Ontology highlight
ABSTRACT:
SUBMITTER: Ohbayashi N
PROVIDER: S-EPMC6129943 | biostudies-literature | 2018 Sep
REPOSITORIES: biostudies-literature
ChemistryOpen 20180910 9
Gefitinib is the molecular target drug for advanced non-small-cell lung cancer. The primary target of gefitinib is the positive mutation of epidermal growth factor receptor, but it also inhibits cyclin G-associated kinase (GAK). To reveal the molecular bases of GAK and gefitinib binding, structure analyses were conducted and determined two forms of the gefitinib-bound nanobody⋅GAK kinase domain complex structures. The first form, GAK_1, has one gefitinib at the ATP binding pocket, whereas the se ...[more]