PathHunter™ GPCR Dimerization Assays

 

GPCRs can interact with each other at the plasma membrane to form homodimeric and heterodimeric complexes that can profoundly impact GPCR pharmacology and signaling. Compounds that specifically target GPCR heterodimers have the potential to achieve higher specificity with reduced side effects, define new drug targets, or behave as modulators of GPCR activity in specific tissues. As a result, there is considerable interest in the design of drugs that target GPCR heterodimers.

Highly Specific and Quantitative Tool for Novel Drug Discovery

Unlike traditional FRET or BRET-based approaches, PathHunter™ GPCR Dimerization Assays provide you with a highly specific and quantitative tool to study the interactions between different pairs of GPCRs, or GPCR heterodimers. These assays are unique in that only activation of the tagged GPCR will yield signal. Thus, they can be used to screen for compounds that enhance or disrupt heterodimerization and enable novel screens for modulators of GPCR activity.

How the PathHunter™ GPCR Dimerization System Works

The PathHunter™ GPCR Dimerization system was designed to identify novel compounds that act through GPCR heterodimer pairs. In this system, Arrestin is fused to the larger portion of β-gal, termed enzyme acceptor of EA, and the smaller, 42 amino acid ProLink™ (PK) tag is localized to one of the GPCR targets of interest. Using PathHunter Arrestin clones as the starting material, a second untagged GPCR receptor can be stably introduced into the cell line and the effects of the untagged GPCR on the PK-tagged GPCR can be measured using PathHunter detection reagents.

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