Selective targeting of mutant adenomatous polyposis coli (APC) in colorectal cancer

@article{Zhang2016SelectiveTO,
  title={Selective targeting of mutant adenomatous polyposis coli (APC) in colorectal cancer},
  author={Lu Zhang and Panayotis C. Theodoropoulos and Ugur Eskiocak and Wentian Wang and Young Ah Moon and Bruce A. Posner and Noelle Sevilir Williams and Woodring E Wright and Sung Bum Kim and Deepak Nijhawan and Jef K. De Brabander and Jerry W Shay},
  journal={Science Translational Medicine},
  year={2016},
  volume={8},
  pages={361ra140-361ra140}
}
Mutations in the adenomatous polyposis coli (APC) gene are common in colorectal cancer (CRC), and more than 90% of those mutations generate stable truncated gene products. We describe a chemical screen using normal human colonic epithelial cells (HCECs) and a series of oncogenically progressed HCECs containing a truncated APC protein. With this screen, we identified a small molecule, TASIN-1 (truncated APC selective inhibitor–1), that specifically kills cells with APC truncations but spares… CONTINUE READING

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