Drug Target Validation | Structural Proteomics

Drug Target Validation

Reveal your compound’s binding site with structural proteomics at peptide-level resolution

Biognosys’ novel Drug Target Validation service offers a unique way to confidently characterize a drug’s binding site and de-risk early drug development. By using our High Resolution Limited Proteolysis (HR-LiP) technology coupled with Mass Spectrometry, we remove the need for molecule tagging, protein modifications, or recombinant proteins. All we need is a cell line overexpressing your target of interest and a stock of your compound.

    Description

    Validating the target of a small molecule compound is key to both de-risking research pipelines and shortening a drug’s time to market. It can be achieved by confidently characterizing the compound’s binding site in its protein target. This provides valuable insights that can guide compound optimization.

    Our Drug Target Validation solution is part of our TrueTarget™ platform offering. Biognosys’ TrueTarget platform uses peptide-level information to enable both drug target deconvolution (LiP-MS) and further compound binding site characterization (HR-LiP) in a label-free manner. Collectively, these technologies empower drug discovery and optimization.

    The Drug Target Validation service can be performed on every kind of protein from all species in a near-native environment. Furthermore, traditionally difficult-to-characterize proteins, such as those with a high molecular mass or membrane localization, can be analyzed in their full length.

    In contrast to conventional structural biology techniques such as crystallography, our Drug Target Validation service leverages structural proteomics and offers a cost-efficient alternative with a few weeks of project turnaround time.

    Biognosys is the sole provider of proteomics solutions based on the patented LiP-MS technology, developed in collaboration with Prof. Paola Picotti Group at ETH Zurich.

    “Biognosys’ TrueTarget platform was instrumental in identifying our target protein’s binding site and in this way provided valuable mechanistic insights that helped us to understand the underlying biology of our observed phenotype.”

    Prof. David Rubinsztein
    Professor of Molecular Neurogenetics, UK Dementia Research Institute Group Leader at the University of Cambridge, and Deputy Director of the Cambridge Institute for Medical Research.

    Resources

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    Deliverables

    The results are presented and discussed with you in a seminar or webinar and delivered electronically in PDF and Excel formats.

    Executive Summary
    Materials and Methods
    (suitable for publication)
    Complete Data Matrix

    Peptide intensities across dose-response treatment

    Target Deconvolution Analysis

    a) Protein target candidate peptides ranked by dose-response correlation

    b) Compound affinity concentration for each peptide candidate

    c) Mapping of peptide candidates and predicted binding location on tertiary protein structures if available

    Sample types and depths

    Drug Target Validation is applicable to complex biological matrices, including a wide variety of cell lines and organisms.

    SAMPLE REQUIREMENTS

    Project management

    Biognosys is committed to providing the best possible results to our customers at the fastest possible project turnaround time.

    WORKING WITH US

    Helpdesk

    Access our knowledge base with relevant resources and guiding information.

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