Original Article
IN SILICO ANALYSIS OF TECOVIRIMAT A REPURPOSED DRUG AGAINST THE MONKEYPOX
VIRUS, ITS OFF-TARGET HUMAN PROTEINS, AND IMPACT ON HUMAN HEALTH
JANVI AGGARWAL
1
, POONAM SHARMA
1*
Department of Zoology, Gargi College, University of Delhi, India
*
Corresponding author: Poonam Sharma;
*
Email: poonam.sharma@gargi.du.ac.in
Received: 19 Aug 2023, Revised and Accepted: 04 Oct 2023
ABSTRACT
Objective: In this study, in silico analysis of human off-target proteins of tecovirimat, an investigational drug reported to stop monkey pox virus
infection by binding to a protein that the virus uses to enter host cells was performed to better understand its off-target long-term and short-term
effects on other important biological processes in patients.
Methods: The target and off-target proteins of the drug, as well as their characteristics, protein-protein interactions, and the pathways they are
involved in, were thoroughly analyzed using a number of databases, including Drug Bank, the NCBI Gene Database, BLAST, the UCSC Gene Sorter,
Gene MANIA, STRING, and the Kyoto Encyclopedia of Genes and Genomes (KEGG) Pathway Database.
Results: The current study showed that although the repurposing drug tecovirimat aids in the treatment of patients with monkeypox by binding to
the viral p37 protein, it can also accidentally interfere with vital biological processes by interacting with off-target proteins or by indirectly
interfering with the proteins that interact with these target proteins.
Conclusion: The findings highlight the importance of extensively assessing and evaluating all repurposed drugs for their off-target effects before
making them available to the general public.
Keywords: Monkeypox, Tecovirimat, p37 protein, Rheumatoid arthritis, Alzheimer's disease
© 2023 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.2023v15i6.49248. Journal homepage: https://innovareacademics.in/journals/index.php/ijap
INTRODUCTION
Monkeypox is caused by a DNA virus (MPV, MPXV, or hMPXV),
which was found in humans in 2003. Monkeypox virus is a
zoonotic virus that belongs to the orthopoxvirus family and has a
genome size of 190 kb. The monkeypox virus, like other
poxviruses, has an oval shape and an outer lipoprotein membrane
that shields viral enzymes, DNA, and transcription factors.
Monkeypox viruses rely mostly on the protein encoded in their
genome that permits them to multiply in the cytoplasm of the host
cells [1]. Like smallpox and rabbitpox, monkeypox is a poxvirus
with a peculiar life cycle. Despite being DNA viruses, monkeypox
totally bypasses the host cell nucleus and instead completes
replication, transcription, translation, and virus assembly in the
cytoplasm. MPXV transmission can occur through an animal bite
or scratch direct contact with an infected animal's blood, biological
fluids, tissue, or sores.
As soon as the virus attaches to and fuses with the host cell, it
uncoats and begins to produce early genes. At this stage, DNA
replication initiates, followed by the transcription of early and late
genes. The p37 protein aids in the formation and coating of
intracellular mature virions (IMVs), which can either remain inside
host cells as cell-associated virus (CEV) particles or migrate outside
cells as extracellular enveloped virus (EEV) particles. p37 is a 37 kDa
peripheral membrane protein expressed by the F13L gene that plays
an important role in IMV particle envelopment. As a result, p37 is
responsible for virulence by producing and egressing wrapped
virions. The emergence of zoonotic diseases has grown increasingly
widespread as a result of a variety of factors such as urbanization,
deforestation, tourism, zoos, climate change, and wildlife
exploitation. Drug repurposing has effectively found promising
candidate drugs that potentially open up new treatment paths for
treating these emerging viruses such as SARS-CoV-2, MERS-CoV, and
H5N1 [2]. Repurposing existing drugs can be appealing, given the
process is often safer, less expensive, and can be carried out in less
time. One such repurposed medicine, tecovirimat, was recently
licensed by the US Food and medicine Administration (FDA) against
poxviruses and targets the critical viral p37 protein [3] (fig. 1).
Fig. 1: Structure of tecovirimat drug (a) 2D structure (b) 3D structure
Tecovirimat inhibits the crucial viral p37 protein and consequently
prevents the formation and egress of enveloped virions, which are
essential for virulence (fig. 2). As most investigational drugs have a range
of mild to severe short-and long-term unfavorable side effects, this study
aimed to understand tecovirimat’s off-target effects by identifying and
analyzing structurally comparable off-target proteins. It also aimed to
explore the possibility of analyzing tecovirimat drug behavior in silico for
effective pathological control and after-effect management.
International Journal of Applied Pharmaceutics
ISSN- 0975-7058 Vol 15, Issue 6, 2023