In-vivo target response analysis platform (INTRAP) for bifunctional ligand screening

Overview

INTRAP® is an innovative high-throughput screening technology developed for in vivo analysis of binders targeting specific protein pockets. This platform enables the identification of high-affinity binders by utilizing a competition assay between a tracer probe and potential binders within living cells. The technology is particularly effective for designing bifunctional small molecules that can modify protein-protein interactions (PPI) or recruit proteins, offering significant applications in drug discovery and development.

Technical specifications

• Tracer Probe Design: Tracer probes are designed based on known or AI-generated ligands for specific protein pockets.
• High-Throughput Screening: The competition assay measures the ability of binders to inhibit the tracer probe signal, indicating their affinity.
• Bifunctional Molecule Development: Identified binders are used to design small molecules that can alter PPI or recruit specific proteins.
• Validation Methods: INTRAP assays are complemented by biological experiments such as Western Blotting (WB) and Co-Immunoprecipitation (co-IP) to verify the regulatory effects of bifunctional molecules.

Technology readiness level

This technology is currently at TRL 3, having been experimentally validated at the proof-of-concept stage in living cell systems. Ongoing development aims to enhance its applicability in drug discovery.