Ontology highlight
ABSTRACT:
SUBMITTER: Woessner DW
PROVIDER: S-EPMC4621806 | biostudies-literature | 2015 Aug
REPOSITORIES: biostudies-literature
Woessner D W DW Eiring A M AM Bruno B J BJ Zabriskie M S MS Reynolds K R KR Miller G D GD O'Hare T T Deininger M W MW Lim C S CS
Leukemia 20150227 8
Targeted therapy of chronic myeloid leukemia (CML) is currently based on small-molecule inhibitors that directly bind the tyrosine kinase domain of BCR-ABL1. This strategy has generally been successful, but is subject to drug resistance because of point mutations in the kinase domain. Kinase activity requires transactivation of BCR-ABL1 following an oligomerization event, which is mediated by the coiled-coil (CC) domain at the N terminus of the protein. Here, we describe a rationally engineered ...[more]