DIANA for drug discovery

Application

In drug discovery, DIANA is used for screening of enzyme inhibitors or ligands of target protein. In this setup, screened compounds compete with the probe for target binding. It offers sensitive hit discovery (ultra-low false-positive and false-negative rate) while providing direct quantification of the compound’s inhibition potency. It also allows highly efficient screening of pooled libraries leading to reduced screening cost and time. This makes it suitable for both large pharma high-throughput-screening facilities and smaller-scale projects at academic institutions (in-house libraries of ~10k compounds can be screened in just few 96-well plates).

Overview presentation – DIANA for drug discovery

DIANA screening assay-Overview-170727

 

Advantages

In screening the major DIANA benefits are:

  • Extremely high signal to noise ratio (Z’ > 0.9; CV < 5%)
  • Quantitative – compound potency directly measured from a single well, hits ranked by inhibition potency, easy to screen for specificity in protein family
  • Sensitive hit discovery, ultra-low false-positive and false-negative rate
  • Robust – no need for recombinant and/or purified proteins, no interference or non-specific binding
  • Cost-efficient – very low compound and target protein consumption (typically picograms of protein needed) and ability to screen inhibitors in pooled compound libraries (reducing ~10-times number of screen runs required)

 Experimental protocol

  • 4-step easy to implement experimental protocol 

Portfolio of clinically relevant targets

Screening assay developed:

  • Prostate Specific Membrane Antigen (PSMA/GCPII)
  • Glutamate carboxy peptidase III (GCPIII)
  • Carbonic anhydrases 7 and 9 (CA-VII and CA-IX)
  • Fibroblast activating protein (FAP)
  • MutT homologue 1 (MTH1)
  • Influenza neuraminidase
  • Insulin receptor
  • Fc receptor (CD64)

R&D pipeline:

  • Carbonic anhydrase family
  • Hydroxysteroid dehydrogenases
  • Insulin growth factor receptors
  • Kinase panel
  • DNA Methyltransferases
  • Aspartic protease family
  • Influenza polymerase
  • C-myc promoter quadruplex

Custom assay development

Assay can be promptly developed on demand to majority of relevant protein targets - potential for collaborative projects

Interested in using DIANA to screen for inhibitors/ligands of your target protein?

  • Please do not hesitate to reach to us to discuss further details