Proteomics

Dataset Information

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Mechanistic insight into RET kinase inhibitors targeting the DFG-out conformation in RET-rearranged cancer

ABSTRACT: We used quantitative (phospho)proteomics to study how cells may escape the activity of RET kinase inhibitors.

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

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Dataset's files

Source:
Action DRS
ISAS_131_02_01_TiO2_Phosphoenriched.msf Msf
ISAS_131_02_01_pH8_GlobalProteome.msf Msf
ISAS_131_02_01_pH8_GlobalProteome_Proteins.xlsx Xlsx
LC10_AD80_phosphoproteomics_full.xlsx Xlsx
qExHF01_03179_ISAS_131_02_01_pH8_F5.raw Raw
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Publications

Drugging the catalytically inactive state of RET kinase in RET-rearranged tumors.

Plenker Dennis D   Riedel Maximilian M   Brägelmann Johannes J   Dammert Marcel A MA   Chauhan Rakhee R   Knowles Phillip P PP   Lorenz Carina C   Keul Marina M   Bührmann Mike M   Pagel Oliver O   Tischler Verena V   Scheel Andreas H AH   Schütte Daniel D   Song Yanrui Y   Stark Justina J   Mrugalla Florian F   Alber Yannic Y   Richters André A   Engel Julian J   Leenders Frauke F   Heuckmann Johannes M JM   Wolf Jürgen J   Diebold Joachim J   Pall Georg G   Peifer Martin M   Aerts Maarten M   Gevaert Kris K   Zahedi René P RP   Buettner Reinhard R   Shokat Kevan M KM   McDonald Neil Q NQ   Kast Stefan M SM   Gautschi Oliver O   Thomas Roman K RK   Sos Martin L ML  

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]

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