Journal
INORGANIC CHEMISTRY
Volume 53, Issue 15, Pages 7812-7814Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ic501509x
Keywords
-
Categories
Funding
- NIH [GM033309, NIH/NRSA 5T32GM7616-33]
Ask authors/readers for more resources
We report the synthesis and characterization of a bimetallic conjugate (RhPt) in which an oxaliplatin derivative is tethered to a rhodium metalloinsertor through an aminomalonate leaving group ligand. The complex interacts with DNA through metalloinsertion at a base pair mismatch followed by formation of a covalent Pt-DNA adduct. Characterization of RhPt in mismatch repair-deficient HCT1160 cells reveals increased cytotoxicity compared to cisplatin and oxaliplatin as well as relative to the unconjugated rhodium and platinum counterparts. Caspase and poly-ADP ribose polymerase inhibition assays indicate that RhPt induces apoptotic cell death. Inductively coupled plasma mass spectrometry (ICP-MS) experiments reveal that RhPt exhibits enhanced cellular uptake properties that contribute to its increased efficacy.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available