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Published August 4, 2014 | Supplemental Material + Published
Journal Article Open

Construction and Application of a Rh–Pt DNA Metalloinsertor Conjugate


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 HCT116O 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.

Additional Information

© 2014 American Chemical Society. ACS AuthorChoice. Received: June 24, 2014. Publication Date (Web): July 17, 2014. We are grateful for instrumentation made available by the Caltech Environmental Analysis Center.

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Supplemental Material - ic501509x_si_001.pdf


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August 20, 2023
October 26, 2023