Platinum(II)-based compounds form stable coordination complexes with a variety of biomolecules. Recently we have investigated the use of cis-[Pt(2-azidopropane-1,3-diamine)Cl2] (1,3-ADAPPt) as a click-functionalized reagent for potential isolation, purification, and identification of Pt(II) biological targets. Upon binding to a folded model DNA hairpin oligonucleotide, this Pt(II) derivative reveals an unequal distribution of structural isomers. Populations of Pt-bound DNA complex isomers, resolved by reverse phase HPLC, are biased by the conformation of the azide in the context of duplex DNA. Current efforts are focused on understanding the conformational bias to improve both Pt binding and click reaction rates and yields. ADAPPt is also being utilized for in vivo studies such as cellular imaging of Pt localization in HeLa cells and extraction of Pt-bound RNA and DNA from S. cerevisiae and HeLa cells followed by post-treatment fluorescent labeling. These efforts will ultimately streamline our approach in using techniques such as high throughput sequencing and proteomics to identify Pt(II) binding sites in biomolecules.

<i>cis</i>-[Pt(2-azidopropane-1,3-diamine)Cl<sub>2</sub>], (1,3-ADAPPt), a clickable derivative for use in post-treatment labeling of Pt(II) targets

248th National Meeting (2014)

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cis-[Pt(2-azidopropane-1,3-diamine)Cl2], (1,3-ADAPPt), a clickable derivative for use in post-treatment labeling of Pt(II) targets

cis-[Pt(2-azidopropane-1,3-diamine)Cl₂], (1,3-ADAPPt), a clickable derivative for use in post-treatment labeling of Pt(II) targets