Selective degradation of histone deacetylase 8 mediated by a proteolysis targeting chimera (PROTAC).

We developed a first-in-class proteolysis targeting chimera (PROTAC) for selective degradation of histone deacetylase 8 (HDAC8). The PROTAC induced degradation of HDAC8 without affecting the levels of other HDACs in cellular assays, and inhibited the growth of T-cell leukemia Jurkat cells more potently than a conventional HDAC8 inhibitor.

evaluation of local antibiotic delivery via fibrin hydrogel.

Background/purpose: Fibrin hydrogel is commonly used as hemostatic agent and scaffold but it is questionable for carrying antibiotics. Thus, this study aimed to investigate whether the fibrin hydrogel can be used to deliver the optimal concentration of ciprofloxacin against oral pathogen.

Materials And Methods: The optimal concentration of ciprofloxacin was investigated from broth microdilution technique against three common oral bacteria.

Identification of ortho-hydroxy anilide as a novel scaffold for lysine demethylase 5 inhibitors.

Fe(II)/α-ketoglutarate-dependent lysine demethylases (KDMs) are attractive drug targets for several diseases including cancer. In this study, we designed and screened ortho-substituted anilides that are expected to function as Fe(II) chelators, and identified ortho-hydroxy anilide as a novel scaffold for KDM5A inhibitors. Treatment of human lung cancer A549 cells with a prodrug form of 4-carboxy-2-hydroxy-formanilide (9c) increased trimethylated lysine 4 on histone H3 level, suggesting KDM5 inhibition in the cells.

Eucalyptus ash alters secondary protein conformation of human grey hair and facilitates anthocyanin dyeing.

Wood ashes infused with water have been traditionally used as hair cosmetics, but little or no research has examined the effects of ash on human hair. This study investigated the effect of eucalyptus ash on the structure and morphology of excised human grey hair and its potential use as a pretreatment in natural hair dyeing using anthocyanins extracted from purple cops of Zea mays. Tensile characteristics and surface morphology of ash-pretreated hair was monitored by texture analysis, scanning electron microscopy and atomic force microscopy.