Fig. 3: Dasabuvir binds to and inhibits ROCK1 activity. | Cell Death & Disease

Fig. 3: Dasabuvir binds to and inhibits ROCK1 activity.

From: Dasabuvir suppresses esophageal squamous cell carcinoma growth in vitro and in vivo through targeting ROCK1

Fig. 3

A Molecular docking showed dasabuvir could bind to ROCK1 kinase domain. (PDB database: 2ESM) B Pull-down assay indicated dasabuvir could bind to recombinant ROCK1 protein. C, D Pull-down assays indicated dasabuvir could bind to the full-length ROCK1. E, F Pull-down assays indicated dasabuvir could bind to endogenous ROCK1. G ATP competition assay indicated dasabuvir bound to ROCK1 in an ATP competitive way. H Dasabuvir bound to WT ROCK1, but not mutant ROCK1 (Met 156, Leu 202, Asp 205) validated by the pull-down assay (upper panel). The SDS-PAGE gel showed the presence of wild type and mutant type ROCK1 proteins (lower panel). I Comparison diagram of ROCK1 sequence of different species. J In vitro kinase assay showed ROCK1 can activate ERK1, while dasabuvir can inhibit its kinase activity (upper panel). The SDS-PAGE gel showed the presence of ROCK1 and ERK1 (lower panel). K In vitro kinase assay showed ROCK1 can activate ERK2, while dasabuvir can inhibit its kinase activity (upper panel). The SDS-PAGE gel showed the presence of ROCK1 and ERK2 (lower panel).

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