Styrylquinoline derivatives: a new class of potent HIV-1 integrase inhibitors that block HIV-1 replication in CEM cells

…, D Desmaële, F Subra, H Leh… - Journal of medicinal …, 1998 - ACS Publications
On the basis of the fact that several polynucleotidyl transferases, related to HIV integrase,
contain in their active site two divalent metal cations, separated by ca. 4 Å, new potential HIV …

Structure− activity relationships and binding mode of styrylquinolines as potent inhibitors of HIV-1 integrase and replication of HIV-1 in cell culture

…, D Desmaële, D Savouré, H Leh… - Journal of medicinal …, 2000 - ACS Publications
Our prior studies showed that polyhydroxylated styrylquinolines are potent HIV-1 integrase (IN)
inhibitors that block the replication of HIV-1 in cell culture at nontoxic concentrations. To …

Oligomeric states of the HIV-1 integrase as measured by time-resolved fluorescence anisotropy

E Deprez, P Tauc, H Leh, JF Mouscadet, C Auclair… - Biochemistry, 2000 - ACS Publications
Self-assembly properties of HIV-1 integrase were investigated by time-resolved fluorescence
anisotropy using tryptophanyl residues as a probe. From simulation analyses, we show that …

Linker-modified quinoline derivatives targeting HIV-1 integrase: synthesis and biological activity

…, M Danet, D Desmaële, H Leh… - Bioorganic & medicinal …, 2004 - Elsevier
A novel series of HIV-1 integrase inhibitors was synthesized and tested in both in vitro and
ex vivo assays. These inhibitors are featured by the presence of a quinoline subunit and an …

Determinants of Mg2+-Dependent Activities of Recombinant Human Immunodeficiency Virus Type 1 Integrase

H Leh, P Brodin, J Bischerour, E Deprez, P Tauc… - Biochemistry, 2000 - ACS Publications
The relationship between Mg 2+ -dependent activity and the self-assembly state of HIV-1
integrase was investigated using different protein preparations. The first preparations, IN …

HIV-1 replication inhibitors of the styrylquinoline class: Introduction of an additional carboxyl group at the C-5 position of the quinoline

…, C Bénard, M Normand-Bayle, JF Mouscadet, H Leh… - Tetrahedron …, 2005 - Elsevier
Novel variants of HIV-1 replication inhibitors of the styrylquinoline class, bearing an additional
acid group or a propenoic acid moiety at the C-5 position of the quinoline have been …

Mechanism of HIV-1 integrase inhibition by styrylquinoline derivatives in vitro

E Deprez, S Barbe, M Kolaski, H Leh, F Zouhiri… - Molecular …, 2004 - ASPET
Styrylquinoline derivatives (SQ) efficiently inhibit the 3′-processing activity of integrase (IN)
with IC 50 values of between 0.5 and 5 μM. We studied the mechanism of action of these …

DNA binding induces dissociation of the multimeric form of HIV-1 integrase: a time-resolved fluorescence anisotropy study

E Deprez, P Tauc, H Leh… - Proceedings of the …, 2001 - National Acad Sciences
Self-assembly of HIV-1 integrase (IN) in solution has been studied previously by time-resolved
fluorescence, using tryptophan anisotropy decay. This approach provides information on …

Styrylquinolines, integrase inhibitors acting prior to integration: a new mechanism of action for anti-integrase agents

…, D Desmaële, J d'Angelo, JF Mouscadet, H Leh - Journal of …, 2004 - Am Soc Microbiol
We have previously shown that styrylquinolines (SQLs) are integrase inhibitors in vitro. They
compete with the long terminal repeat substrate for integrase. Here, we describe the cellular …

Vertically coupled polymer microracetrack resonators for label-free biochemical sensors

C Delezoide, M Salsac, J Lautru, H Leh… - IEEE Photonics …, 2011 - ieeexplore.ieee.org
We report on the efficient design and fabrication of polymeric microracetrack optical resonators
for label-free biosensing purposes. Vertically-coupled microresonators immersed in …