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- W2980848095 abstract "Abstract LIM domain kinase 1 (LIMK1) is a key regulator of actin dynamics. It is thereby a potential therapeutic target for the prevention of fragile X syndrome and amyotrophic lateral sclerosis. Herein, we use X-ray crystallography and activity assays to describe how LIMK1 accomplishes substrate specificity, to suggest a unique ‘rock-and-poke’ mechanism of catalysis and to explore the regulation of the kinase by activation loop phosphorylation. Based on these findings, a differential scanning fluorimetry assay and a RapidFire mass spectrometry activity assay were established, leading to the discovery and confirmation of a set of small-molecule LIMK1 inhibitors. Interestingly, several of the inhibitors were inactive towards the closely related isoform LIMK2. Finally, crystal structures of the LIMK1 kinase domain in complex with inhibitors (PF-477736 and staurosporine, respectively) are presented, providing insights into LIMK1 plasticity upon inhibitor binding." @default.
- W2980848095 created "2019-10-25" @default.
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- W2980848095 date "2019-11-05" @default.
- W2980848095 modified "2023-10-14" @default.
- W2980848095 title "Lessons from LIMK1 enzymology and their impact on inhibitor design" @default.
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- W2980848095 doi "https://doi.org/10.1042/bcj20190517" @default.
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