GPR35的药理研究进展5-HIAA 5-羟色胺代谢物成为配体

IF 6.9 3区 医学 Q1 CHEMISTRY, MEDICINAL Archives of Pharmacal Research Pub Date : 2023-05-25 DOI:10.1007/s12272-023-01449-y
Dong-Soon Im
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引用次数: 1

摘要

GPR35是一种孤儿受体,自1998年克隆以来一直在等待它的配体。许多内源性和外源性分子被认为是GPR35的激动剂,包括犬尿酸、扎普利司特、溶血磷脂酸和CXCL17。然而,除了孤儿状态外,物种之间对配体的复杂和有争议的反应已经成为治疗药物发展的巨大障碍。最近,一种血清素代谢物5-羟基吲哚乙酸(5-HIAA)通过研究GPR35在中性粒细胞中的表达增加,被报道为GPR35的高效配体。此外,我们开发了一种转基因敲入小鼠系,其中GPR35被人类同源物取代,不仅可以克服激动剂在物种之间的不同选择性,而且可以在小鼠模型中对人类GPR35进行治疗实验。本文就GPR35的研究进展及未来治疗方向作一综述。特别想提请读者注意的是,发现5-HIAA作为GPR35的配体,并导致5-HIAA和人GPR35敲入小鼠在多种病理生理条件下应用于各自的研究领域。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Recent advances in GPR35 pharmacology; 5-HIAA serotonin metabolite becomes a ligand

GPR35, an orphan receptor, has been waiting for its ligand since its cloning in 1998. Many endogenous and exogenous molecules have been suggested to act as agonists of GPR35 including kynurenic acid, zaprinast, lysophosphatidic acid, and CXCL17. However, complex and controversial responses to ligands among species have become a huge hurdle in the development of therapeutics in addition to the orphan state. Recently, a serotonin metabolite, 5-hydroxyindoleacetic acid (5-HIAA), is reported to be a high potency ligand for GPR35 by investigating the increased expression of GPR35 in neutrophils. In addition, a transgenic knock-in mouse line is developed, in which GPR35 was replaced with a human ortholog, making it possible not only to overcome the different selectivity of agonists among species but also to conduct therapeutic experiments on human GPR35 in mouse models. In the present article, I review the recent advances and prospective therapeutic directions in GPR35 research. Especially, I’d like to draw attention of readers to the finding of 5-HIAA as a ligand of GPR35 and lead to apply the 5-HIAA and human GPR35 knock-in mice to their research fields in a variety of pathophysiological conditions.

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来源期刊
CiteScore
13.40
自引率
9.00%
发文量
48
审稿时长
3.3 months
期刊介绍: Archives of Pharmacal Research is the official journal of the Pharmaceutical Society of Korea and has been published since 1976. Archives of Pharmacal Research is an interdisciplinary journal devoted to the publication of original scientific research papers and reviews in the fields of drug discovery, drug development, and drug actions with a view to providing fundamental and novel information on drugs and drug candidates.
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