GPCR β-Arrestin Product Solutions

Universal GPCR Assays for Ligand Bias, Receptor Deorphanization, and Antagonist Discovery

With β-arrestins cell-based assays, you can easily monitor GPCR activity for antagonist mode screening, study ligand pharmacologies, and deorphanize GPCRs. Implement these assays to measure GPCR β-arrestin recruitment and subsequent internalization upon ligand or therapeutic activation of GPCRs in a dose-dependent manner.

β-Arrestins are ubiquitously expressed and function in the activation of GPCRs, desensitization of most 7-transmembrane receptors, and regulation of other signaling molecules such as protein kinases. β-Arrestin activation is part of the G protein-independent independent pathway that results from the ligand-activated GPCR phosphorylation by specific GPCR kinases referred to as GKRs. This phosphorylation leads to β-arrestin recruitment and binding that blocks G protein-mediated signaling, and results in the internalization (or endocytosis) of the GPCR; ending of the attenuation of GPCR signaling (known as desensitization). Subsequently, the GPCR is recycled back to the plasma membrane or degraded in the lysosome.

Eurofins DiscoverX® provides a complete set of analytical tools and brings decades of experience and hundreds of customer publications to β-arrestin biology. PathHunter® β-Arrestin cell lines, assays, kits, and reagents all offer a powerful and universal screening and profiling platform that can be used for virtually any Gi-, Gs-, or Gq-coupled receptor.

Product Highlights
  • Largest Portfolio – Covering ~90% of class A & B GPCR targets with over 400 cell-based assays, cell lines, kits, and reagents
  • Accurate Pharmacology – Easily distinguish ligand pharmacological differences with excellent superior performance for screening antagonists, positive allosteric modulators, and partial agonists
  • Multiplexing Capabilities – Run second messenger cAMP or calcium assays using the same β-arrestin cell line for ligand bias studies
  • Universal System – Independent of G-protein coupling, ideal for antagonist screening and GPCR deorphanization

Consider Eurofins DiscoverX’s custom development capabilities for custom cell lines, assays, & enzyme development.

SHOP PRODUCTSGPCR SOLUTIONSOBTAIN PRODUCT LISTDOWNLOAD EBOOK

Products

Product Types

Eurofins DiscoverX GPCR β-arrestin products for specific known, orphan, or ortholog (multiple species) GPCRs.  

  • GPCR β-Arrestin Bioassay Kits – Ready-to-use cell-based assay kits with a simple, homogenous protocol and are provided as qualified or target-based. These physiologically relevant, robust bioassays are fit-for-purpose for use in screening and characterization applications to potency testing in quality control lot-release programs. Learn more about Bioassay Kits.
  • GPCR β-Arrestin eXpress Assay Kits – Ready-to-use cell-based assay kits for quick analysis and implementation in early discovery phases for screening applications, proof-of-concept, mechanism of action confirmation, and rank-ordering studies. Learn more about eXpress Assay Kits.
  • GPCR β-Arrestin Cell Lines – Stable cell lines developed to reflect the target’s mechanism of action with a drug interaction in a standard cell line background. Learn more about Stable Cell Lines.
  • Parental Cell Lines – Engineered cells to generate your own GPCR assays and investigate β-arrestin recruitment and GPCR desensitization and internalization of your GPCR target of interest.
  • Retroviral Particles – Create target-specific, stable β-arrestin cell lines in any divided cell type. The product comes with a complete set of retroparticles and reagents combined with an easy-to-follow protocol to help you generate your own β-arrestin cell-based assays. Learn more about Toolbox Products.

Application Related Assays

  • cAMP Assays – Detect cellular cAMP levels via GPCR signaling by biologics or small molecule therapeutics using robust, simple, homogeneous, and HTS assays.
  • Calcium Assays – Fluorescent dye-based assays to measure calcium mobilization in cell lines as a direct indication of GPCR or ion channel activation or inhibition.
  • GPCR Internalization Assays – Secondary, orthogonal screening cell-based assays for measuring GPCR desensitization and recycling as well as uncovering novel classes of compound pharmacologies and identifying safer drugs without imaging or antibodies.
  • Pharmacotrafficking Assays – Quantitative cell-based assays to identify small molecule pharmacochaperones that act as therapeutic agents to stabilize and correct disease-relevant mutant GPCRs, ion channels, or transporters.
  • Membrane Preparations – Purified membrane preps for obtaining GPCR and ion channel ligand binding affinities and evaluating GPCR activity through GTPγS functional studies in response to the addition of a ligand or therapeutic.
  • Obesity/Diabetes Assays – Accelerate the development of GPCR peptide therapeutics like GLP-1, GIP and glucagon for obesity and diabetes with MOA-reflective assays.