Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.

Dissymmetric cross metathesis of alkenes as a convergent and general synthetic strategy allowed for the preparation of a new small series of human histone deacetylases (HDAC) inhibitors. Alkenes bearing Boc-protected hydroxamic acid and benzamide and trityl-protected thiols were used to provide the zinc binding groups and were reacted with alkenes bearing aromatic cap groups. One compound was identified as a selective HDAC6 inhibitor lead.

Biocompatible Spherical Gold Nanoparticles Synthesis in Aqueous Tetraethylene Oxide Solution and Their Cellular Uptake.

Small well-defined spherical gold nanoparticles were synthesized by a simple non-physical method based on a mixture of gold salt, tetraethylene oxide and water, free of any additional reducing chemical agent or physical method. The ratio of tetraethylene oxide to water was optimized to achieve a fast synthesis within 30 min. Transmission electron microscopy images showed well dispersed gold nanospheres with a size ranging from 10 to 15 nm.

Tri-methylation of H3K79 is decreased in TGF-β1-induced epithelial-to-mesenchymal transition in lung cancer.

Background: The epithelial-to-mesenchymal transition (EMT) enables epithelial cancer cells to acquire mesenchymal features and contributes to metastasis and resistance to treatment. This process involves epigenetic reprogramming for gene expression. We explored global histone modifications during TGF-β1-induced EMT in two non-small cell lung cancer (NSCLC) cell lines and tested different epigenetic treatment to modulate or partially reverse EMT.

Analysis of monomeric mutants of HSC70: a possible relationship between oligomerization and functional properties.

Data of this study showed that alphaD-alphaE helices and the conserved interdomain linker are two interfaces essential not only for the self-association but also for the functional properties of rat HSC70. Self-association which is a conserved property of HSP70 seems to be important for the activity of these proteins.