Ontology highlight
ABSTRACT:
SUBMITTER: Brenner RJ
PROVIDER: S-EPMC10904212 | biostudies-literature | 2023 Nov
REPOSITORIES: biostudies-literature
Brenner Robert J RJ Landgraf Alexander D AD Bum-Erdene Khuchtumur K Gonzalez-Gutierrez Giovanni G Meroueh Samy O SO
Biochemistry 20231108 22
KRAS GTPases harbor oncogenic mutations in more than 25% of human tumors. KRAS is considered to be largely undruggable due to the lack of a suitable small-molecule binding site. Here, we report a unique crystal structure of His-tagged KRAS<sup>G12D</sup> that reveals a remarkable conformational change. The Switch I loop of one His-KRAS<sup>G12D</sup> structure extends into the Switch I/II pocket of another His-KRAS<sup>G12D</sup> in an adjacent unit cell to create an elaborate interface that is ...[more]