title: Discovery of Novel Isatin-Based p53 Inducers
metadata.name: dc.contributor.author
metadata.value: Davidovich, P
metadata.lang: -
metadata.name: dc.contributor.author
metadata.value: Aksenova, V
metadata.lang: -
metadata.name: dc.contributor.author
metadata.value: Petrova, V
metadata.lang: -
metadata.name: dc.contributor.author
metadata.value: Tentler, D
metadata.lang: -
metadata.name: dc.contributor.author
metadata.value: Orlova, D
metadata.lang: -
metadata.name: dc.contributor.author
metadata.value: Smirnov, S
metadata.lang: -
metadata.name: dc.contributor.author
metadata.value: Gurzhiy, Vladislav V.
metadata.lang: -
metadata.name: dc.contributor.author
metadata.value: Okorokov, A L
metadata.lang: -
metadata.name: dc.contributor.author
metadata.value: Garabadzhiu, A
metadata.lang: -
metadata.name: dc.contributor.author
metadata.value: Melino, G
metadata.lang: -
metadata.name: dc.contributor.author
metadata.value: Barlev, N
metadata.lang: -
metadata.name: dc.contributor.author
metadata.value: Tribulovich, V
metadata.lang: -
metadata.name: dc.date.accessioned
metadata.value: 2016-05-06T13:02:27Z
metadata.lang: -
metadata.name: dc.date.available
metadata.value: 2016-05-06T13:02:27Z
metadata.lang: -
metadata.name: dc.date.issued
metadata.value: 2015-08-13
metadata.lang: -
metadata.name: dc.identifier
metadata.value: 10.1021/acsmedchemlett.5b00011
metadata.lang: -
metadata.name: dc.identifier.issn
metadata.value: 1948-5875
metadata.lang: -
metadata.name: dc.identifier.other
metadata.value: 10.1021/acsmedchemlett.5b00011
metadata.lang: -
metadata.name: dc.identifier.uri
metadata.value: http://hdl.handle.net/11701/2244
metadata.lang: -
metadata.name: dc.description.abstract
metadata.value: 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.
metadata.lang: en_GB
metadata.name: dc.language.iso
metadata.value: en
metadata.lang: en_GB
metadata.name: dc.publisher
metadata.value: American Chemichal Society
metadata.lang: en_GB
metadata.name: dc.relation.ispartofseries
metadata.value: ACS Medicinal Chemistry Letters;V. 6. Issue 8
metadata.lang: -
metadata.name: dc.title
metadata.value: Discovery of Novel Isatin-Based p53 Inducers
metadata.lang: en_GB
metadata.name: dc.type
metadata.value: Article
metadata.lang: en_GB
resources.filename: 2015_Davidovich_Med Chem.pdf
resources.url: https://dspace.spbu.ru/bitstream/11701/2244/1/2015_Davidovich_Med%20Chem.pdf
resources.format: Adobe PDF
resources.size: 1,66 MB