Abstract:
:We report new anticancer prodrugs, platinum(IV) derivatives of oxaliplatin conjugated with valproic acid (VPA), a well-known drug having histone deacetylase inhibitory activity. Like most platinum(IV) derivatives, the cytotoxicity of the conjugates was lower in cell culture than that of oxaliplatin, but greater than those of its Pt(IV) derivative containing biologically inactive axial ligands in several cancer cell lines. Notably, these conjugates display activity in both cisplatin sensitive- and resistant tumor cells capable of both markedly enhanced accumulation in tumor cells and acting in a dual threat manner, concurrently targeting histone deacetylase and genomic DNA. These results demonstrate the dual targeting strategy to be a valuable route to pursue in the design of platinum agents which may be more effective in cancer types that are typically resistant to therapy by conventional cisplatin. Moreover, platinum(IV) derivatives containing VPA axial ligands seem to be promising dual-targeting candidates for additional preclinical studies.
journal_name
J Inorg Biochemjournal_title
Journal of inorganic biochemistryauthors
Novohradsky V,Zerzankova L,Stepankova J,Vrana O,Raveendran R,Gibson D,Kasparkova J,Brabec Vdoi
10.1016/j.jinorgbio.2014.07.004subject
Has Abstractpub_date
2014-11-01 00:00:00pages
72-9eissn
0162-0134issn
1873-3344pii
S0162-0134(14)00194-9journal_volume
140pub_type
杂志文章abstract::An iron porphycene, a structural isomer of iron porphyrin, with trifluoromethyl groups at the peripheral position of the framework was incorporated into sperm whale apomyoglobin. The prepared myoglobin shows the higher O(2) affinity than the native protein. However, the oxygen affinity of the reconstituted myoglobin i...
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journal_title:Journal of inorganic biochemistry
pub_type: 杂志文章,评审
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journal_title:Journal of inorganic biochemistry
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journal_title:Journal of inorganic biochemistry
pub_type: 杂志文章,评审
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