High-Throughput Screening Campaign Identified a Potential Small Molecule RXFP3/4 Agonist

doi:10.3390/molecules26247511

	High-Throughput Screening Campaign Identified a Potential Small Molecule RXFP3/4 Agonist
	Lin, Guangyao 1,2; Feng, Yang 1; Cai, Xiaoqing 1; Zhou, Caihong 1; Shao, Lijun2,3 ; Chen, Yan 4; Chen, Linhai 1; Liu, Qing 1; Zhou, Qingtong 4; Bathgate, Ross A. D.5,6; Yang, Dehua 1,2,7,8; Wang, Ming-Wei1,2,3,4,7,8
	2021-12
发表期刊	MOLECULES (IF:4.2[JCR-2023],4.6[5-Year])
EISSN	1420-3049
卷号	26 期号:24
发表状态	已发表
DOI	10.3390/molecules26247511
摘要	Relaxin/insulin-like family peptide receptor 3 (RXFP3) belongs to class A G protein-coupled receptor family. RXFP3 and its endogenous ligand relaxin-3 are mainly expressed in the brain with important roles in the regulation of appetite, energy metabolism, endocrine homeostasis and emotional processing. It is therefore implicated as a potential target for treatment of various central nervous system diseases. Since selective agonists of RXFP3 are restricted to relaxin-3 and its analogs, we conducted a high-throughput screening campaign against 32,021 synthetic and natural product-derived compounds using a cyclic adenosine monophosphate (cAMP) measurement-based method. Only one compound, WNN0109-C011, was identified following primary screening, secondary screening and dose-response studies. Although displayed agonistic effect in cells overexpressing the human RXFP3, it also showed cross-reactivity with the human RXFP4. This hit compound may provide not only a chemical probe to investigate the function of RXFP3/4, but also a novel scaffold for the development of RXFP3/4 agonists.
关键词	RXFP3 RXFP4 high-throughput screening agonist WNN0109-C011
URL	查看原文
收录类别	SCI ; SCIE
语种	英语
WOS研究方向	Biochemistry & Molecular Biology ; Chemistry
WOS类目	Biochemistry & Molecular Biology ; Chemistry, Multidisciplinary
WOS记录号	WOS:000736215700001
出版者	MDPI
引用统计	正在获取...
文献类型	期刊论文
条目标识符	https://kms.shanghaitech.edu.cn/handle/2MSLDSTB/147236
专题	生命科学与技术学院_博士生生命科学与技术学院_特聘教授组_王明伟组
通讯作者	Yang, Dehua; Wang, Ming-Wei
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 3.ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 201210, Peoples R China 4.Fudan Univ, Sch Basic Med Sci, Dept Pharmacol, Shanghai 200032, Peoples R China 5.Univ Melbourne, Florey Inst Neurosci & Mental Hlth, Parkville, Vic 3052, Australia 6.Univ Melbourne, Dept Biochem & Pharmacol, Parkville, Vic 3052, Australia 7.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China 8.Res Ctr Deepsea Bioresources, Sanya 572025, Hainan, Peoples R China
通讯作者单位	生命科学与技术学院
推荐引用方式 GB/T 7714	Lin, Guangyao,Feng, Yang,Cai, Xiaoqing,et al. High-Throughput Screening Campaign Identified a Potential Small Molecule RXFP3/4 Agonist[J]. MOLECULES,2021,26(24).
APA	Lin, Guangyao.,Feng, Yang.,Cai, Xiaoqing.,Zhou, Caihong.,Shao, Lijun.,...&Wang, Ming-Wei.(2021).High-Throughput Screening Campaign Identified a Potential Small Molecule RXFP3/4 Agonist.MOLECULES,26(24).
MLA	Lin, Guangyao,et al."High-Throughput Screening Campaign Identified a Potential Small Molecule RXFP3/4 Agonist".MOLECULES 26.24(2021).