Ontology highlight
ABSTRACT:
SUBMITTER: Canning P
PROVIDER: S-EPMC4579271 | biostudies-literature | 2015 Sep
REPOSITORIES: biostudies-literature
Canning Peter P Ruan Qui Q Schwerd Tobias T Hrdinka Matous M Maki Jenny L JL Saleh Danish D Suebsuwong Chalada C Ray Soumya S Brennan Paul E PE Cuny Gregory D GD Uhlig Holm H HH Gyrd-Hansen Mads M Degterev Alexei A Bullock Alex N AN
Chemistry & biology 20150827 9
RIPK2 mediates pro-inflammatory signaling from the bacterial sensors NOD1 and NOD2, and is an emerging therapeutic target in autoimmune and inflammatory diseases. We observed that cellular RIPK2 can be potently inhibited by type II inhibitors that displace the kinase activation segment, whereas ATP-competitive type I inhibition was only poorly effective. The most potent RIPK2 inhibitors were the US Food and Drug Administration-approved drugs ponatinib and regorafenib. Their mechanism of action w ...[more]