Functional screening and rational design of compounds targeting GPR132 to treat diabetes.

Chronic inflammation due to islet-residing macrophages plays key roles in the development of type 2 diabetes mellitus. By systematically profiling intra-islet lipid-transmembrane receptor signalling in islet-resident macrophages, we identified endogenous 9(S)-hydroxy-10,12-octadecadienoic acid-G-protein-coupled receptor 132 (GPR132)-Gi signalling as a significant contributor to islet macrophage reprogramming and found that GPR132 deficiency in macrophages reversed metabolic disorders in mice fed a high-fat diet. The cryo-electron microscopy structures of GPR132 bound with two endogenous agonists, N-palmitoylglycine and 9(S)-hydroxy-10,12-octadecadienoic acid, enabled us to rationally design both GPR132 agonists and antagonists with high potency and selectivity through stepwise translational approaches.

Electrochemical mineralization of iron-tannate stain on HAp and bovine enamel-A non-peroxide approach.

Prolonged treatments for the destaining of teeth using high concentrations of hydrogen peroxide may cause secondary unwanted effects such as tooth hypersensitivity and gingival irritation. Hence, it is aimed to develop a non-peroxide-based method to oxidize iron-tannate (Fe-TA) stained hydroxyapatite (HAp) and bovine enamel (BE) samples. Constant current electrolysis (CCE) experiments were carried out on Pt working electrode in aqueous NaCl, KCl and KI solutions at discrete concentrations under continuous experiment and a non-continuous experiment.

The novel cereblon modulator CC-885 inhibits mitophagy via selective degradation of BNIP3L.

Mitophagy is a degradative pathway that mediates the degradation of the entire mitochondria, and defects in this process are implicated in many diseases including cancer. In mammals, mitophagy is mediated by BNIP3L (also known as NIX) that is a dual regulator of mitochondrial turnover and programmed cell death pathways. Acute myeloid leukemia (AML) cells with deficiency of BNIP3L are more sensitive to mitochondria-targeting drugs.

TGF-3 Induces Autophagic Activity by Increasing ROS Generation in a NOX4-Dependent Pathway.

Higher concentrations of reactive oxygen species (ROS) have been associated with epithelial cell damage, cell shedding, and airway hyperresponsiveness. Previous studies have indicated that transforming growth factor-beta (TGF-) mediates ROS production and NADPH oxidase (NOX) activity. In our previous study, we also observed that TGF-3 increases mucus secretion in airway epithelial cells in an autophagy-dependent fashion.

[Study on the estrogen derivative marked by CdTe quantum dots].

Water-soluble CdTe quantum dots (QDs) stabilized by thioglycolic acid (TGA) with high quantum yield were synthesized. And the small biomolecule 17beta-amino-estradiol was marked successfully by CdTe QDs. The analysis of UV-Vis spectroscopy, fluorescence spectroscopy, infrared spectroscopy and inverted microscope photographs showed that the surface carboxyl of CdTe quantum dots conjugated with the amino of 17beta-amino-estradiol through the activation of N-hydroxysuccinimide.

[Preparation and evaluation of a new xenogenic implant material].

Objective: To prepare a new xenogenic material using patented biochemical techniques for tissue disposal and investigate its possibility to be used as implant materials.

Methods: The xenogenic implant materials were prepared by treatment of fresh porcine tendon with epoxy cross-linking fixation, antigen minimization procedures, mechanical enhancement by protein molecule modification and surface treatments. Histological and scanning electron microscopic observations were conducted, and physicochemical property assessment was carried out to determine the mechanical properties, protein contents, polyepoxy compound residual and stability of the material.

[Effective expression of ribonuclease-onconase in Escherichia coli and assaying its cytotoxic potential].

Onconase, a ribonuclease purified from Rana pipiens oocytes, has cytotoxic activity against several tumor cell lines in vitro. With the characteristic of containing four pairs of disulfide bonds internal and N terminal sequence attributing mostly to its biological functions, it is difficult to obtain the active Onconase from Escherichia coli expression system with normal strategy. Here, we fused the cDNA coding for Onconase in frame with the pelB signal sequence in pET22b(+) expression vector.