Litcius/Paper detail

Unrevealing sequence and structural features of novel coronavirus using in silico approaches: The main protease as molecular target

Joseph T. Ortega, María Luisa Serrano, Flor H. Pujol, Héctor R. Rangel

2020PubMed108 citationsDOIOpen Access PDF

Abstract

approach, we evaluated SARS-CoV-2 main protease as a target for HIV-1 protease inhibitors to reveal the structural features related to their antiviral effect. Our results showed that several HIV inhibitors such as lopinavir, ritonavir, and saquinavir produce strong interaction with the active site of SARS-CoV-2 main protease. Furthermore, broad library protease inhibitors obtained from PubChem and ZINC (www.zinc.docking.org) were evaluated. Our analysis revealed 20 compounds that could be clustered into three groups based on their chemical features. Then, these structures could serve as leading compounds to develop a series of derivatives optimizing their activity against SARS-CoV-2 and other coronaviruses. Altogether, the results presented in this work contribute to gain a deep understanding of the molecular pharmacology of SARS-CoV-2 treatment and validate the use of protease inhibitors against SARS-CoV-2.

Topics & Concepts

SaquinavirProteaseLopinavirPubChemIn silicoRitonavirIndinavirCoronavirusVirologyComputational biologyDocking (animal)BiologyHuman immunodeficiency virus (HIV)EnzymeMedicineCoronavirus disease 2019 (COVID-19)Viral loadBiochemistryAntiretroviral therapyGeneNursingPathologyDiseaseInfectious disease (medical specialty)Computational Drug Discovery MethodsSARS-CoV-2 and COVID-19 ResearchCOVID-19 Clinical Research Studies