GPR18和gpr55相关配体作为拮抗剂或激动剂:现状、挑战和展望

IF 1.9 4区医学 Q3 CHEMISTRY, MEDICINAL Medicinal Chemistry Pub Date : 2023-01-01 DOI:10.2174/1573406419666230406095220

Linjie Zhang, Yiwen Fang, Sijing Hang, Wenhui Wu, Ruilong Sheng, Ruihua Guo

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引用次数: 0

摘要

GPCR超家族是已知最大的膜受体家族，由A ~ f 6个类组成，为A类的δ分支GPR18和GPR55，据报道没有确定的内源性配体，被称为“孤儿受体”。既往研究表明，GPR18和GPR55都可能与癌细胞、巨噬细胞等炎症相关免疫细胞的迁移和增殖有关。因此，它们可能是炎症、癌症和镇痛治疗的潜在靶点。本文综述了GPR18和GPR55的激动剂和拮抗剂的化学结构和生物活性;此外，我们还简要讨论了该领域的挑战和未来前景。这一综述将有助于进一步设计和合成高效的GPR18和GPR55相关疾病的激动剂和拮抗剂。

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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GPR18 and GPR55-related Ligands Serving as Antagonists or Agonists: Current Situation, Challenges and Perspectives.

GPCR superfamily, the largest known family of membrane receptors, consists of six classes from A to F. GPR18 and GPR55, δ-branch of A class, had been reported to have no confirmed endogenous ligand and were named as "orphan receptors". Previous studies suggest that both GPR18 and GPR55 are possibly related to the migration and proliferation of cancer cells, macrophages and other inflammation-associated immune cells. Thus, they may be potential targets for inflammation, cancer and analgesia therapy. In this paper, we aimed to summarize the chemical structures and bioactivities of the agonists and antagonists of GPR18 and GPR55; moreover, we have briefly discussed the challenges and future perspectives in this field. This review will be beneficial for further design and synthesis of efficient agonists and antagonists towards GPR18 and GPR55- related disease treatment.

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来源期刊

Medicinal Chemistry 医学-医药化学

CiteScore

4.30

自引率

4.30%

发文量

109

审稿时长

12 months

期刊介绍： Aims & Scope Medicinal Chemistry a peer-reviewed journal, aims to cover all the latest outstanding developments in medicinal chemistry and rational drug design. The journal publishes original research, mini-review articles and guest edited thematic issues covering recent research and developments in the field. Articles are published rapidly by taking full advantage of Internet technology for both the submission and peer review of manuscripts. Medicinal Chemistry is an essential journal for all involved in drug design and discovery.