Weidmann, Alyson G. and Barton, Jacqueline K. (2014) Construction and Application of a Rh–Pt DNA Metalloinsertor Conjugate. Inorganic Chemistry, 53 (15). pp. 7812-7814. ISSN 0020-1669. PMCID PMC4123934. https://resolver.caltech.edu/CaltechAUTHORS:20140721-085331031
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Abstract
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.
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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. | |||||||||||||||
Issue or Number: | 15 | |||||||||||||||
PubMed Central ID: | PMC4123934 | |||||||||||||||
Record Number: | CaltechAUTHORS:20140721-085331031 | |||||||||||||||
Persistent URL: | https://resolver.caltech.edu/CaltechAUTHORS:20140721-085331031 | |||||||||||||||
Official Citation: | Construction and Application of a Rh–Pt DNA Metalloinsertor Conjugate Alyson G. Weidmann and Jacqueline K. Barton Inorganic Chemistry 2014 53 (15), 7812-7814 | |||||||||||||||
Usage Policy: | No commercial reproduction, distribution, display or performance rights in this work are provided. | |||||||||||||||
ID Code: | 47355 | |||||||||||||||
Collection: | CaltechAUTHORS | |||||||||||||||
Deposited By: | Tony Diaz | |||||||||||||||
Deposited On: | 21 Jul 2014 19:13 | |||||||||||||||
Last Modified: | 03 Oct 2019 06:52 |
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