing vessels. The recent identification of two influenza …

Baloxavir marboxil: the new influenza drug on the market

R O'Hanlon, ML Shaw - Current opinion in virology, 2019 - Elsevier
Highlights•Approval of first endonuclease inhibitor for influenza treatment.•Represents a
new class of influenza drug.•Single dose is clinically effective.For the first time in nearly 20 …

Common and unique features of viral RNA-dependent polymerases

AJW Te Velthuis - Cellular and molecular life sciences, 2014 - Springer
Eukaryotes and bacteria can be infected with a wide variety of RNA viruses. On average,
these pathogens share little sequence similarity and use different replication and …

[HTML][HTML] Structural insights into RNA synthesis by the influenza virus transcription-replication machine

A Pflug, M Lukarska, P Resa-Infante, S Reich… - Virus research, 2017 - Elsevier
Influenza virus is a segmented, negative strand RNA virus with each genome segment being
packaged in a distinct ribonucleoprotein particle (RNP). The RNP consists of the …

The influenza virus polymerase complex: an update on its structure, functions, and significance for antiviral drug design

A Stevaert, L Naesens - Medicinal research reviews, 2016 - Wiley Online Library
Influenza viruses cause seasonal epidemics and pandemic outbreaks associated with
significant morbidity and mortality, and a huge cost. Since resistance to the existing anti …