Ontology highlight
ABSTRACT:
SUBMITTER: Kuglstatter A
PROVIDER: S-EPMC3048427 | biostudies-literature | 2011 Feb
REPOSITORIES: biostudies-literature
Kuglstatter Andreas A Wong April A Tsing Stan S Lee Simon W SW Lou Yan Y Villaseñor Armando G AG Bradshaw J Michael JM Shaw David D Barnett Jim W JW Browner Michelle F MF
Protein science : a publication of the Protein Society 20110201 2
Bruton's tyrosine kinase (BTK) plays a key role in B cell receptor signaling and is considered a promising drug target for lymphoma and inflammatory diseases. We have determined the X-ray crystal structures of BTK kinase domain in complex with six inhibitors from distinct chemical classes. Five different BTK protein conformations are stabilized by the bound inhibitors, providing insights into the structural flexibility of the Gly-rich loop, helix C, the DFG sequence, and activation loop. The con ...[more]