Screening for inhibitors of RGS protein GAP Activity using the Transcreener GDP Assay

The Only Mix-and-Read Fluorescent GAP Assay

Look at GPCR drug discovery from a whole new angle!

GAP  proteins stimulate the GTPase, which is detected as an increase in GDP formation using the Transcreener GDP GAP Assay. For RGS activity, the required protein and detection reagents are available from BellBrook for purchase or as a service.

  • Universal GAP Detection: HTS-ready assay method for GAP activity
  • A Complete Screening and Profiling Solution: Recombinant RGS proteins and kinetically enhanced Gα proteins are available. Contact us for more info.

HTS Ready Assay for RGS Protein GAP Activity

The most direct way to detect RGS function is by measuring the increased GTPase activity of the associated Gα protein. However, the GTPase activity of isolated Gα proteins is limited by GDP dissociation, so RGS GAP activity is difficult to measure using simple biochemical assays. Use your own GAP protein or overcome this kinetic constraint of RGS function by using proprietary Gα protein variants with altered GTP hydrolysis and GDP dissociation rates that enable detection of RGS GAP activity using the Transcreener® GDP Assay.

Members of the “regulator of G-protein signaling” (RGS)-protein superfumily act as “GTPase-accelerating proteins” (GAP) for heterotrimeric G-protein alpha subunits, thereby attenuating GPCR signaling. Their selectivity for specific GPCRs and downstream signaling components and their tissue-specific expression makes them attractive as potential therapeutic targets, with the potential for modulating the effects of existing GPCR agonists.

Far Red FP, FI & TR-FRET Readouts Validated on Major Multimode Readers

Supplier Instrument FP Assays
FI Assays
TR-FRET Assays
bioteklogo TriStar²S LB 942 in review validated validated
Mithras² LB 943 in review validated validated
bioteklogo Cytation™ 5 validated validated validated
Cytation™ 3 validated validated validated
Cytation™ 1 validated validated validated
Synergy™ H1 validated validated validated
Synergy™ 2/H4/4 validated validated validated
Synergy™ HTX not capable validated not capable
Synergy™ Neo 2 validated validated validated
BMGLABTECH Logo POLARstar® Omega validated validated validated
FLUOstar® Omega not capable validated validated
PHERAstar® FSX validated validated validated
PHERAstar® Plus/FS validated validated validated
CLARIOstar® /Plus validated validated validated
hidex logo Sense in review validated in review
MDS AT logo Analyst® GT/HT validated validated validated
Gemini® XPS/EM not capable validated not capable
SpectraMax® M2/M2e not capable validated not capable
SpectraMax® M5/M5e/FlexStation® 3 not capable validated validated
SpectraMax® Paradigm validated contact us contact us
SpectraMax® iD3/iD5 in review validated validated
perkinElmerLogo EnVision®/EnVision® Xcite validated validated validated
tecanLogo Infinite® M1000/M1000Pro/Safire2™ validated validated validated
Infinite® M200 not capable validated not capable
Infinite® F500 validated validated validated
Infinite® F200/Ultraevolution contact us validated contact us
Spark™ 10M validated validated validated

Transcreener GDP Assay Kits

* For custom or bulk orders (over 100,000 wells) please contact us (info@bellbrooklabs.com) for a quote.

In addition to our GDP GAP Assays, Bellbrook Labs also offers the following products and services to aid in the drug discovery process:

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