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

  • Mol Cell Oncol. 2017 Nov 30;5(1):e1395504. doi: 10.1080/23723556.2017.1395504.
Michael C Nicastri  1 ,  Vito W Rebecca  2 ,  Ravi K Amaravadi  2  3 ,  Jeffrey D Winkler  1  3
Affiliations
  • 1. Department of Chemistry; University of Pennsylvania, Philadelphia, PA.
  • 2. Department of Medicine; University of Pennsylvania, Philadelphia, PA.
  • 3. Abramson Cancer Center; University of Pennsylvania, Philadelphia, PA.
PMID: 29404393 DOI: 10.1080/23723556.2017.1395504
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.

Keywords
PPT1; autophagy; lysosome; mTOR; macropinocytosis.
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