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.

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