研究动态
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铂糖基共轭物:针对癌症治疗的“甜蜜子弹”?

Platinum glycoconjugates: "Sweet bullets" for targeted cancer therapy?

发表日期:2023 Feb
作者: Shreyas P Vaidya, Malay Patra
来源: CURRENT OPINION IN CHEMICAL BIOLOGY

摘要:

癌症是一种以异常细胞不受控制增生为特征的疾病,是全球死亡率和发病率的主要原因。细胞毒性化疗,特别是铂类药物化疗,仍然是临床治疗癌症的主要手段。尽管小分子化学药物取得了令人瞩目的成功,但也存在一些严重缺点。缺乏癌症选择性和随之而来的副作用影响了这些药物的治疗潜力。糖蛋白共轭已成为赋予细胞毒性药剂选择性和改善药物动力学的有吸引力策略。在本综述中,我们提供了糖蛋白共轭策略的概述,然后通过一些铂基糖蛋白共轭物的具体示例来说明该策略的应用。最后我们讨论了这些糖蛋白共轭物的一些重要方面,值得进一步研究。版权所有©2022 Elsevier Ltd.
Cancer, which is characterized by uncontrolled proliferation of abnormal cells, is a leading cause of morbidity and mortality worldwide. Cytotoxic chemotherapy, especially with platinum drugs, remains the mainstay of cancer treatment in the clinical setting. Despite phenomenal success, small-molecule chemotherapeutic drugs suffer from some serious drawbacks. Lack of cancer selectivity and the ensuing side effects mar the therapeutic potential of these drugs. Glycoconjugation has emerged as an attractive strategy for imparting selectivity and improving pharmacokinetics of cytotoxic agents. In this review, we provide an overview of the glycoconjugation strategy and then illustrate the application of this strategy with the help of some concrete examples of platinum based glycoconjugates. At the end we discuss a few important aspects of these glycoconjugates which merit further investigations.Copyright © 2022 Elsevier Ltd. All rights reserved.