Human Kalirin/RAC1 GEF/GTPase Complex
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TEP details
Summary
We have cloned, expressed, purified and crystallised the first DH GEF domain of Kalirin (gene: KALRN) in complex with RAC1 (gene: RAC1) as part of a programme to explore a new way of targeting GTPases. Fragment screening and X-ray crystallography has identified binders within the orthosteric binding site. A nucleotide exchange assay has been developed and GEF activity established.
Structures
Structures available in TEP:
- Structure of GDP-bound Kalirin/RAC1 (PDB:5O33 ): protein, ligand
- Kalirin/RAC1 in complex with fragment (PDB:5QQD ): protein, ligand
- Kalirin/RAC1 in complex with fragment (PDB:5QQE ): protein, ligand
- Kalirin/RAC1 in complex with fragment (PDB:5QQF ): protein, ligand
- Kalirin/RAC1 in complex with fragment (PDB:5QQG ): protein, ligand
- Kalirin/RAC1 in complex with fragment (PDB:5QQH ): protein, ligand
- Kalirin/RAC1 in complex with fragment (PDB:5QQI ): protein, ligand
- Kalirin/RAC1 in complex with fragment (PDB:5QQJ ): protein, ligand
- Kalirin/RAC1 in complex with fragment (PDB:5QQK ): protein, ligand
- Kalirin/RAC1 in complex with fragment (PDB:5QQL ): protein, ligand
- Kalirin/RAC1 in complex with fragment (PDB:5QQM ): protein, ligand
- Kalirin/RAC1 in complex with fragment (PDB:5QQN ): protein, ligand