Functional Screening

Current screening strategies can be categorised as either affinity strategies, where library molecules are scanned against the target molecule in isolation to find potential binders, or functional strategies, where ligands are tested against cells to see if they elicit a functional response. While affinity screening can produce large numbers of potential binders, the process of confirming functional modulation and binding specificity can be time consuming. Functional screening, while mitigating these concerns, is traditionally lower throughput. The Orbit Peptide Display Platform is a bead-based technology that overcomes these challenges by being a universal high-throughput screening platform capable of being used in both affinity and functional screening contexts. We have applied the platform to the identification of peptide agonists against GPCRs and other cell surface targets. Projects can utilise the full or partial suite  of Orbits capabilities, namely:

  1. Complex membrane protein material preparation in a format representing functional conformation to ensure any binding peptides have relevance in functional assay
  2. Reporter cell line development to assess functional activation of a target or the target functional pathways (via flourescence)
  3. High throughput affinity screening using FACS to identify enriched library of peptide hits to functionally active target protein
  4. Functional screening of enriched library (from 3) against reporter cell lines (from 2) using microfluidic systems to observe biologically functional hits suitable for future optimisation
  5. validation of final hits

MC4R Screening - Presorting droplet populations of cells and beads

MC4R Screening - Droplets containing cells and beads post microfluidic sorting showing selection of MC4R agonists

Benefits of functional screening

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    Agonist and blocking screens

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    Cell surface screens

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    High throughput assay formats

If you have interest in functional screening service contact us

Find out how Orbits’s technology solution can support your drug discovery acitivities