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BioAssay: AID 2406

Probe Development Summary for Inhibitors of RGS12 GoLoco Motif Activity

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 ..
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AID: 2406
Data Source: NCGC (RGSP100)
BioAssay Type: Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: NIH Molecular Libraries Screening Center Network
Deposit Date: 2010-02-24
Targets
Related Experiments
AIDNameTypeComment
879qHTS Assay for Inhibitors of RGS12 GoLoco Motif Activity (Green Fluorophore)Confirmatorydepositor-specified cross reference: Counterscreen RGS12 green fluorophore assay, screened against LOPAC library only.
880qHTS Assay for Inhibitors of RGS12 GoLoco Motif Activity (Red Fluorophore)Confirmatorydepositor-specified cross reference: RGS12 red fluorophore primary screen
2390Confirmation qHTS Assay for Inhibitors of RGS12 GoLoco Motif Activity (Red Fluorophore)Confirmatorydepositor-specified cross reference: 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
Protocol
Please see related AIDs for individual BioAssay additional details:
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.
Additional Information
Grant Number: NS053754-01

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