Review Article

神经激肽:拟肽配体的设计和治疗应用

卷 27, 期 9, 2020

页: [1515 - 1561] 页: 47

弟呕挨: 10.2174/0929867325666180913095918

价格: $65

摘要

在许多病理和生理事件中,神经激肽无疑是必需的神经递质。它们的发现被广泛分布在中枢神经系统(CNS)和周围组织中,迅速将它们提升为药物靶标。作为分子工具理解此类生物学作用的必要条件,内源性肽及其受体促使科学界设计出在三种主要神经激肽受体(即NK1,NK2和NK3)上均表现出激动剂和拮抗剂活性的配体。为此目的实施了几种策略。由于偏爱小的非肽配体,许多研究小组投入了大量精力来合成和评估各种支架,但是只有NK1拮抗剂Aprepitant(EMENDT)及其前药Fosaprepitant(IVEMENDT)得到了食品药品监督管理局的批准( FDA)用于治疗化疗引起的和术后恶心和呕吐(分别为CINV和PONV)。尽管非肽类药物显示出局限性,尤其是在副作用控制方面,但肽类和假肽类化合物逐渐引起人们的注意。实施了各种策略来调节新设计的配体的亲和力,选择性和活性。规范氨基酸的替换,构象限制的结合以及与非肽部分的融合产生了显示单个或双重NK1,NK2和NK3拮抗作用的配体家族,这些配体最终与非神经激肽配体(如阿片类药物)结合为目标增强生物影响。

关键词: 神经激肽,配体,拮抗剂,拟肽,小型杂环支架,药物设计。

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