Target Enabling Packages

Well-validated genetic hits provide a rich source of potential drug targets. Realising this potential requires a deep understanding of the molecular basis of the disease. Narrowing the gap between genetic discovery and new therapeutics relies on the availability of high quality, target-specific research tools.

Here, we provide, free to the community, a selection of Target Enabling Packages (TEPs). TEPs are peer-reviewed tool kits for potential drug targets, produced through collaboration between geneticists, biochemists, medicinal chemists and clinicians. Each TEP includes methods, reagents and knowledge of a protein target, allowing for rapid uptake to a medicinal chemistry campaign.

Each TEP contains:

• Protein production methods
• Biochemical/biophysical assays for activity, affinity
• Structures of the protein, potentially including wild type and disease mutant proteins; full-length or domains; protein-ligand complexes; structures of close homologues
• Initial chemical matter from a fragment or small molecule screen

Additional components of TEPs may be developed on a case-by-case basis, based upon reasonable scientific need, in collaboration with TEP target nominators:

• An antibody or nanobody
• Cell-based assay
• CRISPR knockout

For more information on the TEPs programme, or to pursue a medicinal chemistry collaboration on an available TEP, please contact: teps@cmd.ox.ac.uk