Table 1.
Summary of p53-reactivating compounds discussed in the text.
| Reactivators—p53 Cys-Targeting |
Mutations in p53 | Mechanism of Action | Ref. |
|---|---|---|---|
| APR-246 (PRIMA-1MET) Quinuclidinone |
R175H; R273H; D259Y/K286E; K286E; S241F; R273C; P223L/V274F |
Michael Addition | [84,86,87,88,89,90,91,92,93,94] |
| CP-31398 Styrylquinazoline |
V173A; S241F; R249S; R273H |
Michael Addition | [95,96,97,98] |
| HO-3867 Diarylidenyl piperidone curcumin analogue |
Y163H; R175H; H193R; L194F; Y205F; P223L/V274F; C238Y; N239D; S241F; G245S; G245V; M246I; R248Q; R248W; R249S; R273H; C277F; R280K; E285K | Michael Addition | [99,100] |
| KSS-9 Piperlongumine derivative |
R175H | Michael Addition | [101] |
| MIRA-1 Maleimide |
R175H; P176Y/R248W; R248Q; R248W; R273H; R273H/P309S; R280K; R282W | Michael Addition | [102] |
| PK11007 Sulfonylpyrimidine |
Y220; V143A | Nucleophilic aromatic substitution | [103] |
| STIMA-1 2-vinylquinazolin-4-(3H)-one |
R175H; R273H | Michael Addition | [95] |