Therapeutic Exploitation of GPR18: Beyond the Cannabinoids?

Therapeutic Exploitation of GPR18: Beyond the Cannabinoids?
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GPR18的治疗性开发:超越大麻素?

DOI:
10.1021/acs.jmedchem.0c00926
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发表时间:
2020-12-10
影响因子:
7.3
通讯作者:
Jagerovic N
Jagerovic N
中科院分区:
医学1区
文献类型:
--
作者:
Morales P;Lago-Fernandez A;Hurst DP;Sotudeh N;Brailoiu E;Reggio PH;Abood ME;Jagerovic N

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GPR18是一种G蛋白偶联受体,属于孤儿A类家族。尽管它与大麻素受体CB1R和CB2R具有低序列同源性,但越来越多的研究表明它与内源性大麻素系统的关系,不仅因为它能够识别大麻素配体,而且还因为它的表达和与CBR异聚化的能力。从这个角度来看,我们的目标是分析GPR18的生物学相关性,已报道的调节剂和结构特征。为了指导未来的药物设计在这一领域,从GPR18的分子模拟的亮点将提供。
GPR18 is a G protein-coupled receptor that belongs to the orphan class A family. Even though it shares low sequence homology with the cannabinoid receptors, CB1R and CB2R, a growing body of research suggests its relationship with the endocannabinoid system, not only because it is able to recognize cannabinoid ligands, but also because of its expression and ability to heteromerize with CBRs. In this perspective, we aim to analyze the biological relevance, reported modulators and structural features of GPR18. In order to guide future drug design in this field, highlights from molecular modeling of GPR18 will be provided.
n-芳基多烯酰基甘氨酸,GPR55的另一种内源性激动剂。
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发表时间: 2017-09-02
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