PK11007 is a thiol-reactive anticancer agent that stabilizes wild type and mutant p53 through selective alkylation of two surface cysteines without interfering with its DNA binding.
PK11007 is a thiol-reactive anticancer agent that stabilizes wild type and mutant p53 through selective alkylation of two surface cysteines without interfering with its DNA binding. Additionally independently from p53, PK11007 impairs reactive oxygen species (ROS) detoxification in a number of mutant p53 cancer cells. PK11007 exhibits anticancer activity in number of cancer cell lines while shoving low cytotoxicity toward normal cells.
Proceedings of the National Academy of Sciences of the United States of America, 113(36), E5271-E5280 (2016-08-24)
The tumor suppressor p53 has the most frequently mutated gene in human cancers. Many of p53's oncogenic mutants are just destabilized and rapidly aggregate, and are targets for stabilization by drugs. We found certain 2-sulfonylpyrimidines, including one named PK11007, to
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