Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction
Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction
Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction
Aidan G Gilmartin, Thomas H Faitg, Mark Richter, Arthur Groy, Mark A Seefeld, Michael G Darcy, Xin Peng, Kelly Federowicz, Jingsong Yang, Shu-Yun Zhang, Elisabeth Minthorn, Jon-Paul Jaworski, Michael Schaber, Stan Martens, Dean E McNulty, Robert H Sinnamon, Hong Zhang, Robert B Kirkpatrick, Neysa Nevins, Guanglei Cui, Beth Pietrak, Elsie Diaz, Amber Jones, Martin Brandt, Benjamin Schwartz, Dirk A Heerding & Rakesh Kumar
Published online: 05 January 2014 | doi:10.1038/nchembio.1427
Allosteric small-molecule inhibitors of the p53-induced oncogenic phosphatase Wip1 bind at a ‘flap’ subdomain near the catalytic site. Inhibitor GSK2830371 inhibits the phosphatase and oncogenic activities in cell lines and a xenograft tumor model.