Human Kalirin/RAC1 GEF/GTPase Complex
Description
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.
Resources
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http://data.europa.eu/88u/dataset/oai-zenodo-org-3271348 |
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http://data.europa.eu/88u/dataset/oai-zenodo-org-3271348 |
Tags
- neuropsychiatry
- disease
- neurological-genetic-disorders
- structural-genomics
- target-enabling-package
- metabolic-diseases
- structure
- malaria
- structure-discovery
- drug-target
- probe
- protein
- orphan-disease
- chemical-biology
- rac1
- kalrn
- cancer
- drug-discovery
- infectious-disease
- oncology
- neuro