Title of article
Novel Isatin-based activator of p53 transcriptional functions in tumor cells
Author/Authors
Mirgayazova ، Regina Kazan Federal University , Khadiullina ، Raniya Kazan Federal University , Mingaleeva ، Rimma Kazan Federal University , Chasov ، Vitaly Kazan Federal University , Gomzikova ، Marina Kazan Federal University , Garanina ، Ekaterina Kazan Federal University , Rizvanov ، Albert Kazan Federal University , Bulatov ، Emil Kazan Federal University
Pages
10
From page
119
To page
128
Abstract
Bioinorganic medicinal chemistry remains a hot field for research aimed at developing novel anti-cancer treatments. Discovery of metal complexes as potent antitumor chemotherapeutics such as cisplatin led to a significant shift of focus toward organometallic/ bioinorganic compounds containing transition metals and their chelates as novel scaffolds for drug discovery. In that way, transition metal complexes coordinated to essential biological scaffolds represent a highly promising class of compounds for design of novel target-specific therapeutics. Here, we report novel data on p53 activating Isatin-based Cu(II) complex exhibiting cytotoxic properties towards HCT116 and MCF7 tumor cell lines, as confirmed by cell viability assay and flow cytometry analysis of apoptosis. Furthermore, putative p53-mediated mechanism of action of this compound is supported by quantitative analysis of TP53, MDM2 and PUMA genes expression, as well as luciferase-based p53 pathway activation assay. Multiplex immunoassay analysis of inflammatory markers revealed potential modulation of several cytokines and chemokines.
Keywords
p53 , Transcriptional activity , Isatin , Schiff base , Metal complex , Tumor cells
Journal title
Molecular Biology Research Communications
Serial Year
2019
Journal title
Molecular Biology Research Communications
Record number
2474003
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