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开发用于癌症治疗的潜在药物肽。

Development of peptides as potential drugs for cancer therapy.

机构信息

School of Biomedical Sciences, Faculty of Medicine, The Chinese University of Hong Kong, Hong Kong, PR China.

出版信息

Curr Pharm Des. 2010;16(10):1180-9. doi: 10.2174/138161210790945913.

Abstract

The development of more selective agents focused on targeted delivery of imaging probes and drugs to different tumor sites is the current trend in cancer diagnosis and therapies. Peptides are small amino acid sequences that can be isolated to bind to a predetermined target and are potentially capable of interfering with its function. These specific peptides isolated can inhibit individual signaling components, which are essential in cancer development and progression. Phage display is a powerful technology for selecting and cloning peptides displayed on the surface of bacteriophage. Billionclone-peptide libraries can be rapidly and simultaneously selected by phage biopanning, leading to large numbers of hits. Although peptides account for only a small part of current therapeutic agents, their potential is being improved by new technologies affecting their modification, delivery, stability and their application in preclinical settings. This review will highlight how to isolate peptides that target pivotal molecules in cancer development and progression through phage library biopanning and how to modify these peptides to enhance their anticancer efficacy.

摘要

当前癌症诊断和治疗的一个趋势是开发更具选择性的药物,以将成像探针和药物靶向递送至不同的肿瘤部位。肽是可以分离出来与预定靶标结合的小氨基酸序列,并且有可能干扰其功能。从这些分离出来的特定肽可以抑制个体信号传导成分,这些成分在癌症的发生和发展中是必不可少的。噬菌体展示是一种从噬菌体表面展示的肽进行选择和克隆的强大技术。通过噬菌体生物淘选,可以快速且同时选择数十亿个克隆肽文库,从而获得大量的命中。尽管肽仅占当前治疗剂的一小部分,但通过影响其修饰、递送、稳定性以及在临床前环境中的应用的新技术,正在提高它们的潜力。这篇综述将重点介绍如何通过噬菌体文库生物淘选分离靶向癌症发生和发展关键分子的肽,以及如何修饰这些肽以增强其抗癌功效。

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