Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 6, Issue 8, Pages 856-860Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.5b00011
Keywords
in silico; isatin Mannich and Schiff bases; p53 activators; in vivo assay; protein-protein interactions; MDM2
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Funding
- Ministry of Education and Science of Russia [11.G34.31.0069, 14.B25.31.0013, 14.132.21.1334]
- BBSRC [BB/E019862/1]
- BBSRC [BB/E019862/1] Funding Source: UKRI
- MRC [MC_U132670600] Funding Source: UKRI
- Biotechnology and Biological Sciences Research Council [BB/E019862/1] Funding Source: researchfish
- Medical Research Council [MC_U132670600] Funding Source: researchfish
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A series of isatin Schiff base derivatives were identified during in silk screening of the small molecule library for novel activators of p53. The compounds selected based on molecular docking results were further validated by a high-content screening assay using U2OS human osteosarcoma cells with an integrated EGFP-expressing p53-dependent reporter. The hit compounds activated and stabilized p53, as shown by Western blotting, at higher rates than the well-known positive control Nutlin-3. Thus, the p53-activating compounds identified by this approach represent useful molecular probes for various cancer studies.
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