Radiographic Inspection of Carbon Fiber-Reinforced Polymer Composites (Laminates) with Epoxy and PEEK Binders After Impact and Subsequent Compression Loading.

An approach to detecting discontinuities in carbon fiber-reinforced polymers, caused by impact loading followed by compression testing, was developed. An X-ray sensor-based installation was used, while some algorithms were developed to improve the quality of the obtained low-contrast radiographic images with negligible signal-to-noise ratios. For epoxy/AF (#1) composite subjected to a "high-velocity" steel-ball impact with subsequent compression loading, it was not possible to detect discontinuities since the orientation of the extended zone of interlayer delamination was perpendicular to the irradiation axis.

Structure-based design of small-molecule ligands of phosphofructokinase-2 activating or inhibiting glycolysis.

Glycolysis lies at the basis of metabolism and cell energy supply. The disregulation of glycolysis is involved in such pathological processes as cancer proliferation, neurodegenerative diseases, and amplification of ischemic damage. Phosphofructokinase-2 (PFK-2), a bifunctional enzyme and regulator of glycolytic flux, has recently emerged as a promising anticancer target.

Identification of a small-molecule inhibitor of HIV-1 assembly that targets the phosphatidylinositol (4,5)-bisphosphate binding site of the HIV-1 matrix protein.

The development of drug resistance remains a critical problem for current HIV-1 antiviral therapies, creating a need for new inhibitors of HIV-1 replication. We previously reported on a novel anti-HIV-1 compound, N(2)-(phenoxyacetyl)-N-[4-(1-piperidinylcarbonyl)benzyl]glycinamide (14), that binds to the highly conserved phosphatidylinositol (4,5)-bisphosphate (PI(4,5)P(2)) binding pocket of the HIV-1 matrix (MA) protein. In this study, we re-evaluate the hits from the virtual screen used to identify compound 14 and test them directly in an HIV-1 replication assay using primary human peripheral blood mononuclear cells.

Discovery of a small-molecule antiviral targeting the HIV-1 matrix protein.

Due to the emergence of drug-resistant strains and the cumulative toxicities associated with current therapies, demand remains for new inhibitors of HIV-1 replication. The HIV-1 matrix (MA) protein is an essential viral component with established roles in the assembly of the virus. Using virtual and surface plasmon resonance (SPR)-based screening, we describe the identification of the first small molecule to bind to the HIV-1 MA protein and to possess broad range anti-HIV properties.

Transcription Factor DLX5 As a New Target for Promising Antitumor Agents.

The crystal structure of the human transcription factor DLX5 has been used for the screening of a library consisting of 10(6 )compounds by the molecular docking technique.In vitro testsof the 14 top-rated ligands showed that compound Q12 displays the best ability to inhibit the proliferation ofDlx5 positive mouse lymphoma cells, which correlates with the down-regulation ofc-mycexpression. Compound Q12 has low toxicity on normal human ovarian epithelial cells and mouse lymphoma cells with absent expression ofDlx5, and can be used for further chemical optimization and for the development of novel, highly efficient cancer treatments.