[HTML][HTML] Remdesivir, Molnupiravir and Nirmatrelvir remain active against SARS-CoV-2 Omicron and other variants of concern

…, B Slechten, J Raymenants, E André, P Leyssen… - Antiviral research, 2022 - Elsevier
We assessed the in vitro antiviral activity of remdesivir and its parent nucleoside GS-441524,
molnupiravir and its parent nucleoside EIDD-1931 and the viral protease inhibitor …

α-Ketoamides as broad-spectrum inhibitors of coronavirus and enterovirus replication: structure-based design, synthesis, and activity assessment

…, Q Ma, J Wang, A Von Brunn, P Leyssen… - Journal of medicinal …, 2020 - ACS Publications
The main protease of coronaviruses and the 3C protease of enteroviruses share a similar
active-site architecture and a unique requirement for glutamine in the P1 position of the …

[HTML][HTML] STAT2 signaling restricts viral dissemination but drives severe pneumonia in SARS-CoV-2 infected hamsters

…, L Coelmont, W Chiu, P Leyssen… - Nature …, 2020 - nature.com
Emergence of SARS-CoV-2 causing COVID-19 has resulted in hundreds of thousands of
deaths. In search for key targets of effective therapeutics, robust animal models mimicking …

Bioactivity-based molecular networking for the discovery of drug leads in natural product bioassay-guided fractionation

…, Z Zhang, A Sarvepalli, P Leyssen… - Journal of natural …, 2018 - ACS Publications
It is a common problem in natural product therapeutic lead discovery programs that despite
good bioassay results in the initial extract, the active compound(s) may not be isolated during …

The predominant mechanism by which ribavirin exerts its antiviral activity in vitro against flaviviruses and paramyxoviruses is mediated by inhibition of IMP …

P Leyssen, J Balzarini, E De Clercq, J Neyts - Journal of virology, 2005 - Am Soc Microbiol
It is not yet clear to what extent depletion of intracellular GTP pools contributes to the antiviral
activity of ribavirin. Therefore, the antiviral activities of (i) ribavirin, (ii) its 5-ethynyl analogue…

Perspectives for the Treatment of Infections withFlaviviridae

P Leyssen, E De Clercq, J Neyts - Clinical microbiology reviews, 2000 - Am Soc Microbiol
The family Flaviviridae contains three genera: Hepacivirus, Flavivirus, and Pestivirus. Worldwide,
more than 170 million people are chronically infected with Hepatitis C virus and are at …

Mutations in the chikungunya virus non-structural proteins cause resistance to favipiravir (T-705), a broad-spectrum antiviral

…, J Neyts, MJ van Hemert, P Leyssen - Journal of …, 2014 - academic.oup.com
Objectives T-705, also known as favipiravir, is a small-molecule inhibitor that is currently in
clinical development for the treatment of influenza virus infections. This molecule also inhibits …

[PDF][PDF] Itraconazole inhibits enterovirus replication by targeting the oxysterol-binding protein

…, L Albulescu, J Bigay, M Arita, L Delang, P Leyssen… - Cell reports, 2015 - cell.com
Itraconazole (ITZ) is a well-known antifungal agent that also has anticancer activity. In this
study, we identify ITZ as a broad-spectrum inhibitor of enteroviruses (eg, poliovirus, …

[HTML][HTML] The combined treatment of Molnupiravir and Favipiravir results in a potentiation of antiviral efficacy in a SARS-CoV-2 hamster infection model

…, J Pang, R Williams, V Vergote, E Heylen, P Leyssen… - …, 2021 - thelancet.com
Background Favipiravir and Molnupiravir, orally available antivirals, have been reported to
exert antiviral activity against SARS-CoV-2. First efficacy data have been recently reported in …

Identification of inhibitors of SARS-CoV-2 3CL-pro enzymatic activity using a small molecule in vitro repurposing screen

…, E Tramontano, AR Beccari, P Leyssen… - ACS pharmacology & …, 2021 - ACS Publications
Compound repurposing is an important strategy for the identification of effective treatment
options against SARS-CoV-2 infection and COVID-19 disease. In this regard, SARS-CoV-2 …