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1. Dimeric quinacrines as chemical tools to identify PPT1, a new regulator of autophagy in cancer cells

Author

Jeffrey D. Winkler, Vito W. Rebecca, Ravi K. Amaravadi, and Michael C. Nicastri

Subjects
0301 basic medicine, autophagy, Cancer Research, macropinocytosis, Regulator, mTORC1, PPT1, 03 medical and health sciences, Lysosome, medicine, Mechanistic target of rapamycin, biology, Chemistry, Autophagy, Cancer, medicine.disease, 3. Good health, Cell biology, Author's Views, 030104 developmental biology, medicine.anatomical_structure, Cancer cell, mTOR, lysosome, biology.protein, Molecular Medicine
Abstract

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.

Published
2017

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