Figure 1 from A Small Molecule Reacts with the p53 Somatic Mutant Y220C to Rescue Wild-type Thermal Stability
Year: 2025
Type: other
Abstract: Development of a covalent PhiKan083. A, Chemical structures of the carbazole series. B, 1 μmol/L p53 Y220C-CL was incubated with 10 μmol/L of the carbazole compounds at 4°C for 24 hours. Adduct formation was observed by LC/MS. C, HepG2 (p53WT/+) or Huh-7 (p53 Y220C/−) cells were treated with the indicated KG5 concentration for 1 hour at 37°C and target engagement was observed by gel shift following a copper click reaction with TAMRA-azide. D, Crystal structure of p53 Y220C-CL bound to KG3 at 2.4 Å resolution. E, Crystal structure of the p53 Y220C–PhiKan083 complex (Protein Data Bank 2VUK; ref. 8).
Authors: Keelan Z. Guiley, Kevan M. Shokat
Language: English
Subfield: Oncology
Field: Medicine
Domain: Health Sciences
Open Access status: gold
OpenAlex ID: W4417194343