HIV‐1 reverse transcriptase still remains a new drug target: structure, function, classical inhibitors, and new inhibitors with innovative mechanisms of actions

F Esposito, A Corona… - Molecular biology …, 2012 - Wiley Online Library
During the retrotranscription process, characteristic of all retroviruses, the viral ssRNA
genome is converted into integration‐competent dsDNA. This process is accomplished by …

Ribonuclease H, an unexploited target for antiviral intervention against HIV and hepatitis B virus

E Tramontano, A Corona, L Menendez-Arias - Antiviral research, 2019 - Elsevier
Abstract Ribonucleases H (RNases H) are endonucleolytic enzymes, evolutionarily related
to retroviral integrases, DNA transposases, resolvases and numerous nucleases. RNases H …

Design, synthesis, biochemical, and antiviral evaluations of C6 benzyl and C6 biarylmethyl substituted 2-hydroxylisoquinoline-1, 3-diones: dual inhibition against HIV …

SKV Vernekar, Z Liu, E Nagy, L Miller… - Journal of medicinal …, 2015 - ACS Publications
Reverse transcriptase (RT) associated ribonuclease H (RNase H) remains the only virally
encoded enzymatic function not targeted by current chemotherapy against human …

The hepatitis B virus ribonuclease H is sensitive to inhibitors of the human immunodeficiency virus ribonuclease H and integrase enzymes

JE Tavis, X Cheng, Y Hu, M Totten, F Cao… - PLoS …, 2013 - journals.plos.org
Nucleos (t) ide analog therapy blocks DNA synthesis by the hepatitis B virus (HBV) reverse
transcriptase and can control the infection, but treatment is life-long and has high costs and …

Hydroxylated tropolones inhibit hepatitis B virus replication by blocking viral ribonuclease H activity

G Lu, E Lomonosova, X Cheng, EA Moran… - Antimicrobial agents …, 2015 - Am Soc Microbiol
Hepatitis B virus (HBV) remains a major human pathogen despite the development of both
antiviral drugs and a vaccine, in part because the current therapies do not suppress HBV …

The hepatitis B virus ribonuclease H as a drug target

JE Tavis, E Lomonosova - Antiviral research, 2015 - Elsevier
Chronic hepatitis B virus (HBV) infection is a leading cause of hepatitis, liver failure, and
hepatocellular carcinoma. An outstanding vaccine is available; however, the number of …

Identification of highly conserved residues involved in inhibition of HIV-1 RNase H function by diketo acid derivatives

A Corona, FS Di Leva, S Thierry… - Antimicrobial agents …, 2014 - Am Soc Microbiol
ABSTRACT HIV-1 reverse transcriptase (RT)-associated RNase H activity is an essential
function in viral genome retrotranscription. RNase H is a promising drug target for which no …

Insights into HIV-1 Reverse Transcriptase (RT) inhibition and drug resistance from thirty years of structural studies

AK Singh, K Das - Viruses, 2022 - mdpi.com
The enzyme reverse transcriptase (RT) plays a central role in the life cycle of human
immunodeficiency virus (HIV), and RT has been an important drug target. Elucidations of the …

Design, synthesis, and biological evaluations of hydroxypyridonecarboxylic acids as inhibitors of HIV reverse transcriptase associated RNase H

J Kankanala, KA Kirby, F Liu, L Miller… - Journal of medicinal …, 2016 - ACS Publications
Targeting the clinically unvalidated reverse transcriptase (RT) associated ribonuclease H
(RNase H) for human immunodeficiency virus (HIV) drug discovery generally entails …

“Old friends in new guise”: exploiting privileged structures for scaffold re-evolution/refining

Y Song, W Chen, D Kang, Q Zhang… - … Chemistry & High …, 2014 - ingentaconnect.com
The attempts to increase novel drug productivity through creative discovery technologies
have fallen short of producing the satisfactory results. For these reasons, evolved from the …