Target Enabling Packages (TEPs)
Published June 13, 2019 | Version 2
Dataset Open

Human Kalirin/RAC1 GEF/GTPase Complex

Authors/Creators

  • 1. Structural Genomics Consortium, Nuffield Department of Medicine, University of Oxford
  • 2. Diamond Light Source
  • 3. Structural Genomics Consortium
  • 4. Max Plank Institute of Molecular Physiology, Dortmund

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.

Notes

This document represents version 2 of the TEP datasheet and includes all updates on the project as of October 2020. For more information about TEPs and the TEP Programme, please visit https://thesgc.org/tep

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KALRN_RAC1_TEP_datasheet_v2.pdf

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Additional details

Related works

Is part of
https://www.thesgc.org/tep (URL)

Funding

European Commission
ULTRA-DD - Unrestricted Leveraging of Targets for Research Advancement and Drug Discovery 115766
Wellcome Trust
A UK Hub to Catalyse Open Target Discovery. 106169