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A selective p53 activator and anticancer agent to improve colorectal cancer the...

Ramos, H; Soares, MIL; Silva, J; Raimundo, L; Calheiros, J; Gomes, C; Reis, F; Monteiro, FA; Nunes, C; Reis, S; Bosco, B; Piazza, S; Domingues, L

Impairment of the p53 pathway is a critical event in cancer. Therefore, reestablishing p53 activity has become one of the most appealing anticancer therapeutic strategies. Here, we disclose the p53-activating anticancer drug (3S)-6,7-bis(hydroxymethyl)-5-methyl-3-phenyl-1H,3H-pyrrolo[1,2-c]thiazole (MANIO). MANIO demonstrates a notable selectivity to the p53 pathway, activating wild-type (WT)p53 and restoring W...


SLMP53-2 restores wild-type-like function to mutant p53 through hsp70: Promisin...

Gomes, S; Bosco, B; Loureiro, JB; Ramos, H; Raimundo, L; Soares, J; Nazareth, N; Barcherini, V; Domingues, L; Oliveira, C; Bisio, A; Piazza, S

Half of human cancers harbor TP53 mutations that render p53 inactive as a tumor suppressor. In these cancers, reactivation of mutant p53 (mutp53) through restoration of wild-type-like function constitutes a valuable anticancer therapeutic strategy. In order to search for mutp53 reactivators, a small library of tryptophanol-derived oxazoloisoindolinones was synthesized and the potential of these compounds as mut...


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