Title:Monofunctional Platinum (PtII) Compounds – Shifting the Paradigm in Designing New Pt-based Anticancer Agents
Volume: 23
Issue: 12
Author(s): Shu Xian Chong, Steve Chik Fun Au-Yeung, Kenneth Kin Wah To
Affiliation:
关键词:
顺铂，卡铂，奥沙利铂，铂类药物，单功能铂类药物。
摘要: Platinum (Pt)-based anticancer drugs, exemplified by cisplatin, are key components
in combination chemotherapy. However, their effective use is hindered by toxicity and
emergence of drug resistance. They bind to DNA and mainly form the Pt-GG diadduct, subsequently
leading to apoptosis to mediate cell death. On the other hand, the Pt drug –proteins
and –metabolites interactions, which involve the reaction between Pt and sulfur sites located
in protein side chains and important bionucleophiles (e.g., glutathione), are responsible for the toxicity and
drug resistance problem. Therefore, carefully designed coordinating ligands may provide the means of fine
tuning the electronic environment around the core Pt atom and allow the resulting Pt compounds to bind with
the DNA in a different manner. This may produce alternative cell death mechanisms in cancer cells, thereby
circumventing Pt resistance. This article reviewed the recent development in monofunctional Pt complexes
and their prospects in becoming a new generation of anticancer drugs.
