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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
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
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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