Drug Screening - 7TM Ligand Profiling
GPCR ligands can stabilize different receptor active states that interact with cellular signaling proteins in varying degrees. This leads to selective activation of some signaling pathways at the expense of others. A prominent example of such signaling bias is G-protein vs. arrestin signaling. A wide range of studies has applied this knowledge to design better drugs with fewer side effects. However, the major hurdle in the application of this mechanism to therapeutics is the translation of in vitro bias to in vivo effect. This is in part due to the wide spread use of conventional arrestin recruitment assays for the determination of arrestin signaling.
At the receptor level, phosphorylation precedes arrestin activation. In fact, recent work clearly shows that determination of agonist-induced phosphorylation using premium phosphosite-specific 7TM antibodies provides valuble information on ligand bias beyond that obtained with conventional ß-arrestin recruitment assays. In the design of better drugs, it is important to know whether your ligand is a full, partial or biased agonist. Thus, ligand profiling using premium phosphosite-specific 7TM antibodies can provide critical previously not available information. If you need help in ligand profiling, please contact us.
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