In order to characterize binding sites of insecticidal compounds on GABA gated chloride channel, new photoaffinity probe candidates based on 5e-t-butyl-2e-[4-（substituted-propynyl）phenyl]-1,3-dithiane for the noncom...In order to characterize binding sites of insecticidal compounds on GABA gated chloride channel, new photoaffinity probe candidates based on 5e-t-butyl-2e-[4-（substituted-propynyl）phenyl]-1,3-dithiane for the noncompetitive blocker （NCB） site of the γ-aminobutyric acid （GABA）-gated chloride channel were designed and synthesized, and their potency as an inhibitor on NCB was measured by 4＇-ethynyl-4-n-[2,3-^3H2]-propylbicycloorthobenzoate （^3H EBOB） assay. The synthesized compounds showed high inhibition activities with half maximum inhibition concentrations （IC50） of lower than 35 nmol/L and were very stable in binding conditions as well photoreacted quickly at 300 nm light. These new compounds are expected to be good photoaffinity labeling probes if radioisotope iodine is incorporated.展开更多
经5步反应、以9%的总收率合成了一种含生物素修饰和光亲和标记的异戊烯侧链功能探针分子,初步考察了反应条件下该探针分子与Saccharomyces cerevisiae AS 2.399粗蛋白的相互作用;生物素印迹分析结果表明,酵母中多种蛋白被探针分子修饰,...经5步反应、以9%的总收率合成了一种含生物素修饰和光亲和标记的异戊烯侧链功能探针分子,初步考察了反应条件下该探针分子与Saccharomyces cerevisiae AS 2.399粗蛋白的相互作用;生物素印迹分析结果表明,酵母中多种蛋白被探针分子修饰,为进一步开展化学蛋白组学研究奠定了基础.展开更多
文摘In order to characterize binding sites of insecticidal compounds on GABA gated chloride channel, new photoaffinity probe candidates based on 5e-t-butyl-2e-[4-（substituted-propynyl）phenyl]-1,3-dithiane for the noncompetitive blocker （NCB） site of the γ-aminobutyric acid （GABA）-gated chloride channel were designed and synthesized, and their potency as an inhibitor on NCB was measured by 4＇-ethynyl-4-n-[2,3-^3H2]-propylbicycloorthobenzoate （^3H EBOB） assay. The synthesized compounds showed high inhibition activities with half maximum inhibition concentrations （IC50） of lower than 35 nmol/L and were very stable in binding conditions as well photoreacted quickly at 300 nm light. These new compounds are expected to be good photoaffinity labeling probes if radioisotope iodine is incorporated.
