High-Throughput Screening Campaign Identified a Potential Small Molecule RXFP3/4 Agonist
文献类型：期刊论文
| 作者 | Lin, Guangyao1,2; Feng, Yang2; Cai, Xiaoqing2; Zhou, Caihong2; Shao, Lijun1,3; Chen, Yan4; Chen, Linhai2 ; Liu, Qing2; Zhou, Qingtong4; Bathgate, Ross A. D.5,6
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| 刊名 | MOLECULES
 |
| 出版日期 | 2021-12-01 |
| 卷号 | 26期号:24页码:10 |
| 关键词 | RXFP3 RXFP4 high-throughput screening agonist WNN0109-C011 |
| DOI | 10.3390/molecules26247511 |
| 通讯作者 | Yang, Dehua() ; Wang, Ming-Wei() |
| 英文摘要 | 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. |
| WOS关键词 | RELAXIN FAMILY PEPTIDES ; NUCLEUS INCERTUS ; RECEPTOR RXFP3 ; H3 RELAXIN ; CHIMERIC PEPTIDE ; MESSENGER-RNA ; MICE DISPLAY ; H2 RELAXIN ; ANTAGONIST ; BINDING |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000736215700001 |
| 出版者 | MDPI |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/300655]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Yang, Dehua; Wang, Ming-Wei |
| 作者单位 | 1.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, 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 |
| 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):10. |
| 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),10. |
| MLA | Lin, Guangyao,et al."High-Throughput Screening Campaign Identified a Potential Small Molecule RXFP3/4 Agonist".MOLECULES 26.24(2021):10. |
入库方式： OAI收割
来源：上海药物研究所
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