蛋白降解靶向嵌合体(PROTAC)技术是目前小分子药物研发领域最火热的技术之一。它颠覆了传统药物化学中“占位驱动 (occupancy driven)”的开发理念,借助内源性的泛素蛋白酶体系统有效地特异性降解致病蛋白,尤其是“不可成药(undruggable)”靶点。如此优秀的技术,不但让国内外众多制药巨头和Biotech公司趋之若鹜,更为科学家们打开了新世界的大门。中国科学院司龙龙课题组刚刚在Nature子刊发表了基于PROTAC技术的流感疫苗[1],沈阳药科大学陈丽霞和李华团队又创造性地将这项技术引入到了中药研究领域,在Acta Pharmaceutica Sinica B(APSB)发表了题为“PROTAC Technology as a Novel Tool to Identify the Target of Lathyrane Diterpenoids”的研究论文 [2]。
SummaryImpurities and contaminants in the material used in the production of Li-ion batteries can havecatastrophic impacts on the finished products. As such, monitoring of the quality and cleanliness ofmaterials throughout the production process is essential if contaminants are to be found and theirsources controlled. This monitoring must start with the raw materials produced at the mine andcontinue through to the final battery grade powders.This application note demonstrates a scanning electron microscopy (SEM) based solution forautomatic detection and identification of impurities in battery raw material powders. By takingsamples at different steps of the production process it is possible to identify where contaminants areintroduced thereby allowing sources to be identified and solutions developed.
The discovery of potent benzimidazole stearoyl-CoA desaturase (SCD1) inhibitors by ligand-based virtual screening is described. ROCS 3D-searching gave a favorable chemical motif that was subsequently optimized to arrive at a chemical series of potent and promising SCD1 inhibitors. In particular, compound SAR224 was selected for further pharmacological profiling based on favorable in vitro data. After oral administration to male ZDF rats, this compound significantly decreased the serum fatty acid desaturationindex, thus providing conclusive evidence for SCD1 inhibition in vivo by SAR224.