Davidovich, P; Aksenova, V; Petrova, V; Tentler, D; Orlova, D; Smirnov, S; Gurzhiy, V; ... Tribulovich, V; + view all Davidovich, P; Aksenova, V; Petrova, V; Tentler, D; Orlova, D; Smirnov, S; Gurzhiy, V; Okorokov, AL; Garabadzhiu, A; Melino, G; Barlev, N; Tribulovich, V; - view fewer (2015) Discovery of Novel Isatin-Based p53 Inducers. ACS Medicinal Chemistry Letters , 6 (8) pp. 856-860. 10.1021/acsmedchemlett.5b00011.

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Abstract

A series of isatin Schiff base derivatives were identified during in silico 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.

Type:	Article
Title:	Discovery of Novel Isatin-Based p53 Inducers
Location:	United States
DOI:	10.1021/acsmedchemlett.5b00011
Publisher version:	http://dx.doi.org/10.1021/acsmedchemlett.5b00011
Language:	English
Keywords:	MDM2, in silico, in vivo assay, isatin Mannich and Schiff bases, p53 activators, protein−protein interactions
UCL classification:	UCL UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Div of Medicine UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Div of Medicine > Wolfson Inst for Biomedical Research
URI:	https://discovery.ucl.ac.uk/id/eprint/1492346

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