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针对肿瘤细胞的去端肽酶:从体外到临床试验的里程碑。

Depsipeptides Targeting Tumor Cells: Milestones from In Vitro to Clinical Trials.

机构信息

Tecnológico de Monterrey, School of Engineering, and Sciences, Avenida Eugenio Garza Sada 2501, Monterrey 64849, Nuevo León, Mexico.

出版信息

Molecules. 2023 Jan 9;28(2):670. doi: 10.3390/molecules28020670.

DOI:10.3390/molecules28020670
PMID:36677728
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9864405/
Abstract

Cancer is currently considered one of the most threatening diseases worldwide. Diet could be one of the factors that can be enhanced to comprehensively address a cancer patient's condition. Unfortunately, most molecules capable of targeting cancer cells are found in uncommon food sources. Among them, depsipeptides have emerged as one of the most reliable choices for cancer treatment. These cyclic amino acid oligomers, with one or more subunits replaced by a hydroxylated carboxylic acid resulting in one lactone bond in a core ring, have broadly proven their cancer-targeting efficacy, some even reaching clinical trials and being commercialized as "anticancer" drugs. This review aimed to describe these depsipeptides, their reported amino acid sequences, determined structure, and the specific mechanism by which they target tumor cells including apoptosis, oncosis, and elastase inhibition, among others. Furthermore, we have delved into state-of-the-art in vivo and clinical trials, current methods for purification and synthesis, and the recognized disadvantages of these molecules. The information collated in this review can help researchers decide whether these molecules should be incorporated into functional foods in the near future.

摘要

癌症目前被认为是全球最具威胁性的疾病之一。饮食可能是可以改善癌症患者病情的因素之一。不幸的是,大多数能够靶向癌细胞的分子存在于不常见的食物来源中。其中,环二肽已成为癌症治疗最可靠的选择之一。这些环状氨基酸寡聚物,其中一个或多个亚基被羟基羧酸取代,导致核心环中有一个内酯键,广泛证明了它们的抗癌效果,有些甚至已经进入临床试验并被商业化作为“抗癌”药物。本综述旨在描述这些环二肽,它们的报道的氨基酸序列、确定的结构以及它们靶向肿瘤细胞的特定机制,包括细胞凋亡、胀亡和弹性蛋白酶抑制等。此外,我们还深入研究了最新的体内和临床试验、当前的纯化和合成方法,以及这些分子的公认缺点。本综述中收集的信息可以帮助研究人员决定这些分子是否应该在不久的将来被纳入功能性食品中。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0982/9864405/42899d72141b/molecules-28-00670-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0982/9864405/d0748389bd00/molecules-28-00670-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0982/9864405/0ddc8f40d406/molecules-28-00670-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0982/9864405/4ba1b1dacbe4/molecules-28-00670-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0982/9864405/f27aa1ec152b/molecules-28-00670-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0982/9864405/7b604c9ada9c/molecules-28-00670-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0982/9864405/113d98758ad8/molecules-28-00670-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0982/9864405/2991b68f1097/molecules-28-00670-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0982/9864405/6dfc07e8b631/molecules-28-00670-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0982/9864405/42899d72141b/molecules-28-00670-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0982/9864405/d0748389bd00/molecules-28-00670-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0982/9864405/0ddc8f40d406/molecules-28-00670-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0982/9864405/4ba1b1dacbe4/molecules-28-00670-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0982/9864405/f27aa1ec152b/molecules-28-00670-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0982/9864405/7b604c9ada9c/molecules-28-00670-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0982/9864405/113d98758ad8/molecules-28-00670-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0982/9864405/2991b68f1097/molecules-28-00670-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0982/9864405/6dfc07e8b631/molecules-28-00670-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0982/9864405/42899d72141b/molecules-28-00670-g009.jpg

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