Mechanistic studies of the anticancer activity of an octahedral hexanuclear Pt(II) cage
The cellular response evoked by a hexanuclear platinum complex, Pt6L4(1), is reported. Compound 1, a 3-nm octahedral cage formed by self-assembly of six Pt(II) centers and four 2,4,6-tris(4-pyridyl)-1,3,5-triazine ligands (L), exhibits promising in vitro potency against a panel of human cancer cell...
| Main Authors: | , , , , , , |
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| Other Authors: | |
| Format: | Article |
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Elsevier
2018
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| Online Access: | http://hdl.handle.net/1721.1/119635 https://orcid.org/0000-0003-3383-0118 https://orcid.org/0000-0002-2693-4982 |
| Summary: | The cellular response evoked by a hexanuclear platinum complex, Pt6L4(1), is reported. Compound 1, a 3-nm octahedral cage formed by self-assembly of six Pt(II) centers and four 2,4,6-tris(4-pyridyl)-1,3,5-triazine ligands (L), exhibits promising in vitro potency against a panel of human cancer cell lines. Unlike classical platinum-based anticancer agents, 1 interacts with DNA in a non-covalent, intercalative manner and promotes DNA condensation. In cancer cells, 1 induces DNA damage, upregulates p53, its phosphorylated form phospho-p53 and its downstream effector, p21, as well as both apoptosis and senescence. Keywords: Self-assembly; Cage; Anticancer; DNA damage |
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