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GPCR Activation
(i.e. by Ligand/Drug)
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Activity-dependent adapter Recruitment
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Reconstituted TEV protease activity cleaves off the artificial transcription factor GV
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Nuclear GV activates the expression of molecular barcodes termed expressed sequence tags (EXT)
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Multiplexed assay using various different GPCRs
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Screening at various conditions (i.e. drugs, concentrations of drugs, time points).
The targetPROFILER is a profiling assay to monitor the activities of G protein-coupled receptors (GPCRs) and receptor tyrosine kinases (RTKs) under diverse stimuli conditions. Activities and target specificities of various GPCRs can be simultaneously analysed using the EXTassay technology. The activity of a given GPCR is measured using the splitSENSOR technology and the individual signaling events can be simultaneously analysed using the EXTassay technology.
A wide range of GPCRs are covered in this assay:
α-adrenergic receptors
ADRA1A
ADRA2B
ADRA2C
β-adrenergic receptors
ADRB2
Vasopressin receptors
AVPR1A
AVPR2
Dopamine receptors
DRD1
DRD2
DRD4
DRD5
Serotonin receptors
HTR1A
HTR2A
HTR4
HTR5A
HTR7
Somatostatin receptors
SSTR1
SSTR2
SSTR3