Figure 4: Interaction of KPT-6566 with PIN1 promotes its structural change and degradation.
From: A covalent PIN1 inhibitor selectively targets cancer cells by a dual mechanism of action
Immunoblotting of the indicated proteins in cell lysates from (a) MDA-MB-231 cells treated with the indicated compounds (+) or DMSO (−) for 48 h; (b) PC3, PANC1 and H1299 cells treated with 5 μM KPT-6566 (+) or DMSO (−) for 48 h; (c) PIN1 KO MDA-MB-231 cells transduced with empty (−) or PIN1 vectors (+) treated with 5 μM KPT-6566 (+) or DMSO (−) for 48 h; (d) PIN1 KO MDA-MB-231 cells reconstituted with HA-PIN1, treated with increasing amounts of KPT-6566 or DMSO; (e) PIN1 KO MDA-MB-231 cells reconstituted with HA-PIN1, treated with 5 μM KPT-6566 (+) or DMSO (−) followed by cycloheximide (CHX) chase for the indicated hours; (f) PIN1 KO MDA-MB-231 cells reconstituted with HA-PIN1, treated with 5 μM KPT-6566 (+), 10 μM MG132 (+) or DMSO (−) for 16 h. a–f Actin levels are reported as loading control; size markers are indicated.
