Science (New York, N.Y.) · 2021
Plitidepsin has potent preclinical efficacy against SARS-CoV-2 by targeting the host protein eEF1A.
СтатьяПоддержка NIH: внешняя программаПоддержка исследования: вне правительства СШАНазвание и аннотация: Перевод пока не подготовлен
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White Kris M, Rosales Romel, Yildiz Soner, Kehrer Thomas, Miorin Lisa, Moreno Elena, Jangra Sonia, Uccellini Melissa B, Rathnasinghe Raveen, Coughlan Lynda, Martinez-Romero Carles, Batra Jyoti, Rojc Ajda, Bouhaddou Mehdi, Fabius Jacqueline M, Obernier Kirsten, Dejosez Marion, Guillén María José, Losada Alejandro, Avilés Pablo, Schotsaert Michael, Zwaka Thomas, Vignuzzi Marco, Shokat Kevan M, Krogan Nevan J, García-Sastre Adolfo
Аннотация
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) viral proteins interact with the eukaryotic translation machinery, and inhibitors of translation have potent antiviral effects. We found that the drug plitidepsin (aplidin), which has limited clinical approval, possesses antiviral activity (90% inhibitory concentration = 0.88 nM) that is more potent than remdesivir against SARS-CoV-2 in vitro by a factor of 27.5, with limited toxicity in cell culture. Through the use of a drug-resistant mutant, we show that the antiviral activity of plitidepsin against SARS-CoV-2 is mediated through inhibition of the known target eEF1A (eukaryotic translation elongation factor 1A). We demonstrate the in vivo efficacy of plitidepsin treatment in two mouse models of SARS-CoV-2 infection with a reduction of viral replication in the lungs by two orders of magnitude using prophylactic treatment. Our results indicate that plitidepsin is a promising therapeutic candidate for COVID-19.
Предметные рубрики MeSH
Adenosine MonophosphateAlanineAnimalsAntiviral AgentsCOVID-19Coronavirus Nucleocapsid ProteinsDepsipeptidesDrug Evaluation, PreclinicalFemaleHEK293 CellsHumansLungMice, Inbred C57BLMutationPeptide Elongation Factor 1Peptides, CyclicPhosphoproteinsRNA, ViralSARS-CoV-2Virus ReplicationCOVID-19 Drug TreatmentMice