Data from extensive comparative measurements of conventional, conservation and organic agricultures in southwestern France.

This article present observational and experimental data describing a range of biotic and abiotic parameters that can be related to ecosystem services under contrasted types of crop management: conventional, conservation and organic agricultures. Ninety fields, either cultivated with winter wheat or fava bean, located in Southwestern France, near Toulouse, were monitored for two growing seasons (2014-2016). The dataset encompass data about crop pests (aphids, grain borer, bean beetles, slugs), crop pest natural enemies (hoverflies, parasitoids, predators), soil sensitivity to erosion, crop productivity, pathogenic fungal infection and root colonization by mycorrhiza.

Rational design of small-molecule inhibitors of the LEDGF/p75-integrase interaction and HIV replication.

Lens epithelium-derived growth factor (LEDGF/p75) is a cellular cofactor of HIV-1 integrase that promotes viral integration by tethering the preintegration complex to the chromatin. By virtue of its crucial role in the early steps of HIV replication, the interaction between LEDGF/p75 and integrase represents an attractive target for antiviral therapy. We have rationally designed a series of 2-(quinolin-3-yl)acetic acid derivatives (LEDGINs) that act as potent inhibitors of the LEDGF/p75-integrase interaction and HIV-1 replication at submicromolar concentration by blocking the integration step.

Study of a lipophilic captopril analogue binding to angiotensin I converting enzyme.

Human ACE is a central component of the renin-angiotensin system and a major therapeutic target for cardiovascular diseases. The somatic form of the enzyme (sACE) comprises two homologous metallopeptidase domains (N and C), each bearing a zinc active site with similar but distinct substrate and inhibitor specificities. In this study, we present the biological activity of silacaptopril, a silylated analogue of captopril, and its binding affinity towards ACE.

alpha,alpha'-disubstituted amino acids with silylated side chains as lipophilic building blocks for the synthesis of peptaibol analogues.

New alpha,alpha'-disubstituted amino acids with silylated side chains have been synthesized in racemic form. Starting from a Schiff base of glycine tert-butyl ester, a large variety of alpha,alpha'-dialkylated amino acids has been obtained, depending on the alkylating reagents. The application of a hydrosilylation methodology enabled the synthesis of the same unnatural amino acids in an enantiomerically pure form.

Complexation of lipofectamine and cholesterol-modified DNA sequences studied by single-molecule fluorescence techniques.

Lipoplex formation for normal and cholesterol-modified oligonucleotides is investigated by fluorescence correlation spectroscopy (FCS). To overcome the problems related to the fitting of autocorrelation curves when fluorescence bursts are present, the baseline fluorescence levels and the fluorescence bursts in the same trace were separately analyzed. This approach was not previously used in FCS studies of lipoplexes and allowed a more detailed characterization of this heterogeneous system.

Synthesis of a pyridoxine-peptide based delivery system for nucleotides.

As a first step in the development of a nucleotide delivery system making use of oligopeptide permease, we have synthesized pyridoxine-peptide-nucleotide conjugates. The nucleotides are bonded on serine residues. The peptides terminate with a pyroglutamate residue.

Conformational studies of proline-, thiaproline- and dimethylsilaproline-containing diketopiperazines.

As proline plays an important role in biologically active peptides, many analogues of this residue have been developed to modulate the proportion of cis and trans conformers. A correlation between the pyrrolidine ring shape and structural properties of proline has been established. Diketopiperazine (DKP) is the model of choice to study the influence of the proline ring modification.