One stone two birds: Introducing piperazine into a series of nucleoside derivatives as potent and selective PRMT5 inhibitors.

The protein arginine methyltransferase 5 (PRMT5) has emerged as potential target for the treatment of cancer. Many efforts have been made to develop potent and selective PRMT5 inhibitors targeting either S-adenosyl methionine (SAM) pocket or substrate binding pocket. Here, we rationally designed a series of nucleoside derivatives incorporated with piperazine as novel PRMT5 inhibitors occupying both pockets.

Targeting Arginine Methyltransferase PRMT5 for Cancer Therapy: Updated Progress and Novel Strategies.

As a predominant type II protein arginine methyltransferase, PRMT5 plays critical roles in various normal cellular processes by catalyzing the mono- and symmetrical dimethylation of a wide range of histone and nonhistone substrates. Clinical studies have revealed that high expression of PRMT5 is observed in different solid tumors and hematological malignancies and is closely associated with cancer initiation and progression. Accordingly, PRMT5 is becoming a promising anticancer target and has received great attention in both the pharmaceutical industry and the academic community.

Discovery of a New-Generation S-Adenosylmethionine-Noncompetitive Covalent Inhibitor Targeting the Lysine Methyltransferase Enhancer of Zeste Homologue 2.

The first-generation enhancer of zeste homologue 2 (EZH2) inhibitors suffer from several limitations, such as high dosage, cofactor S-adenosylmethionine (SAM) competition, and acquired drug resistance. Development of covalent EZH2 inhibitors that are noncompetitive with cofactor SAM offers an opportunity to overcome these disadvantages. The structure-based design of compound (BBDDL2059) as a highly potent and selective covalent inhibitor of EZH2 is presented in this context.

Preparation and characterization of pure phase CdMnTe nanopowders by a hydrothermal route.

In this paper, CdMnTe nanopowders with uniform shapes were prepared through a facile hydrothermal route using 3-mercaptopropionic acid (MPA) as the stabilizer and modifier. The effects of different experimental conditions including Cd-to-MPA ratio, pH value and reaction temperature on the phase composition and formation mechanism of as-prepared nanopowders were studied. XRD results indicated as-prepared CdMnTe nanopowders were pure phase and had cubic sphalerite structure with high crystallinity.

Study on In-Doped CdMgTe Crystals Grown by a Modified Vertical Bridgman Method Using the ACRT Technique.

Cadmium-magnesium-telluride (CdMgTe) crystal was regarded as a potential semiconductor material. In this paper, an indium-doped CdMgTe ingot with 30 mm diameter and 120 mm length grown by a modified Bridgman method with excess Te condition was developed for room temperature gamma-ray detection. Characterizations revealed that the as-grown CdMgTe crystals had a cubic zinc-blende structure and additionally Te-rich second phase existed in the crystals.

Thermo-responsive molecularly imprinted sensor based on the surface-enhanced Raman scattering for selective detection of R6G in the water.

In this study, a novel SERS sensor was successfully prepared by combining a molecular imprinted technique (MIT) with a SERS technique to improve the selectivity of the traditional SERS technique. Moreover, a thermo-sensitive technique was also introduced to confer stimuli-responsive properties to the materials. In a typical procedure, the Ag nanoparticles (NPs) were reduced on the surface of ZnO nanorods (NRs), and the ZnO/Ag heterostructures were used as the SERS substrates.