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A selective p53 activator and anticancer agent to improve colorectal cancer the...
Ramos, Helena; Soares, Maria I. L.; Silva, Joana; Raimundo, Liliana; Calheiros, Juliana; Gomes, Célia; Reis, Flávio; Monteiro, Filipe A.; Nunes, CláudiaImpairment 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...
A selective p53 activator and anticancer agent to improve colorectal cancer the...
Ramos, Helena; Soares, Maria I. L.; Silva, Joana; Raimundo, Liliana; Calheiros, Juliana; Gomes, Célia; Reis, Flávio; Monteiro, Filipe A; Nunes, CláudiaImpairment 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...
A selective p53 activator and anticancer agent to improve colorectal cancer the...
Ramos, Helena; Soares, Maria I. L.; Silva, Joana; Raimundo, Liliana; Calheiros, Juliana; Gomes, Célia; Reis, Flávio; Monteiro, Filipe A.; Nunes, CláudiaImpairment 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, Sara; Bosco, Bartolomeo; Loureiro, Joana B.; Ramos, Helena; Raimundo, Liliana; Soares, Joana; Nazareth, Nair; Barcherini, ValentinaHalf 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...
SLMP53-2 Restores Wild-Type-Like Function to Mutant p53 through Hsp70: Promisin...
Gomes, Sara; Bosco, Bartolomeo; Loureiro, Joana B.; Ramos, Helena; Raimundo, Liliana; Soares, Joana; Nazareth, Nair; Barcherini, ValentinaHalf of human cancers harbor <i>TP53</i> 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...