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Babak, Maria V.; Chong, Kai Ren; Rapta, Peter; Zannikou, Markella; Tang, Hui Min; Reichert, Lisa; Chang, Meng Rui; Kushnarev, Vladimir; Heffeter, Petra; Meier‐Menches, Samuel M.; Lim, Zhi Chiaw; Yap, Jian Yu; Casini, Angela; Balyasnikova, Irina V.; Ang, Wee Han

Interfering with Metabolic Profile of Triple‐Negative Breast Cancers Using Rationally Designed Metformin Prodrugs

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  • Media type: E-Article
  • Title: Interfering with Metabolic Profile of Triple‐Negative Breast Cancers Using Rationally Designed Metformin Prodrugs
  • Contributor: Babak, Maria V.; Chong, Kai Ren; Rapta, Peter; Zannikou, Markella; Tang, Hui Min; Reichert, Lisa; Chang, Meng Rui; Kushnarev, Vladimir; Heffeter, Petra; Meier‐Menches, Samuel M.; Lim, Zhi Chiaw; Yap, Jian Yu; Casini, Angela; Balyasnikova, Irina V.; Ang, Wee Han
  • Published: Wiley, 2021
  • Published in: Angewandte Chemie International Edition, 60 (2021) 24, Seite 13405-13413
  • Language: English
  • DOI: 10.1002/anie.202102266
  • ISSN: 1433-7851; 1521-3773
  • Origination:
  • Footnote:
  • Description: AbstractTriple‐negative breast cancer (TNBC) is the most aggressive subtype of breast cancer, characterized by an aberrant metabolic phenotype with high metastatic capacity, resulting in poor patient prognoses and low survival rates. We designed a series of novel AuIIIcyclometalated prodrugs of energy‐disrupting Type II antidiabetic drugs namely, metformin and phenformin. Prodrug activation and release of the metformin ligand was achieved by tuning the cyclometalated AuIIIfragment. The lead complex3metwas 6000‐fold more cytotoxic compared to uncoordinated metformin and significantly reduced tumor burden in mice with aggressive breast cancers with lymphocytic infiltration into tumor tissues. These effects was ascribed to3metinterfering with energy production in TNBCs and inhibiting associated pro‐survival responses to induce deadly metabolic catastrophe.