Human SET domain bifurcated 1 (SETDB1), Tudor domain
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TEP details
Summary
SETDB1 is a H3K9 methyltransferase that features a triple Tudor domain, is recurrently amplified in lung cancer, and its depletion reduces cancer growth in vitro and in vivo. No inhibitor was reported to date. Here we present crystal structures of 5 compounds in complex with the Tudor domain of SETDB1 with associated binding assays by HSQC NMR, SPR and ITC. These compounds should be optimized into a chemical probe to be tested against SETBD1 amplified cancer cells.
Structures
Structures available in TEP:
- Structures SETDB1 Tudor domain in complex with fragments (PDB:5KH6 ): protein, ligand
- Structures SETDB1 Tudor domain in complex with fragments (PDB:5KCO ): protein, ligand
- Structures SETDB1 Tudor domain in complex with fragments (PDB:5KCH ): protein, ligand
- Structures SETDB1 Tudor domain in complex with fragments (PDB:5KE2 ): protein, ligand
- Structures SETDB1 Tudor domain in complex with fragments (PDB:5KE3 ): protein, ligand