Staff View: Search for new therapeutics against HIV-1 via dual inhibition of RNase H and integrase: Current status and future challenges

Search for new therapeutics against HIV-1 via dual inhibition of RNase H and integrase: Current status and future challenges

Reverse transcriptase and integrase are key enzymes that play a pivotal role in HIV-1 viral maturation and replication. Reverse transcriptase consists of two active sites: RNA-dependent DNA polymerase and RNase H. The catalytic domains of integrase and RNase H share striking similarity, comprising t...

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Main Authors:	Kharkwal, Harsha, Kumar, Banoth K., Murugesan, Sankaranarayanan, Singhvi, Gautam, Avasthi, Preeti, Goyal, Ankush, Jamalis, Joazaizulfazli, Chander, Subhash
Format:	Article
Published:	Future Medicine Ltd. 2021
Subjects:	QD Chemistry
Online Access:	http://eprints.utm.my/id/eprint/94876/ http://dx.doi.org/10.4155/fmc-2020-0257
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id	my.utm.94876
record_format	eprints
spelling	my.utm.948762022-04-29T22:22:01Z http://eprints.utm.my/id/eprint/94876/ Search for new therapeutics against HIV-1 via dual inhibition of RNase H and integrase: Current status and future challenges Kharkwal, Harsha Kumar, Banoth K. Murugesan, Sankaranarayanan Singhvi, Gautam Avasthi, Preeti Goyal, Ankush Jamalis, Joazaizulfazli Chander, Subhash QD Chemistry Reverse transcriptase and integrase are key enzymes that play a pivotal role in HIV-1 viral maturation and replication. Reverse transcriptase consists of two active sites: RNA-dependent DNA polymerase and RNase H. The catalytic domains of integrase and RNase H share striking similarity, comprising two aspartates and one glutamate residue, also known as the catalytic DDE triad, and a Mg2+ pair. The simultaneous inhibition of reverse transcriptase and integrase can be a rational drug discovery approach for combating the emerging drug resistance problem. In the present review, the dual inhibition of RNase H and integrase is systematically discussed, including rationality of design, journey of development, advancement and future perspective. Future Medicine Ltd. 2021 Article PeerReviewed Kharkwal, Harsha and Kumar, Banoth K. and Murugesan, Sankaranarayanan and Singhvi, Gautam and Avasthi, Preeti and Goyal, Ankush and Jamalis, Joazaizulfazli and Chander, Subhash (2021) Search for new therapeutics against HIV-1 via dual inhibition of RNase H and integrase: Current status and future challenges. Future Medicinal Chemistry, 13 (3). pp. 269-286. ISSN 1756-8919 http://dx.doi.org/10.4155/fmc-2020-0257
institution	Universiti Teknologi Malaysia
building	UTM Library
collection	Institutional Repository
continent	Asia
country	Malaysia
content_provider	Universiti Teknologi Malaysia
content_source	UTM Institutional Repository
url_provider	http://eprints.utm.my/
topic	QD Chemistry
spellingShingle	QD Chemistry Kharkwal, Harsha Kumar, Banoth K. Murugesan, Sankaranarayanan Singhvi, Gautam Avasthi, Preeti Goyal, Ankush Jamalis, Joazaizulfazli Chander, Subhash Search for new therapeutics against HIV-1 via dual inhibition of RNase H and integrase: Current status and future challenges
description	Reverse transcriptase and integrase are key enzymes that play a pivotal role in HIV-1 viral maturation and replication. Reverse transcriptase consists of two active sites: RNA-dependent DNA polymerase and RNase H. The catalytic domains of integrase and RNase H share striking similarity, comprising two aspartates and one glutamate residue, also known as the catalytic DDE triad, and a Mg2+ pair. The simultaneous inhibition of reverse transcriptase and integrase can be a rational drug discovery approach for combating the emerging drug resistance problem. In the present review, the dual inhibition of RNase H and integrase is systematically discussed, including rationality of design, journey of development, advancement and future perspective.
format	Article
author	Kharkwal, Harsha Kumar, Banoth K. Murugesan, Sankaranarayanan Singhvi, Gautam Avasthi, Preeti Goyal, Ankush Jamalis, Joazaizulfazli Chander, Subhash
author_facet	Kharkwal, Harsha Kumar, Banoth K. Murugesan, Sankaranarayanan Singhvi, Gautam Avasthi, Preeti Goyal, Ankush Jamalis, Joazaizulfazli Chander, Subhash
author_sort	Kharkwal, Harsha
title	Search for new therapeutics against HIV-1 via dual inhibition of RNase H and integrase: Current status and future challenges
title_short	Search for new therapeutics against HIV-1 via dual inhibition of RNase H and integrase: Current status and future challenges
title_full	Search for new therapeutics against HIV-1 via dual inhibition of RNase H and integrase: Current status and future challenges
title_fullStr	Search for new therapeutics against HIV-1 via dual inhibition of RNase H and integrase: Current status and future challenges
title_full_unstemmed	Search for new therapeutics against HIV-1 via dual inhibition of RNase H and integrase: Current status and future challenges
title_sort	search for new therapeutics against hiv-1 via dual inhibition of rnase h and integrase: current status and future challenges
publisher	Future Medicine Ltd.
publishDate	2021
url	http://eprints.utm.my/id/eprint/94876/ http://dx.doi.org/10.4155/fmc-2020-0257
_version_	1732945404948905984
score	13.211869

Search for new therapeutics against HIV-1 via dual inhibition of RNase H and integrase: Current status and future challenges

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