Article
Covalent drug rescue of multiple p53 mutants by stabilizing vinyl sulfone fragments hints to a specific refolding mechanism for R282W.
Protein science : a publication of the Protein Society - 1 Jun 2026
Stahlecker Jason, Klett Theresa, Spiegel Robert, Schwer Martin, Mier Finn, Aldea Sven, Masberg Benedikt, Lämmerhofer Michael, Stehle Thilo, Böckler Frank M
Abstract excerpt
The tumor suppressor protein p53 plays a crucial role in cell cycle regulation. In approximately 50% of all tumors, mutations in p53 are observed. Although the top hot spot mutations impair DNA binding, other mutations affect the thermal stability of the protein, leading to its rapid denaturation in physiological conditions. Previously, we have identified VS004, a vinyl sulfone containing fragment that stabilized...
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