Platinum-based drugs have been a mainstay of anticancer chemotherapies since the late 1970s. A persistent challenge with these drugs is their overall toxicity, largely driven by non-specific binding of Pt to cellular targets in non-cancerous cells. Despite the determined push to develop the next generation of Pt drugs, within the last few decades only a small number of new drugs have demonstrated improved efficacy in any clinical trials, and none have received regulatory approval in the USA. Most of these efforts have focused on either developing non-classical Pt complexes with alternative binding modes, or on alternative delivery methods. Towards the latter aim, we have explored tethering Pt compounds to small-molecule phospholipid metabolite precursors. Cancerous cells are characterized by numerous metabolic re-programming events. Many of these phenotypes, such as increased reliance on external uptake of metabolic precursors, have increasingly been utilized as avenues for enhanced, targeted drug uptake. We have investigated the cellular reactivity of a Pt compound conjugated to a choline derivative, with the aim of “hijacking” lipogenic pathways for enhanced cancer targeting of Pt. Currently, we have demonstrated target binding to DNA in vitro, and are investigating reactivity in cell models.

Synthesis and biochemical characterization of a Pt anticancer compound tethered to a lipogenic metabolic precursor

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.