Litcius/Paper detail

Identification of potential natural inhibitors of SARS-CoV2 main protease by molecular docking and simulation studies

Sanjay Gupta, Atul Kumar Singh, Prem Prakash Kushwaha, Kumari Sunita Prajapati, Mohd Shuaib, Sabyasachi Senapati, Shashank Kumar

2020Journal of Biomolecular Structure and Dynamics183 citationsDOIOpen Access PDF

Abstract

showed minimum binding score (-9.08 and -8.07 kcal/mole) against Mpro protein in comparison to shikonin and lopinavir (≈ -5.4 kcal/mole) a standard Mpro inhibitor. Furthermore, principal component analysis, free energy landscape and protein-ligand energy calculation studies revealed that these two compounds strongly bind to the catalytic core of the Mpro protein with higher efficacy than lopinavir, a standard antiretroviral of the protease inhibitor class. Taken together, this structure based optimization has provided lead on two natural Mpro inhibitors for further testing and development as therapeutics against human coronavirus.Communicated by Ramaswamy H. Sarma.

Topics & Concepts

Docking (animal)ProteaseIn silicoLopinavirChemistryStereochemistryCoronavirusCatalytic triadActive siteBiochemistryEnzymeComputational biologyBiologyHuman immunodeficiency virus (HIV)VirologyCoronavirus disease 2019 (COVID-19)GeneInfectious disease (medical specialty)DiseaseViral loadPathologyNursingAntiretroviral therapyMedicineComputational Drug Discovery MethodsSynthesis and biological activityCurcumin's Biomedical Applications