Novel therapeutic strategies targeting HIV integrase

PK Quashie, RD Sloan, MA Wainberg - BMC medicine, 2012 - Springer
Integration of the viral genome into host cell chromatin is a pivotal and unique step in the
replication cycle of retroviruses, including HIV. Inhibiting HIV replication by specifically …

Molecular mechanisms of retroviral integrase inhibition and the evolution of viral resistance

S Hare, AM Vos, RF Clayton… - Proceedings of the …, 2010 - National Acad Sciences
The development of HIV integrase (IN) strand transfer inhibitors (INSTIs) and our
understanding of viral resistance to these molecules have been hampered by a paucity of …

Recent advances in the discovery of small-molecule inhibitors of HIV-1 integrase

E Choi, JR Mallareddy, D Lu, S Kolluru - Future science OA, 2018 - Taylor & Francis
AIDS caused by the infection of HIV is a prevalent problem today. Rapid development of
drug resistance to existing drug classes has called for the discovery of new targets. Within …

First-in-class small molecule inhibitors of the single-strand DNA cytosine deaminase APOBEC3G

M Li, SMD Shandilya, MA Carpenter… - ACS chemical …, 2012 - ACS Publications
APOBEC3G is a single-stranded DNA cytosine deaminase that comprises part of the innate
immune response to viruses and transposons. Although APOBEC3G is the prototype for …

Inhibiting the HIV integration process: past, present, and the future

R Di Santo - Journal of medicinal chemistry, 2014 - ACS Publications
HIV integrase (IN) catalyzes the insertion into the genome of the infected human cell of viral
DNA produced by the retrotranscription process. The discovery of raltegravir validated the …

HIV drug resistance and the advent of integrase inhibitors

PK Quashie, T Mesplède, MA Wainberg - Current infectious disease …, 2013 - Springer
This review focuses on the topic of HIV integrase inhibitors that are potent antiretroviral
drugs that efficiently decrease viral load in patients. However, emergence of resistance …

The HIV-1 integrase monomer induces a specific interaction with LTR DNA for concerted integration

KK Pandey, S Bera, DP Grandgenett - Biochemistry, 2011 - ACS Publications
The assembly mechanism for the human immunodeficiency virus type 1 (HIV) synaptic
complex (SC) capable of concerted integration is unknown. Molecular and structural studies …

[HTML][HTML] Multifunctional facets of retrovirus integrase

DP Grandgenett, KK Pandey, S Bera… - World Journal of …, 2015 - ncbi.nlm.nih.gov
The retrovirus integrase (IN) is responsible for integration of the reverse transcribed linear
cDNA into the host DNA genome. First, IN cleaves a dinucleotide from the 3'OH blunt ends of …

The Need for Development of New HIV‐1 Reverse Transcriptase and Integrase Inhibitors in the Aftermath of Antiviral Drug Resistance

MA Wainberg - Scientifica, 2012 - Wiley Online Library
The use of highly active antiretroviral therapy (HAART) involves combinations of drugs to
achieve maximal virological response and reduce the potential for the emergence of …

Critical appraisal of elvitegravir in the treatment of HIV-1/AIDS

KK Pandey - HIV/AIDS-Research and Palliative Care, 2014 - Taylor & Francis
Human immunodeficiency virus type 1 (HIV-1) integrase inhibitors belong to a novel class of
antiretroviral drugs with high potency and better tolerability. Elvitegravir (EVG) is the second …