Targeting metalloenzymes for therapeutic intervention
AY Chen, RN Adamek, BL Dick, CV Credille… - Chemical …, 2018 - ACS Publications
Metalloenzymes are central to a wide range of essential biological activities, including
nucleic acid modification, protein degradation, and many others. The role of metalloenzymes …
nucleic acid modification, protein degradation, and many others. The role of metalloenzymes …
Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection
V Summa, A Petrocchi, F Bonelli… - Journal of medicinal …, 2008 - ACS Publications
Human immunodeficiency virus type-1 (HIV-1) integrase is one of the three virally encoded
enzymes required for replication and therefore a rational target for chemotherapeutic …
enzymes required for replication and therefore a rational target for chemotherapeutic …
HIV‐1 integrase inhibitors: 2005–2006 update
Abstract HIV‐1 integrase (IN) catalyzes the integration of proviral DNA into the host genome,
an essential step for viral replication. Inhibition of IN catalytic activity provides an attractive …
an essential step for viral replication. Inhibition of IN catalytic activity provides an attractive …
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 …
DNA produced by the retrotranscription process. The discovery of raltegravir validated the …
Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1, 6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties
Among a large number of HIV-1 integrase (IN) inhibitors, the 8-hydroxy-[1, 6] naphthyridines
(ie, L-870,810) were one of the promising class of antiretroviral drugs developed by Merck …
(ie, L-870,810) were one of the promising class of antiretroviral drugs developed by Merck …
[HTML][HTML] Chemistry and structure-activity relationship of the styrylquinoline-type HIV integrase inhibitors
JF Mouscadet, D Desmaële - Molecules, 2010 - mdpi.com
In spite of significant progress in anti-HIV-1 therapy, current antiviral chemo-therapy still
suffers from deleterious side effects and emerging drug resistance. Therefore, the …
suffers from deleterious side effects and emerging drug resistance. Therefore, the …
Targeting HIV-1 integrase with strand transfer inhibitors
Y Li, S Xuan, Y Feng, A Yan - Drug Discovery Today, 2015 - Elsevier
Highlights•Overview of structural and functional properties of HIV-1 integrase
(IN).•Classifying the HIV-1 integrase strand transfer inhibitors (INSTIs) into ten …
(IN).•Classifying the HIV-1 integrase strand transfer inhibitors (INSTIs) into ten …
Inhibiting HCMV pUL89-C Endonuclease with Metal-Binding Compounds: Miniperspective
Human cytomegalovirus (HCMV) infects individuals of all ages and establishes a lifelong
latency. Current antiviral drugs are suboptimal in efficacy and safety and ineffective against …
latency. Current antiviral drugs are suboptimal in efficacy and safety and ineffective against …
Design and synthesis of bicyclic pyrimidinones as potent and orally bioavailable HIV-1 integrase inhibitors
E Muraglia, O Kinzel, C Gardelli… - Journal of medicinal …, 2008 - ACS Publications
HIV integrase is one of the three enzymes encoded by HIV genome and is essential for viral
replication, but integrase inhibitors as marketed drugs have just very recently started to …
replication, but integrase inhibitors as marketed drugs have just very recently started to …
[HTML][HTML] Antiviral drugs
R Vardanyan, V Hruby - Synthesis of best-seller drugs, 2016 - ncbi.nlm.nih.gov
Antiviral Drugs - PMC Back to Top Skip to main content NIH NLM Logo Access keys NCBI
Homepage MyNCBI Homepage Main Content Main Navigation Search PMC Full-Text Archive …
Homepage MyNCBI Homepage Main Content Main Navigation Search PMC Full-Text Archive …