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Human Kalirin/RAC1 GEF/GTPase Complex

Authors: Janine L Gray; Carmen Jimenez Antunez; Tobias Krojer; Michael Fairhead; Romain Talon; Nicola Burgess-Brown; Roger Goody; +2 Authors

Human Kalirin/RAC1 GEF/GTPase Complex

Abstract

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.

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

Keywords

KALRN, Protein, Structure Discovery, Target Enabling Package, Structure, Infectious Disease, Neuropsychiatry, Probe, Malaria, Metabolic Diseases, Oncology, Drug Discovery, Chemical Biology, Neurological Genetic Disorders, Disease, Structural Genomics, Neuro, Orphan Disease, Drug Target, RAC1, Cancer

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selected citations
These citations are derived from selected sources.
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
views
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15