Dataset Information
Mechanistic insight into RET kinase inhibitors targeting the DFG-out conformation in RET-rearranged cancer
Ontology highlight
ABSTRACT:
OTHER RELATED OMICS DATASETS IN: EGAC00001000064EGAS00001002335EGAD00001003316EGAO00000000020EGAO00000000078EGAO00000000086
INSTRUMENT(S): Q Exactive
ORGANISM(S): Homo Sapiens (human)
TISSUE(S): Cell Culture
SUBMITTER: 
René Zahedi
LAB HEAD: René Zahedi
PROVIDER: PXD006006 | Pride | 2017-06-21
REPOSITORIES: Pride
Dataset's files
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Publications
Drugging the catalytically inactive state of RET kinase in RET-rearranged tumors.
Science translational medicine 20170601 394
Oncogenic fusion events have been identified in a broad range of tumors. Among them, <i>RET</i> rearrangements represent distinct and potentially druggable targets that are recurrently found in lung adenocarcinomas. We provide further evidence that current anti-RET drugs may not be potent enough to induce durable responses in such tumors. We report that potent inhibitors, such as AD80 or ponatinib, that stably bind in the DFG-out conformation of RET may overcome these limitations and selectively ...[more]
