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Target Enabling Packages (TEPs)logo

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

 

GeneDescriptionTherapeutic Area
ACRV1 Activin A receptor, type I (ACVR1) Inflammation and Oncology
NSP15 SARS-CoV-2 Nidoviral RNA Uridylate‐Specific Endoribonuclease (NSP15) Infectious diseases
NSP13 SARS-CoV-2 NSP13 Infectious diseases
SLC12A4/SLC12A6 Potassium/Chloride Co-transporter 1 and 3 (KCC1/KCC3; SLC12A4/SLC12A6) Sickle cell disease (SCD), Neurological
EPB41L3 EPB41L3 Neurodegeneration
INPP5D INPP5D (SHIP1) Neurological Disorders
Moesin MSN (Moesin) Alzheimer’s disease
TNC Fibrinogen-like globe domain of human Tenascin-C (hFBG-C) Inflammatory diseases
ELOVL7 Elongation of very long chain fatty acids protein 7 (ELOVL7) Metabolic diseases
DHTKD1 Dehydrogenase E1 and transketolase domain-containing protein 1 (DHTKD1) Metabolic diseases
DCLRE1C Artemis (DCLRE1C, SNM1C) Oncology
TBXT Human T-box transcription factor T (Brachyury) Cancer
KLHL20 Human Kelch-like protein 20 (KLHL20) Cancer, Neuropsychiatry
STAG1 Human Stromal Antigen 1 (STAG1) Cohesin Subunit SA-1 Cancer
KEAP1 Human Kelch-like ECH Associated Protein 1 (KEAP1) Neuropsychiatry
TMEM16K Human TMEM16K (ANO10) Neurological Disorders
TASK1 TWIK-Related Acid-Sensitive K+ Channel 1 (TASK1) Neurological Disorders
MTHFR Methylene-Tetrahydrofolate Reductase (MTHFR) Metabolic disorders, Cancer
ALAS2 5'-Aminolevulinate synthase, erythoid-specific (ALAS2) Metabolic disorders
KALRN/RAC1 Human Kalirin/RAC1 GEF/GTPase Complex Neurological Disorders
PARP14 Human Poly (ADP-ribose) Polymerase Family Member 14 (PARP14) Cancer, Inflammation
GALT/GALK1 Human Galactose-1-phosphate uridylyltransferase (GALT), Galactokinase 1 (GALK1) Metabolic diseases
RIPK2 Human Receptor-Interacting Serine/Threonine-Protein Kinase 2 (RIPK2) Inflammatory diseases
NUDT7 Human Peroxisomal Coenzyme A Diphosphatase NUDT7 (NUDT7) Metabolic diseases
MLLT1 Human Mixed- Lineage Leukemia, Translocated to 1 (MLLT1) Cancer (Acute Myeloid Leukaemia)
HCN4 Hyperpolarization Activated Cyclic Nucleotide Gated Ion Channel 4 (HCN4) Cardiovascular, Inflammation (homologue of HCN2, an inflammatory pain target), Neuropsychiatry and neuro genetic disorders
HAO1 Human Hydroxyacid Oxidase (HAO1) Metabolic disorders
FAM83B Human Family With Sequence Similarity 83 Member B (FAM83B) Cancer
LIMK1 Human LIM Domain Kinase 1 (LIMK1), Kinase Domain Neuropsychiatry
DCLRE1A Human DNA Cross-Link Repair 1A (DCLRE1A, SNM1A) Cancer
DPAGT1 Human Dolichyl-Phosphate Alpha-N-Acetyl glucosaminyl transferase (DPAGT1) Neuropsychiatry and neuro genetic disorders
AASS Human Alpha-Aminoadipic Semialdehyde Synthase (AASS) Metabolic & Neurological disorders
WNK3 Human With No Lysine Kinase 3 (WNK3) Metabolic diseases
KDM3B Lysine Demethylase JMJD1B (KDM3B) Cancer
KDM4D Lysine Demethylase JMJD2D (KDM4D) Cancer
PHIP Human Pleckstrin Homology Domain Interacting Protein (PHIP) Cancer
RECQL5 Human RECQL5 helicase Cancer
CDK12 Human Cyclin-Dependent Kinase 12 (CDK12), Kinase Domain Oncology