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Functional Assays

Functional Assays

GTP binding is a method used to study distribution and functional activation of seven transmembrane, heterotrimeric G protein coupled family (GPCRs) receptors.

This assay works best with Gi-coupled receptors. Upon activation of the GPCR by an agonist, the receptor changes conformation exposing a binding site for a G-protein complex. Once this G-protein complex is bound, the Gα protein can release GDP and bind GTP. These types of assays are sometimes referred to as a GTP exchange assay. Because the GTP used in this assay is a radiolabeled non-hydrolyzable analog ([35S]-GTPγS, which is GTP labeled on the gamma phosphate with 35S), you will be able to measure the activation of the GPCR being studied by measuring the amount of [35S]-GTPγS bound to the receptor.

Functional Assays can be used to:

  • Created by potrace 1.10, written by Peter Selinger 2001-2011 Determine the pharmacological values of potency (EC50) & efficacy (EMAX) of the ligand to activate the GPCR of interest.
  • Created by potrace 1.10, written by Peter Selinger 2001-2011 Visualize regional differences of activated GPCRs by a ligand using Functional Autoradiography.
  • Created by potrace 1.10, written by Peter Selinger 2001-2011 Determine if the ligand is a full agonist, partial agonist, inverse agonist or antagonist.

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Case Studies

Compound Characterization

Compound Characterization

Compound Characterization Study Goal Determine ex vivo receptor occupancy of CMPDx at Orexin-1 (OX1) receptors using radiolabeled Orexin antagonist Created by potrace 1.10, written by Peter Selinger 2

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Compound Characterization 1

Compound Characterization 1

Compound Characterization Study Goal Determine ex vivo receptor occupancy of CMPDx at Orexin-1 (OX1) receptors using radiolabeled Orexin antagonist Created by potrace 1.10, written by Peter Selinger 2

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