Volume 7(6): 367-373 (2015) - 367
J Microb Biochem Technol
ISSN: 1948-5948 JMBT, an open access journal
Sharma et al., J Microb Biochem Technol 2015, 7:6
DOI: 10.4172/1948-5948.1000240
Research Article Open Access
Denovo Designing, Virtual Screening and Lead Optimization of Potential
Drug Candidate for Herpes Disease
Monica Sharma
1,2
*, Puneet Rawat
2
and Ankita Mehta
2
1
Department of Biotechnology, School of Biosciences and Biotechnology, Babasaheb Bhimrao Ambedkar University, Vidya Vihar, Raebareli Road, Lucknow, Uttar
Pradesh, India
2
Department of Biotechnology, Delhi Technological University, Main Bawana Road, Shahbad Daulatpur, Delhi, India
*Corresponding authors: Monica Sharma, Department of Biotechnology, Delhi
Technological University, Main Bawana Road, Shahbad Daulatpur, Delhi, India, Tel:
+91-9717386785; E-mail: monashimla@gmail.com
Received September 26, 2015; Accepted October 17, 2015; Published October
24, 2015
Citation: Sharma M, Rawat P, Mehta A (2015) Denovo Designing, Virtual Screening
and Lead Optimization of Potential Drug Candidate for Herpes Disease. J Microb
Biochem Technol 7: 367-373. doi:10.4172/1948-5948.1000240
Copyright: © 2015 Sharma M, et al. This is an open-access article distributed
under the terms of the Creative Commons Attribution License, which permits
unrestricted use, distribution, and reproduction in any medium, provided the
original author and source are credited.
Keywords: HSV; ICP-47; eLEA3D; Denovo designing; Bioisosteres
Introduction
Herpes simplex viruses (HSV) 1 and 2, the members of herpes
virus family Herpesviridae are ubiquitous, highly contigious agents
which infect humans [1,2]. Tey cause cold sores, herpetic keratitis
and genital herpes [3-5]. An estimated 400 million people worldwide
are currently infected by HSV-2 and infection of HSV-1 is spreading
to developed regions like USA, Western Europe, Australia and
New Zealand [WHO Fact Sheet, 2015]. HSV-1 persists in the body
in dormant state by escaping the immune system and results in
sporadic viral reactivation [6].
HSV evades the immune system by interfering with MHC Class
I antigen presentation on the cell surface. Infected cell protein (ICP)
47 caused major histocompatibility complex (MHC) class I proteins
retaintion in the endoplasmic reticulum (ER). MHC presents the
antigen to CD
+
8 T cells that are inhibited afer expression of ICP 47 in
the cell [7]. ICP 47 blocks peptide (viral epitope) transport across the
ER membrane by transporter associated with antigen processing (TAP)
[8,9] so that MHC class I proteins remain in ER without peptides and
cytotoxic T- lymphocytes activation can be stopped. Tis allows virus
to reside for a protracted period in the host.
Due to serious threat to human population a proper treatment and
cure of HSV is required. For last two decades HSV glycoprotein D, has
been the predominant HSV vaccine candidate [10,11], but the outcome
of clinical trials of the vaccine have been really disappointing [12].
Antiviral drugs (valacyclovir, acyclovir, famciclovir, etc.) used against
HSV infection, inhibit DNA polymerases and slows down infection by
reducing viral replication but does not cure the infection completely
[13]. Inappropriate prescribing and wide spread uncontrolled use of
antiviral drugs led to emergence of resistance in the viruses. Recently,
it has been observed that natural serine protease inhibitor (serpins)
like serpinantithrombin III (AT III) inhibit HSV infection during
an entry event. Antithrombin III demonstrated a promising result at
experimental levels but yet it is far from any therapeutic use [13,14].
Due to inaccessibility of any efective drug and vaccine there is
therefore, an urgent need for an efective HSV vaccine or drug that
provides protection against infection and also thwart the virus entering
a latent state [15]. Computer aided drug discovery design (CADD) has
emerged as a way to signifcantly decrease compounds screening while
retaining same level of lead compound discovery at the same time [16].
In the present manuscript we have designed lead compound by de-
novo designing strategy and molecule having highest score was further
optimized by virtual screening to increase its afnity to target and
reduce toxicity by toxicological analysis by online ADMET profling
tools of FAF DRUG 20 online tool and ORISIS data warrior.
Methodology
Sequence retrival
DNA sequence of ICP-47 of HSV-2 was retrieved from NCBI and
it was blasted to human genomic and transcriptomic database. Te
structure of target protein ICP-47 was retrieved from rcsb.org in PDB
(text) format (PDB I.D. 1QLO).
Denovo drug designing
Afer exhaustive literature survey and database searching, no ligand
was found that bind to this target, so automated de-novo drug design
strategy was adopted to get a hit molecule. eLEA3D program was used
for denovo generation of ligand, which create new molecules by using a
library of molecular fragments and by determining best combinations
of molecular fragments that ft user-defned physicochemical properties
Abstract
Herpes simplex virus (HSV1, HSV 2) is a neurotropic and neuroinvasive virus which becomes latent and causes
a lifelong infection. HSV-1 and 2 produce infected cell protein (ICP)-47 against MHC class I antigen presentation
pathway by inhibiting the transporter associated with antigen processing (TAP). ICP 47 is also responsible for
evasive nature of HSV in human immune system. Currently available antiviral drugs and vaccines only slowdowns
the infection but it does not cure the infection. In present study, we have in silico designed a potential drug candidate
against HSV ICP-47 target through de-novo pathway using eLEA3D. The derived ligand docked with the natural viral
receptor ICP-47 showed the binding affnity of -4.07, but it was found toxic in FAF DRUG online ADMET tool, due to
presence of high risk imine group. Further manual optimization led to generation of many bioisosteres and fnal lead
structure showed no toxicity and a high binding affnity of -7.53. Our designed lead can act as a potential therapeutic
compound against HSV.
Journal of
Microbial & Biochemical Technology
J
o
u
r
n
a
l
o
f
M
i
c
r
o
b
i
a
l
&
B
i
o
c
h
e
m
i
c
a
l
T
e
c
h
n
o
l
o
g
y
ISSN: 1948-5948