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

Name Format Description Link
0 http://data.europa.eu/88u/dataset/oai-zenodo-org-3271348
0 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

Topics

Categories