Litcius/Paper detail

Elucidating the Multimodal Anticancer Mechanism of an Organometallic Terpyridine Platinum(II) N-Heterocyclic Carbene Complex against Triple-Negative Breast Cancer In Vitro and In Vivo

Jing‐Jing Zhang, Qi-Jie Xu, Claudia Schmidt, Mohamed A. Abu el Maaty, Jinlin Song, Chunqiu Yu, Jun Zhou, Kang Han, Hao Sun, Angela Casini, Ingo Ott, Stefan Wölfl

2023Journal of Medicinal Chemistry28 citationsDOI

Abstract

Treatment of triple-negative breast cancer (TNBC) has long been a medical challenge because of the lack of effective therapeutic targets. Targeting lipid, carbohydrate, and nucleotide metabolism pathways has recently been proven as a promising option in view of three heterogeneous metabolic-pathway-based TNBC subtypes. Here, we present a multimodal anticancer platinum(II) complex, named Pt(II)caffeine, with a novel mode of action involving simultaneous mitochondrial damage, inhibition of lipid, carbohydrate, and nucleotide metabolic pathways, and promotion of autophagy. All these biological processes eventually result in a strong suppression of TNBC MDA-MB-231 cell proliferation both in vitro and in vivo . The results indicate that Pt(II)caffeine, influencing cellular metabolism at multiple levels, is a metallodrug with increased potential to overcome the metabolic heterogeneity of TNBC.

Topics & Concepts

ChemistryTriple-negative breast cancerIn vivoIn vitroCancer researchAutophagyBiochemistryPharmacologyBreast cancerCancerApoptosisBiologyGeneticsClick Chemistry and ApplicationsRNA modifications and cancerN-Heterocyclic Carbenes in Organic and Inorganic Chemistry