METHODS AND COMPOSITIONS FOR RESTORING CONFORMATIONAL STABILITY OF A PROTEIN OF THE p53 FAMILY

摘要

The invention provides pharmaceutical non-peptidic organic compounds capable of interacting with a functionally defective form of a mutant or a wild-type tumor suppressor protein of the p53 family (such as p53, p63 or p73). The interaction allows stabilization or folding of the protein in a functional conformation, thereby restoring all or part of its wild-type normal activity. More particularly said compounds interact with the DNA binding domain of p53 family proteins, are acridine, quinoline, quinazoline or phenothiazine derivatives, and are used in cancer therapy. Also provided are methods for screening such pharmacological compounds.