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受体亚型或物种同源物:与药物发现的相关性。

Receptor subtypes or species homologues: relevance to drug discovery.

作者信息

Hall J M, Caulfield M P, Watson S P, Guard S

机构信息

Biomedical Sciences Division, King's College, London, UK.

出版信息

Trends Pharmacol Sci. 1993 Oct;14(10):376-83. doi: 10.1016/0165-6147(93)90096-3.

Abstract

Cell surface receptors are targets for the pharmacological manipulation of physiological processes and thus represent a key direction for the development of selective therapeutic agents. Traditional pharmacological techniques, together with the development of synthetic ligands, have led to the identification of differences in receptor recognition properties and the proposal of multiple receptor subtypes. Molecular biological studies have confirmed the existence of receptor subtypes within a single species by demonstrating differences in receptor primary sequences. However, equivalent receptors between species also show differences in primary structure, albeit to a much lower degree. This review by Judith Hall and colleagues addresses the question of how differences in receptor primary structure between species relate to changes in pharmacology. The relevance of this to the choice of screens in the testing of potential therapeutic drugs is discussed.

摘要

细胞表面受体是生理过程药物调控的靶点,因此是选择性治疗药物开发的一个关键方向。传统药理学技术以及合成配体的发展,已促使人们识别出受体识别特性的差异,并提出了多种受体亚型。分子生物学研究通过证明受体一级序列的差异,证实了单一物种内受体亚型的存在。然而,不同物种间的等效受体在一级结构上也存在差异,尽管程度要低得多。朱迪思·霍尔及其同事的这篇综述探讨了物种间受体一级结构的差异与药理学变化之间的关系问题。文中还讨论了这一点对潜在治疗药物测试中筛选方法选择的相关性。

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