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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 (ncbitaxon:9606)

SUBMITTER: Uwe Rix

PROVIDER: MSV000081935 | MassIVE | Sat Jan 13 11:14:00 GMT 2018

SECONDARY ACCESSION(S): PXD007137

REPOSITORIES: MassIVE

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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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Dual-mechanism ERK1/2 inhibitors exploit a distinct binding mode to block phosphorylation and nuclear accumulation of ERK1/2, resulting in enhanced potency

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