TP53 inhibitor PFTα increases the sensitivity of arsenic trioxide in TP53 wildtype tumor cells was written by Wang, Haiwei;Wang, Xinrui;Xu, Liangpu;Zhang, Ji. And the article was included in FEBS Open Bio in 2022.Electric Literature of C16H19BrN2OS The following contents are mentioned in the article:
Arsenic trioxide (ATO) has been shown to be effective in treating acute promyelocytic leukemia. TP53 mutated/null tumor cells are more sensitive to ATO treatment compared to tumor cells carrying wildtype TP53 gene copies. However, it is unclear whether TP53 inhibitors can increase the sensitivity of TP53 wildtype tumor cells to ATO. Here we show that breast, colon, and lung cancer cell lines with mutated/null TP53 are more sensitive to ATO-induced cell growth inhibition than cells with wildtype TP53. Moreover, inhibition of TP53 by a TP53 inhibitor, PFTα, increased the ATO sensitivity of TP53 wildtype tumor cells, coincident with ATO-induced cell growth arrest and cell apoptosis. Furthermore, combined treatment with ATO and PFTα synergistically inhibited tumor growth in mouse xenografts in vivo. Through microarray transcriptional anal., we found that ATO-regulated genes were associated with TP53 and cell cycle signaling pathways. Cotreatment with PFTα enhanced ATO-induced dynamic transcriptional changes. Overall, our results provide evidence for using TP53 chem. inhibitors to enhance the ATO-mediated therapeutic response against TP53 wildtype tumor cells. This study involved multiple reactions and reactants, such as 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2Electric Literature of C16H19BrN2OS).
2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. Thiazole is a versatile building block for the construction and lead generation of new drug discoveries. Numerous diazole-based compounds are in clinical use as anticancer, antileukemic, antiinflammatory, antiviral, antifungal, antirheumatic, immunomodulator, and antiparasitic agents.Electric Literature of C16H19BrN2OS
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica