Etomoxir as a Promiscuous Chemoproteomic Probe.

Primary hepatocytes from WT or Pex5KO mouse livers were treated with 100uM clickable etomoxir analogues and the proteins bound to etomoxir were pulled down and identified. The small molecule inhibitor etomoxir has been used for many years as a specific inhibitor of Cpt1 but these data show that etomoxir binds a large array of proteins and is not appropriate as a tool for evaluating the biological effects of fatty acid oxidation. Primary hepatocytes were treated with 100uM clickable etomoxir analogues and the proteins bound to etomoxir were pulled down and identified. The small molecule inhibitor etomoxir has been used for many years as a specific inhibitor of Cpt1 but these data show that etomoxir binds a large array of proteins and is not appropriate as a tool for evaluating the biological effects of fatty acid oxidation.

以野生型（Wild Type, WT）或Pex5基因敲除（Pex5KO）小鼠肝脏来源的原代肝细胞（primary hepatocytes）为材料，使用100μM可点击化学修饰的依托莫司（etomoxir）类似物处理细胞，随后通过亲和拉下实验富集并鉴定与依托莫司结合的蛋白质。
小分子抑制剂依托莫司多年来一直被作为肉碱棕榈酰转移酶1（Carnitine Palmitoyltransferase 1, Cpt1）的特异性抑制剂使用，但本实验数据显示，依托莫司可结合大量蛋白质，并不适合作为评估脂肪酸氧化生物学效应的研究工具。
以野生型或Pex5基因敲除小鼠肝脏来源的原代肝细胞为材料，使用100μM可点击化学修饰的依托莫司类似物处理细胞，随后通过亲和拉下实验富集并鉴定与依托莫司结合的蛋白质。
小分子抑制剂依托莫司多年来一直被作为肉碱棕榈酰转移酶1的特异性抑制剂使用，但本实验数据显示，依托莫司可结合大量蛋白质，并不适合作为评估脂肪酸氧化生物学效应的研究工具。