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P53 activator APR-246

A quinuclidinone derivative that targets the p53 protein with potential antineoplastic activity. The p53 activator APR-246 refolds/reactivates the p53 protein, which may lead to an induction of cell cycle arrest or apoptosis in tumour cells. This agent may work synergistically with other antineoplastic agents. p53, a tumour suppressor and transcription factor normally activated upon DNA damage, is mutated or absent in various cancer cell types and plays a key role in DNA repair and the induction of apoptosis.

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