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作为治疗干预的拮抗剂,设计和开发肽及肽模拟物。

Design and development of peptides and peptide mimetics as antagonists for therapeutic intervention.

机构信息

Department of Biological Sciences, University of Essex, Wivenhoe Park, Colchester, CO4 3SQ, UK.

出版信息

Future Med Chem. 2010 Dec;2(12):1813-22. doi: 10.4155/fmc.10.259.

DOI:10.4155/fmc.10.259
PMID:21428804
Abstract

The concept of peptides as therapeutic agents has been historically disregarded by the pharmaceutical industry on account of their susceptibility to degradation, their size and consequent limitations in methods of delivery. Recently, however, there has been a surge of interest in peptides and their mimetics as potential antagonists for therapeutic intervention. This is in part due to the increased half-life and oral availability that has been achieved for a number of peptide-based systems, the introduction and acceptance of alternative delivery methods, and the prevalence of proteomics to identify countless protein-protein interaction targets. The use of peptides and molecules that mimic their function therefore has great potential to effectively target a range of proteins that are pathogenically implicated in numerous diseases.

摘要

肽作为治疗剂的概念在历史上一直被制药行业所忽视,这是由于它们易于降解,体积较大,因此在给药方法上存在限制。然而,最近人们对肽及其类似物作为潜在治疗干预的拮抗剂产生了浓厚的兴趣。这在一定程度上是由于一些基于肽的系统的半衰期和口服生物利用度的提高,替代给药方法的引入和接受,以及蛋白质组学的普及,以鉴定无数的蛋白质-蛋白质相互作用靶标。因此,使用肽和模拟其功能的分子具有很大的潜力,可以有效地针对许多疾病中与病原体相关的一系列蛋白质。

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