G-quadruplexes in viruses: function and potential therapeutic applications

M Métifiot, S Amrane, S Litvak… - Nucleic acids …, 2014 - academic.oup.com
G-rich nucleic acids can form non-canonical G-quadruplex structures (G4s) in which four
guanines fold in a planar arrangement through Hoogsteen hydrogen bonds. Although many …

HIV integrase inhibitors: 20-year landmark and challenges

M Métifiot, C Marchand, Y Pommier - Advances in pharmacology, 2013 - Elsevier
Since the discovery of HIV as the cause for AIDS 30 years ago, major progress has been
made, including the discovery of drugs that now control the disease. Here, we review the …

[HTML][HTML] Resistance to integrase inhibitors

M Métifiot, C Marchand, K Maddali, Y Pommier - Viruses, 2010 - mdpi.com
Integrase (IN) is a clinically validated target for the treatment of human immunodeficiency
virus infections and raltegravir exhibits remarkable clinical activity. The next most advanced IN …

Structure–activity relationship of pyrrolyl diketo acid derivatives as dual inhibitors of HIV-1 integrase and reverse transcriptase ribonuclease H domain

G Cuzzucoli Crucitti, M Métifiot… - Journal of medicinal …, 2015 - ACS Publications
The development of HIV-1 dual inhibitors is a highly innovative approach aimed at reducing
drug toxic side effects as well as therapeutic costs. HIV-1 integrase (IN) and reverse …

Bronchial epithelia from adults and children: SARS-CoV-2 spread via syncytia formation and type III interferon infectivity restriction

…, P Esteves, M Faure, M Métifiot… - Proceedings of the …, 2022 - National Acad Sciences
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infections initiate in the
bronchi of the upper respiratory tract and are able to disseminate to the lower respiratory tract, …

HIV-1 IN inhibitors: 2010 update and perspectives

C Marchand, K Maddali, M Métifiot… - Current topics in …, 2009 - ingentaconnect.com
Integrase (IN) is the newest validated target against AIDS and retroviral infections. The
remarkable activity of raltegravir (Isentress®) led to its rapid approval by the FDA in 2007 as the …

Basic quinolinonyl diketo acid derivatives as inhibitors of HIV integrase and their activity against RNase H function of reverse transcriptase

R Costi, M Métifiot, S Chung… - Journal of Medicinal …, 2014 - ACS Publications
A series of antiviral basic quinolinonyl diketo acid derivatives were developed as inhibitors
of HIV-1 IN. Compounds 12d,f,i inhibited HIV-1 IN with IC 50 values below 100 nM for strand …

Elvitegravir overcomes resistance to raltegravir induced by integrase mutation Y143

M Métifiot, N Vandegraaff, K Maddali, A Naumova… - Aids, 2011 - journals.lww.com
Objective: In this study, we characterized elvitegravir activity in the context of raltegravir
resistance mutations. Design: Using site-directed mutagenesis, we generated recombinant …

4-amino-1-hydroxy-2-oxo-1, 8-naphthyridine-containing compounds having high potency against raltegravir-resistant integrase mutants of HIV-1

XZ Zhao, SJ Smith, M Métifiot, C Marchand… - Journal of Medicinal …, 2014 - ACS Publications
There are currently three HIV-1 integrase (IN) strand transfer inhibitors (INSTIs) approved by
the FDA for the treatment of AIDS. However, the emergence of drug-resistant mutants …

6-(1-Benzyl-1H-pyrrol-2-yl)-2,4-dioxo-5-hexenoic Acids as Dual Inhibitors of Recombinant HIV-1 Integrase and Ribonuclease H, Synthesized by a Parallel Synthesis …

R Costi, M Métifiot, F Esposito… - Journal of medicinal …, 2013 - ACS Publications
The increasing efficiency of HAART has helped to transform HIV/AIDS into a chronic disease.
Still, resistance and drug–drug interactions warrant the development of new anti-HIV …