Sep 29, 2016
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Influential Citations
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Citations
Journal
Nature Reviews Drug Discovery
Abstract
The Hippo signalling pathway has a pivotal role in regulating stem cell renewal, tissue regeneration and organ size control. Fan et al. now describe the use of an enzyme-linked immunosorbent assay (ELISA)-based high-throughput screen of a kinase-directed compound library, to identify the benzenesulfonamide-based small molecule XMU-MP-1 as a reversible, selective, ATP-competitive inhibitor of the mammalian Hippo orthologues, MST1 and MST2. In mice, intraperitoneal injection of XMU-MP-1 inhibited MST1/2 activities and promoted repair and regeneration in multiple models of intestinal and liver injury.