MULTISCREEN™ GPCR β-Arrestin Solutions

HTS detection of biased cell signaling by unmodified GPCRs for improved identification and optimization of qualified drug candidates

To enable easy access to MULTISCREEN™ Beta-Arrestin Sensor Technology, Multispan offers complete solutions for academic and industry drug discovery assay needs. This portfolio includes: viral delivery tools for cell transduction, assay reagents, recombinant stable cell lines, and compound screening services.

For example...

An academic lab is in need to generate publication quality data for just a couple of tool molecules in the β-Arrestin cell signaling pathway. Instead of the older β-Arrestin technologies that they already have in the lab, they choose to examine their molecules using our new MULTISCREEN™ β-Arrestin Sensor, to avoid tagging their GPCR that may skew its pharmacology. Since the lab already has a stable cell line expressing the GPCR validated in the cAMP assay, they can purchase just the MULTISCREEN™ β-Arrestin BacMam Assay Kit. After simply adding the viral particles to the cell culture, 24-48 hours later,  they will be able to measure both signaling pathways in the one cell line using the substrate included in the kit, without having to modify their receptor. The assay is mix-and-read, no-wash, and homogeneous. It takes 30 minutes total with less than 10-minute hands-on time.  The same viral delivery assay kit can also be applied to primary cells for similar purposes. If the academic lab does not have any cell line expressing their GPCR target, they can purchase Multispan’s division-arrested cells expressing both the GPCR and the β-Arrestin Sensor instead or just the GPCR target alone plus the β-Arrestin BacMam Assay Kit. All these solutions are fast, convenient and reasonably priced at a standard reagent rate, amenable for academic budget.

In contrast, a pharmaceutical company with an orphan GPCR could be an example at the other end of the spectrum. Because very little biology is known, our team of experts will get involved early by studying the receptor in both β-Arrestin and cAMP pathways using transient transfection. Based on these initial results, we will generate and select stable cell lines co-expressing both the orphan GPCR and the β-Arrestin Sensor. We will determine the best clone to use for surrogate ligand screening based on baseline activity level and carry out the HTS screening campaign. The surrogate ligand candidate may be further studied in alternative clones to select the best clone for compound lead optimization. Combined with Multispan’s assay expertise-driven service, the MULTISCREEN™ β-Arrestin Sensor can be a powerful tool in deciphering the biology of orphan GPCRs and discovering novel therapeutics by utilizing these untapped, mysterious but highly “druggable” receptors.

MULTISCREEN™ β-Arrestin assay kits:

  • MULTISCREEN™ β-Arrestin Assay Kit: This basic assay kit contains Substrate and Assay Buffer. It’s validated by MULTISCREEN™ stable cell lines co-expressing target GPCRs and MULTISCREEN™ β-Arrestin sensors. The kit is validated by MULTISCREEN™ GPCR stable cell lines and division-arrested cells.
  • MULTISCREEN™ β-Arrestin BacMam Assay Kit: This viral delivery kit contains BacMam viral particles expressing the bi-cistronic MULTISCREEN™ β-Arrestin sensor cDNA, control GFP BacMam viral particle, the Substrate and Assay Buffer. The kit is validated by MULTISCREEN™ GPCR stable cell lines and division-arrested cells.
  • MULTISCREEN™ β-Arrestin HSV Assay Kit: This viral delivery kit contains Herpes Simplex viral (HSV) particles expressing the bi-cistronic MULTISCREEN™ β-Arrestin sensor cDNA, control GFP HSV viral particle, the Substrate and Assay Buffer. The kit is validated by MULTISCREEN™ GPCR stable cell lines and division-arrested cells.

Cell Lines

  • Validated MULTISCREEN™ stable cell lines co-expression β-Arrestin Sensor and GPCR
  • 500+ Validated MULTISCREEN™ stable cell lines expressing GPCRs readily transduced by MULTISCREEN™ β-Arrestin viral particles
  • Custom MULTISCREEN™ stable cell line generation co-expression β-Arrestin Sensor and GPCR
  • Division-arrested cells from stable cell lines co-expression β-Arrestin Sensor and GPCR or GPCR alone
  • In-licensing for institute-wide access: Parental CHO and HEK293T cells stablyexpressing  MULTISCREEN™ β-Arrestin Sensors: β-Arrestin 1 and β-Arrestin 2

Full Services

  • Custom stable cell line generation co-expression β-Arrestin Sensor and GPCR
  • Development of MULTISCREEN™ β-Arrestin HTS assays and all secondary and tertiary assays required from target to IND
  • HTS screening, hit-to-lead, lead optimization and profiling services using β-Arrestin assays
  • Deliverable: IND-enabling candidate

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