Fig. 3.
Kinase inhibitor screen using the LATS-BS. a Experimental design for kinase inhibitor screen. LATS-BS was transfected into HEK293A and cells were passed into a 384-well plate the next day. Forty-eight hours after transfection, cells were treated with a kinase inhibitor library (Tocriscreen Kinase Inhibitor Toolbox) with each drug administered at 10 μM for 4 h in duplicate. Biosensor activity was measured by luciferase assay. b Heat map summarizing the results of the kinase inhibitor screen. Red color denotes drug treatments that activated the LATS-BS, whereas green color indicates treatments that inhibited the LATS-BS. c, d Validation of the top candidate drugs activating (c) or inhibiting (d) the LATS-BS from the small-scale kinase inhibitor screen. LATS-BS or STBS-luciferase reporter (YAP/TAZ/TEAD reporter) were transfected into HEK293A. Forty-eight hours after transfection, cells were treated with each inhibitor for 4 h at 10 μM. Reporter activity was measured by luciferase assay (n = 3). Data are represented as mean ± SD