| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T15739 | ||||
| Target Name | Cellular tumor antigen p53 (TP53) | ||||
| Type of Target |
Clinical trial |
||||
| Drug Potency against Target | NU-8231 | Drug Info | IC50 = 5300 nM | [1] | |
| NUTLIN-3 | Drug Info | IC50 = 1000 nM | [2] | ||
| Action against Disease Model | Mepacrine | Drug Info | The potential role of quinacrine in enhancing the effects of cisplatin was investigated in Hela, SCC-VII, SACC-83 and C6 cancer cell lines by using a CCK-8 assay for viability and a TUNEL assay for apoptosis. quinacrine markedly enhanced the cytotoxicity of cisplatin in a dose-dependant manner in the 4 cancer cell lines. The TUNEL assay showed that treating the 4 cell lines for 24 h with cisplatin plus quinacrine significantly increased the percentage of apoptotic cells compared to treatment with single-agent treatment or untreated controls. Western blot analysis showed that quinacrine plus cisplatin significantly down-regulated cIAP-1 and up-regulated Bax and cleaved caspase-3 expression in Hela and SCC-VII cells compared with single-agent treatment. | [3] | |
| References | |||||
| REF 1 | Small-molecule inhibitors of the MDM2-p53 protein-protein interaction based on an isoindolinone scaffold. J Med Chem. 2006 Oct 19;49(21):6209-21. | ||||
| REF 2 | Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein intera... J Med Chem. 2009 Nov 26;52(22):7044-53. | ||||
| REF 3 | Quinacrine enhances cisplatin-induced cytotoxicity in four cancer cell lines. Chemotherapy. 2010;56(2):127-34. | ||||
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