Developing an Anticancer Platinum(II) Compound Based on the Uniqueness of Human Serum Albumin

J Med Chem. 2023 Apr 27;66(8):5669-5684. doi: 10.1021/acs.jmedchem.3c00001. Epub 2023 Apr 18.

Abstract

To develop the next-generation Pt drug with remarkable activity and low toxicity to maximally inhibit tumor growth, we optimized a Pt(II) thiosemicarbazone compound (C4) with remarkable cytotoxicity to SK-N-MC cells and then constructed a new human serum albumin-C4 (HSA-C4) complex delivery system. The in vivo results showed that C4 and the HSA-C4 complex have remarkable therapeutic efficiency and almost no toxicity; they induced apoptosis and inhibited tumor angiogenesis. This system showed potential as a practical Pt drug. This study could pave the way for developing next-generation dual-targeted Pt drugs and achieving their targeting therapy for cancer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents* / pharmacology
  • Cell Line, Tumor
  • Drug Delivery Systems / methods
  • Humans
  • Neoplasms* / drug therapy
  • Platinum
  • Serum Albumin, Human

Substances

  • Serum Albumin, Human
  • Platinum
  • Antineoplastic Agents