Evidence map›Paper›PMID 34946593›Full record

ArticleMolecules (Basel, Switzerland)2021

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

Guangyao Lin, Yang Feng, Xiaoqing Cai, Caihong Zhou, Lijun Shao, Yan Chen, Linhai Chen, Qing Liu, Qingtong Zhou, Ross A D Bathgate and 2 more

Open access · goldAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Molecules (Basel, Switzerland), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
1.2field-weighted citation impact, top 20% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

4 citing papers in PubMed, 8 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

12 authors at 5 institutions in 2 countries.

Guangyao LinThe National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Yang FengThe National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Xiaoqing CaiThe National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Caihong ZhouThe National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Lijun ShaoUniversity of Chinese Academy of Sciences, Beijing 100049, China.
Yan ChenDepartment of Pharmacology, School of Basic Medical Sciences, Fudan University, Shanghai 200032, China.
Linhai ChenThe National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Qing LiuThe National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.ORCID 0000-0003-1825-6760
Qingtong ZhouDepartment of Pharmacology, School of Basic Medical Sciences, Fudan University, Shanghai 200032, China.
Ross A D BathgateFlorey Institute of Neuroscience and Mental Health and Department of Biochemistry and Pharmacology, The University of Melbourne, Parkville, VIC 3052, Australia.ORCID 0000-0001-6301-861X
Dehua YangThe National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Ming-Wei WangThe National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
Shanghai Institute of Materia Medica · CNChinese Academy of Sciences · CNFudan University · CNShanghaiTech University · CNThe University of Melbourne · AU

Funding

National Key R&D Program of China 2018YFA0507000 (M-WW)National Natural Science Foundation of China 81872915 (M.-W.W.), 82073904 (M.-W.W.), 81573479 (DHY) and 81773792 (DHY)National Science & Technology Major Project "Key New Drug Creation and Manufacturing Pro-gram" of China 2018ZX09735-001 to M-WW, 2018ZX09711002-002-005 to DHY and 2018ZX09711002-002-011 to QLNovo Nordisk-CAS Research Fund NNCAS-2017-1-CC to DHYVictorian Government's Operational Infrastructure Support Program to RADB
6 · The paper itself

Abstract

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.

Indexed as

High-Throughput Screening AssaysDose-Response Relationship, DrugHumansModels, MolecularReceptors, G-Protein-CoupledReceptors, PeptideSmall Molecule LibrariesReceptors, G-Protein-CoupledReceptors, PeptideRXFP3 protein, humanRXFP4 protein, humanSmall Molecule Librariesagonisthigh-throughput screeningRXFP3RXFP4WNN0109-C011

Identifiers

PMID34946593
PMCPMC8709172
OpenAlexW4200580263

What OpenQuestion holds

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Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.