Current chemotherapeutic agents, specifically platinum-based drugs, are highly effective at treating a variety of cancers, however, these drugs have several drawbacks, such as systemic toxicity and development of resistant forms of the disease. Chemotherapeutic agents that have different mechanisms of action can help overcome some of the issues associated with platinum-based drugs. Complexes of the element rhenium have recently been shown to possess promising anticancer activity via mechanisms of action that are distinct from the conventional metal-based drugs cisplatin and carboplatin. In this study, we have found that rhenium complexes bearing an axial isonitrile ligand possess potent anticancer activity in both wild-type and cisplatin-resistant cancer cell lines. These rhenium complexes induce apoptosis by targeting the endoplasmic reticulum and eliciting the unfolded protein response. This stress response is different from both previously reported metal-based complexes, as well as the clinically approved ER-stress inducing compounds. These results illustrate the potential of rhenium isonitrile complexes as potent anticancer agents.<br/>

Rhenium isonitrile complexes induce unfolded protein response-mediated apoptosis in cancer cells

2019 Fall National Meeting

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