Attenuation of SARS‐CoV‐2 replication and associated inflammation by concomitant targeting of viral and host cap 2'‐O‐ribose methyltransferases

V Bergant, S Yamada, V Grass, Y Tsukamoto… - The EMBO …, 2022 - embopress.org
The SARS‐CoV‐2 infection cycle is a multistage process that relies on functional
interactions between the host and the pathogen. Here, we repurposed antiviral drugs …

Bisubstrate inhibitors of severe acute respiratory syndrome coronavirus-2 nsp14 methyltransferase

E Jung, R Soto-Acosta, J Xie, DJ Wilson… - ACS Medicinal …, 2022 - ACS Publications
Taking advantage of the uniquely constricted active site of SARS-CoV-2 Nsp14
methyltransferase, we have designed bisubstrate inhibitors interacting with the SAM and …

[HTML][HTML] Potential Drugs Targeting Early Innate Immune Evasion of SARS-Coronavirus 2 via 2'-O-Methylation of Viral RNA

JA Encinar, JA Menendez - Viruses, 2020 - mdpi.com
The severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) causing the COVID-19
respiratory disease pandemic utilizes unique 2′-o-methyltransferase (2′-O-MTase) …

High-resolution structures of the SARS-CoV-2 2′-O-methyltransferase reveal strategies for structure-based inhibitor design

M Rosas-Lemus, G Minasov, L Shuvalova, NL Inniss… - Science …, 2020 - science.org
There are currently no antiviral therapies specific for SARS-CoV-2, the virus responsible for
the global pandemic disease COVID-19. To facilitate structure-based drug design, we …

Identifying SARS-CoV-2 antiviral compounds by screening for small molecule inhibitors of Nsp14 RNA cap methyltransferase

S Basu, T Mak, R Ulferts, M Wu, T Deegan… - Biochemical …, 2021 - portlandpress.com
The COVID-19 pandemic has presented itself as one of the most critical public health
challenges of the century, with SARS-CoV-2 being the third member of the Coronaviridae …

SARS-CoV-2 uses nonstructural protein 16 to evade restriction by IFIT1 and IFIT3

C Schindewolf, K Lokugamage, MN Vu… - Journal of …, 2023 - Am Soc Microbiol
Understanding the molecular basis of innate immune evasion by severe acute respiratory
syndrome coronavirus 2 (SARS-CoV-2) is an important consideration for designing the next …

Structure-guided optimization of adenosine mimetics as selective and potent inhibitors of coronavirus nsp14 N7-methyltransferases

M Hausdorff, A Delpal, S Barelier, L Nicollet… - European Journal of …, 2023 - Elsevier
The COVID-19 pandemic reveals the urgent need to develop new therapeutics targeting the
SARS-CoV-2 replication machinery. The first antiviral drugs were nucleoside analogues …

[HTML][HTML] Discovery of SARS-CoV-2 Nsp14 and Nsp16 methyltransferase inhibitors by high-throughput virtual screening

R Bobrovs, I Kanepe, N Narvaiss, L Patetko, G Kalnins… - Pharmaceuticals, 2021 - mdpi.com
The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) uses mRNA capping to
evade the human immune system. The cap formation is performed by the SARS-CoV-2 …

Nsp16 shields SARS–CoV‐2 from efficient MDA5 sensing and IFIT1‐mediated restriction

A Russ, S Wittmann, Y Tsukamoto, A Herrmann… - EMBO …, 2022 - embopress.org
Methylation of the mRNA 5′ cap by cellular methyltransferases enables efficient translation
and avoids recognition by innate immune factors. Coronaviruses encode viral 2′‐O …

A universal fluorescence polarization high throughput screening assay to target the SAM-binding sites of SARS-CoV-2 and other viral methyltransferases

SK Samrat, Q Bashir, R Zhang, Y Huang… - Emerging Microbes & …, 2023 - Taylor & Francis
ABSTRACT SARS-CoV-2 has caused a global pandemic with significant humanity and
economic loss since 2020. Currently, only limited options are available to treat SARS-CoV-2 …