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BioAssay: AID 2703

qHTS Assay for Agonists of the Relaxin Receptor RXFP1: Summary

The relaxin hormone is involved in the variety of biological functions in normal tissues and diseases. The role of relaxin is well-established in female reproduction and parturition, mammary gland and endometrial development, maintenance of myometrial quiescence during pregnancy. Relaxin signaling through its G protein-coupled receptor (GPCR) RXFP1 results in ECM remodeling through regulation of more ..
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AID: 2703
Data Source: NCGC (RXFP146)
BioAssay Type: Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: NIH Molecular Libraries Probe Production Network
Deposit Date: 2010-03-26
Target
Depositor Specified Assays
Show more
AIDNameTypeComment
2676qHTS Assay for Agonists of the Relaxin Receptor RXFP1confirmatory
492949qHTS Assay for Agonists of the Relaxin Receptor RXFP1: THP1 Hit Validationconfirmatory
492948qHTS Assay for Agonists of the Relaxin Receptor RXFP1: V1B Hit Validationconfirmatory
602256qHTS Assay for Agonists of the Relaxin Receptor RXFP1: RXFP1 SARconfirmatory
602288qHTS Assay for Agonists of the Relaxin Receptor RXFP1: Cytotoxicity SARconfirmatory
602291qHTS Assay for Agonists of the Relaxin Receptor RXFP1: Cell Impedanceother
602262qHTS Assay for Agonists of the Relaxin Receptor RXFP1: V1B SARconfirmatory
602286qHTS Assay for Agonists of the Relaxin Receptor RXFP1: Mouse Liver Microsome Stabilityother
489043qHTS Assay for Agonists of the Relaxin Receptor RXFP1: RXFP2 Hit Validationconfirmatory
602258qHTS Assay for Agonists of the Relaxin Receptor RXFP1: RXFP2 SARconfirmatory
602287qHTS Assay for Agonists of the Relaxin Receptor RXFP1: PBS Solubilityother
602290qHTS Assay for Agonists of the Relaxin Receptor RXFP1: VEGF expressionother
489012qHTS Assay for Agonists of the Relaxin Receptor RXFP1: RXFP1 Hit Validationconfirmatory
Description:
NIH Chemical Genomics Center [NCGC]
NIH Molecular Libraries Probe Production Centers Network [MLPCN]

MLPCN Grant: R03 MH085705-01A1
Assay Submitter (PI): Alexander Agoulnik

NCGC Assay Overview:

The relaxin hormone is involved in the variety of biological functions in normal tissues and diseases. The role of relaxin is well-established in female reproduction and parturition, mammary gland and endometrial development, maintenance of myometrial quiescence during pregnancy. Relaxin signaling through its G protein-coupled receptor (GPCR) RXFP1 results in ECM remodeling through regulation of collagen deposition, cell invasiveness, proliferation and overall tissue homeostasis. Significantly, the therapeutic effects of relaxin in the treatment of renal, cardiac, skin, lung fibrosis, inflammation, and wound healing in animal models are well-established. Recombinant human relaxin (rhRlx) is currently being tested in clinical trials as a protective agent in congestive heart failure, in treating severe preeclampsia, and as an anti-fibrotic agent in systemic sclerosis.

Upon relaxin binding RXFP1 activation leads to the activation of adenylate cyclase (AC) via Gs. cAMP will activate PKA, which phosphorylates many signaling proteins. Thus, detection of cAMP increase is an easy and reliable indication of relaxin receptor activation. To screen for agonists of the relaxin receptor, a HEK293T cell line stably transfected with RXFP1 was used. RXFP1 activation was assayed by changes in cAMP levels as detected with a time-resolved fluorescence energy transfer (TR-FRET) cAMP detection kit.
Protocol
See specific AIDs (AID 2676) for detailed assay protocols.
Comment
This is a summary for the entire project. The primary screen has been completed, but no results yet confirmed. No probes have been declared for this project.
Additional Information
Grant Number: MH085705-01A1

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