MOLECULAR DOCKING AND SCREENING OF DRUGS FOR 6LU7 PROTEASE INHIBITOR AS A
POTENTIAL TARGET FOR COVID-19
Original Article
MANOJ GADEWAR
1
, BHARAT LAL
2
1
Department of Pharmacology, K. R. Mangalam University, Gurugram, Haryana, India,
2
Department of Pharmaceutics, K. R. Mangalam
University, Gurugram, Haryana, India
Email: manojgadewar@gmail.com
Received: 14 Sep 2021, Revised and Accepted: 25 Oct 2021
ABSTRACT
Objective: The aim of present investigation is docking of various existing antiviral, anti-tubercular and anti-malarial drugs on 6LU7 receptor of
SARS-CoV-2 in the treatment of COVID-19.
Methods: In this study, the structure of coronavirus binding protein and ligands for various drugs were collected from the protein data bank and
pub chem. Molecular docking was carried out using Schrodinger 9.0 software. In molecular docking study, 19 different drugs of various categories
like antiviral, anti-malarial and anti-tubercular were investigated for analyzing binding to 6LU7 receptors of COVID-19.
Results: The docking result showed a high affinity of zanamivir, montelukast, ramdesvir, ritonavir, cobicistat and favipravir to the 6LU7 receptor of
novel coronavirus. Thus the combination of these drugs may be useful in preventing further infection and can be used as a potential target for
further in vitro and in vivo studies of SARS-CoV-2.
Conclusion: Treatment of COVID-19 has been challenge due to the non-availability of effective drug therapy. In this study, we reported drugs for
targeting 6LU7 Mpro/3Clpro protein, which showed prominent effects as potential inhibitors of COVID-19 Mpro.
Keywords: COVID-19, RNA dependant RNA polymerase, Molecular docking, Antiviral, Anti-malarial
© 2022 The Authors. Published by Innovare Academic Sciences Pvt Ltd. This is an open access article under the CC BY license (https://creativecommons.org/licenses/by/4.0/)
DOI: https://dx.doi.org/10.22159/ijap.2022v14i1.43132. Journal homepage: https://innovareacademics.in/journals/index.php/ijap
INTRODUCTION
Since December 2019, an epidemic of corona has been spreading all
across the globe. China reported a case of pneumonia of unknown
cause on 31st Dec 2019 in some patient operating in Huanan
seafood market of Wuhan in Hubei province and caused outbreak of
a novel corona (nCOVID-19). After genome analysis it was found that
causative agent for the infection was zoonotic coronavirus and this
novel Coronavirus (2019-nCoV) which resembles similarity with
severe acute respiratory syndrome coronavirus (SARS-CoV) and
Middle East Respiratory Syndrome coronavirus (MERS-CoV) but
with fast transmission and rapid rate of infection. On 11
th
March
2020 WHO characterized COVID-19 outbreak is a pandemic and
released interim guidelines on critical preparedness, readiness and
response actions to keep people safe from the COVID-19 [1, 2].
Due to the characteristic appearance of crown-like spikes around the
virion it is renamed as corona virus. Coronaviruses belongs to
the sub family Orthocoronavirinae, of the family Coronaviridae,
order Nidovirales. Coronaviruses are spherical-shaped viruses
having size around 120 nm diameters. These are lipid bilayered
viruses consist of membrane (M), envelope (E) and spike
(S) structural proteins. Inside the envelope it contains nucleocapsid
formed from multiple copies of the nucleocapsid (N) protein,
which are anchored with a positive-sense single-
stranded RNA genome in a continuous beads-on-a-string type
conformation. The genome size of coronaviruses is largest among
RNA viruses which ranges approximately from 27 to
34 kilobases3and it has a 5′ methylated cap and a 3′ polyadenylated
tail fig. 1 [3].
Fig. 1: Structure of COVID-19
Genetically they are classified into four major genera Alpha, Beta,
Gamma, and Delta coronavirus; the former two genera primarily
infect mammals, whereas the latter two predominantly infect birds.
Six kinds of human coronavirus have been previously identified,
which include HCoV-NL63 and HCoV229E (Alpha coronavirus) and
HCoV-OC43, HCoVHKU1, SARS-CoV, MERS-CoV (Beta coronavirus)
and COVID-19 is seventh [4].
The life cycle of COVID-19 begins in host cells once it reaches to
lungs and binds to the type-II pneumocytes of the alveoli using its
International Journal of Applied Pharmaceutics
ISSN- 0975-7058 Vol 14, Issue 1, 2022