Dimeric quinacrines as chemical tools to identify PPT1, a new regulator of autophagy in cancer cells.
Dimeric quinacrines as chemical tools to identify PPT1, a new regulator of autophagy in cancer cells.
复制标题
DOI：
10.1080/23723556.2017.1395504
复制
发表时间：
2018
影响因子：
2.1
通讯作者：
Winkler JD
中科院分区：
文献类型：
--
作者：
Nicastri MC;Rebecca VW;Amaravadi RK;Winkler JD
DQ 661是一种新型的二聚奎纳克林，通过特异性靶向蛋白质-棕榈酰硫酯酶1（PPT 1）影响多种溶酶体功能（自噬和巨胞饮）和mTORC 1（雷帕霉素的机械靶标）活性。DQ 661在免疫活性小鼠癌症模型中具有体内活性，并构成了用于研究癌症中溶酶体功能和治疗抗性的新工具化合物。
DQ661 is a novel dimeric quinacrine that affects multiple lysosomal functions (autophagy and macropinocytosis) and mTORC1 (mechanistic target of rapamycin) activity by specifically targeting protein-palmitoyl thioesterase 1 (PPT1). DQ661 has in vivo activity in immunocompetent mouse models of cancer, and constitutes a new tool compound for the study of lysosomal function in cancer and therapeutic resistance.