Pawel Leznicki’s Post

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Associate Principal Scientist, Sygnature Discovery

Kinases in motion…. Interesting adaptation of an enzyme complementation assay where the same protein is fused to two fragments of Renilla luciferase, one at each of the target protein's ends. As a result, luciferase complementation that leads to bioluminescence can be used to monitor conformational changes in the studied protein. This system, called Kinase Conformation (KinCon) reporter assay, has been used before but in the current study published in eLife Sciences Publications, Ltd., Eduard STEFAN and colleagues extend its application to monitoring changes in kinase conformations in response to partner protein and small molecule binding as well as to study consequences of disease-associated mutations. The kinases chosen as case studies include LKB1, BRAF, RIPK1 and CDK6, and so this method of identifying compounds that trigger opening or closing of these kinases is of interest to researchers working in the field of cancer and inflammation. Link to the paper: https://lnkd.in/e9VcqyrM #DrugDiscovery, #Cancer, #Inflammation

Kinases in motion: impact of protein and small molecule interactions on kinase conformations

Kinases in motion: impact of protein and small molecule interactions on kinase conformations

elifesciences.org

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