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Ceritinib Functional Proteomics

ABSTRACT: To elucidate the mechanism of action (MoA) of ceritinib’s antiproliferative activity in these cells, we applied a systems approach combining both chemical and phosphoproteomics to gain a global view of ceritinib’s target profile and network-wide phosphorylation changes following ceritinib treatment.

INSTRUMENT(S): LTQ Orbitrap, Q Exactive

ORGANISM(S): Homo Sapiens (human)

TISSUE(S): Lung

SUBMITTER: Brent Kuenzi

LAB HEAD: Uwe Rix

PROVIDER: PXD007137 | Pride | 2018-01-12

REPOSITORIES: Pride

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			Action	DRS
	20150216_Rix_PD418.RAW	Raw
	20150216_Rix_PD418.RAW (F031615).mzid_20150216_Rix_PD418.RAW_(F031615).pride.mgf.gz	Mzid
	20150216_Rix_PD418.RAWF031615.mzid.gz	Mzid
	20150216_Rix_PD418.RAWF031615.mzid_20150216_Rix_PD418.RAW_F031615.MGF	Mzid
	20150216_Rix_PD419.RAW	Raw

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Publications

Polypharmacology-based ceritinib repurposing using integrated functional proteomics.

Kuenzi Brent M BM Remsing Rix Lily L LL Stewart Paul A PA Fang Bin B Kinose Fumi F Bryant Annamarie T AT Boyle Theresa A TA Koomen John M JM Haura Eric B EB Rix Uwe U

Nature chemical biology 20171009 12

Targeted drugs are effective when they directly inhibit strong disease drivers, but only a small fraction of diseases feature defined actionable drivers. Alternatively, network-based approaches can uncover new therapeutic opportunities. Applying an integrated phenotypic screening, chemical and phosphoproteomics strategy, here we describe the anaplastic lymphoma kinase (ALK) inhibitor ceritinib as having activity across several ALK-negative lung cancer cell lines and identify new targets and netw ...[more]

PMID: 28991240

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