There is a compelling need to discover type II inhibitors targeting the unique DFG-out inactive kinase conformation since they are likely to possess greater potency and selectivity relative to traditional type I inhibitors. Using a known inhibitor, such as a currently available and approved drug or inhibitor, as a template to design new drugs via computational de novo design is helpful when wor...

Polar extracts of Tapirira guianensis Aubl. were prepared for evaluation biological activities. Identification and quantification phenolic compounds, antioxidant activity, inhibition acetylcholinesterase enzyme antifungal potential performed in all extracts. High contents total phenols detected the ethanolic aqueous leaves (237.10±5.39 mg EAG/g 346.46±5.67 EAG) respectively. The same had a free...

Changes in acetylcholinesterase activity in blood and some organs of rats after intoxication with sarin, soman, VX, and 2-dimethylaminoethyl-(dimethylamido)-phosphonofluoridate (GV), in doses of roughly 2 x LD50 given intramuscularly, were obtained from published data and by experiment. The time course of inhibition of acetylcholinesterase in blood, regions of brain, and diaphragm and the occur...