G-protein-coupled receptors (GPCRs) are major targets for drug discovery. The regulator of G-protein signaling (RGS)-protein family has important roles in GPCR signal transduction. RGS proteins contain a conserved RGS-box, which is often accompanied by other signaling regulatory elements. RGS proteins accelerate the deactivation of G proteins to reduce GPCR signaling; however, some also have an more ..
Targets
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Depositor Specified Assays
| AID | Name | Type | Comment |
|---|---|---|---|
| 879 | qHTS Assay for Inhibitors of RGS12 GoLoco Motif Activity (Green Fluorophore) | confirmatory | Counterscreen RGS12 green fluorophore assay, screened against LOPAC library only. |
| 880 | qHTS Assay for Inhibitors of RGS12 GoLoco Motif Activity (Red Fluorophore) | confirmatory | RGS12 red fluorophore primary screen |
| 2390 | Confirmation qHTS Assay for Inhibitors of RGS12 GoLoco Motif Activity (Red Fluorophore) | confirmatory | RGS12 red fluorophore confirmation screen |
Description:
G-protein-coupled receptors (GPCRs) are major targets for drug discovery. The regulator of G-protein signaling (RGS)-protein family has important roles in GPCR signal transduction. RGS proteins contain a conserved RGS-box, which is often accompanied by other signaling regulatory elements. RGS proteins accelerate the deactivation of G proteins to reduce GPCR signaling; however, some also have an effector function and transmit signals. Combining GPCR agonists with RGS inhibitors should potentiate responses, and could markedly increase the agonist's regional specificity. The diversity of RGS proteins with highly localized and dynamically regulated distributions in brain makes them attractive targets for pharmacotherapy of central nervous system disorders. Inhibitors of the RGS:GPCR interaction should prove useful as small molecule tools in this research field.
This assay will summarize the probe development efforts that are currently ongoing.
Assay Submitter: Siderovski, David P, University of North Carolina at Chapel Hill
Screening Center PI: Austin, C.P.
Screening Center: NIH Chemical Genomics Center [NCGC]
NIH Grant: NS053754-01
This assay will summarize the probe development efforts that are currently ongoing.
Assay Submitter: Siderovski, David P, University of North Carolina at Chapel Hill
Screening Center PI: Austin, C.P.
Screening Center: NIH Chemical Genomics Center [NCGC]
NIH Grant: NS053754-01
Protocol
Please see related AIDs for individual BioAssay additional details:
879 - red fluorophore primary screen
880 - green fluorophore counterscreen
2390 - confirmation red fluorophore screen
879 - red fluorophore primary screen
880 - green fluorophore counterscreen
2390 - confirmation red fluorophore screen
Comment
Keywords: NIH Roadmap, MLSCN, MLI, MLSMR, qHTS, NCGC, rgs, rgs12, regulator of G-protein signalling 12, GTPase accelerating protein
Compound ranking comments will be provided here as small molecule probes are developed and are updated with results in PubChem.
Compound ranking comments will be provided here as small molecule probes are developed and are updated with results in PubChem.
Additional Information
Grant Number: NS053754-01
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