单功能铂（PtII）化合物–铂抗癌药物设计的新范例的转变

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.

Cite this article as:

Shu Xian Chong, Steve Chik Fun Au-Yeung, Kenneth Kin Wah To , Monofunctional Platinum (PtII) Compounds – Shifting the Paradigm in Designing New Pt-based Anticancer Agents, Current Medicinal Chemistry 2016; 23 (12) . https://dx.doi.org/10.2174/0929867323666160311114509