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ProteomicsDifferential Chemoproteomics Reveals MARK2/3 as Cell Migration-Relevant Targets of the ALK Inhibitor Brigatinib
Metastasis poses a major challenge in cancer management, including EML4-ALK-rearranged non-small cell lung cancer (NSCLC). As cell migration is a critical step during metastasis, we assessed the anti-migratory activities of several clinical ALK inhibitors in NSCLC cells and observed differential ant...
ORGANISM(S): Homo sapiens (Human) 
2024-04-05 | PXD036716 | Pride
Anaplastic lymphoma kinase Lung cancer Brigatinib Chemical proteomics Alk 
ProteomicsCeritinib Functional Proteomics
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.
ORGANISM(S): Homo Sapiens (ncbitaxon:9606) 
2018-01-13 | MSV000081935 | MassIVE
ProteomicsIntegrative functional proteomics identifies PARP1 protein complex differences and PARP inhibitor-mediated DDR and AKT-mTOR signaling in ovarian carcinoma: Chemical Proteomics
BRCA1/2-deficient ovarian carcinoma (OC) has been shown to be particularly sensitive to PARP inhibitors (PARPis) and BRCA1/2 mutation status is currently used as a predictive biomarker for PARPi therapy. Despite eliciting major clinical benefit for the majority of patients, a significant proportion ...
ORGANISM(S): Homo sapiens (Human) 
2022-10-21 | PXD029424 | Pride
Parp1 Chemical proteomics Brca-deficient Ovarian cancer 
ProteomicsIntegrative functional proteomics identifies PARP1 protein complex differences and PARP inhibitor-mediated DDR and AKT-mTOR signaling in ovarian carcinoma: ADP-Ribosylation
BRCA1/2-deficient ovarian carcinoma (OC) has been shown to be particularly sensitive to PARP inhibitors (PARPis) and BRCA1/2 mutation status is currently used as a predictive biomarker for PARPi therapy. Despite eliciting major clinical benefit for the majority of patients, a significant proportion ...
ORGANISM(S): Homo sapiens (Human) 
2022-10-21 | PXD029428 | Pride
Ovarian cancer Adp-ribosylation Parp1 Brca 
ProteomicsCeritinib Functional Proteomics
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.
ORGANISM(S): Homo sapiens (Human) 
2018-01-12 | PXD007137 | Pride
Phosphoproteomics Chemical proteomics 
ProteomicsDifferential network analysis of ROS1 inhibitors reveals lorlatinib polypharmacology: Chemical Proteomics
Multiple tyrosine kinase inhibitors (TKIs) are often developed for the same indication. However, their relative overall efficacy is frequently incompletely understood and they may harbor unrecognized targets that cooperate with the intended target. We compared several ROS1 TKIs for inhibition of ROS...
ORGANISM(S): Homo sapiens (Human) 
2024-04-05 | PXD031690 | Pride
Polypharmacology Tyrosine kinase inhibitors Chemical proteomics Ros1 Lung cancer Lorlatinib 
ProteomicsDifferential network analysis of ROS1 inhibitors reveals lorlatinib polypharmacology: Phosphotyrosine Profiling
Multiple tyrosine kinase inhibitors (TKIs) are often developed for the same indication. However, their relative overall efficacy is frequently incompletely understood and they may harbor unrecognized targets that cooperate with the intended target. We compared several ROS1 TKIs for inhibition of ROS...
ORGANISM(S): Homo sapiens (Human) 
2024-04-05 | PXD031346 | Pride
Polypharmacology Tyrosine kinase inhibitors Phosphotyrosine Ros1 Lung cancer Lorlatinib 
ProteomicsDifferential network analysis of ROS1 inhibitors reveals lorlatinib polypharmacology: Phosphoproteomics
Multiple tyrosine kinase inhibitors (TKIs) are often developed for the same indication. However, their relative overall efficacy is frequently incompletely understood and they may harbor unrecognized targets that cooperate with the intended target. We compared several ROS1 TKIs for inhibition of ROS...
ORGANISM(S): Homo sapiens (Human) 
2024-04-05 | PXD031359 | Pride
Polypharmacology Tyrosine kinase inhibitors Phosphoproteomics Ros1 Lung cancer Lorlatinib 
ProteomicsFunctional proteomics of midostaurin in lung cancer cells: Phosphotyrosine Profiling
Lung cancer is associated with high prevalence and mortality, and despite significant successes with targeted drugs in genomically defined subsets of lung cancer and immunotherapy, the majority of patients currently does not benefit from these therapies. Through a targeted drug screen, we found the ...
ORGANISM(S): Homo sapiens (Human) 
2018-10-03 | PXD009041 | Pride
Tyrosine phosphorylation Midostaurin Lung cancer 
ProteomicsDual targeting of RET and SRC synergizes in RET fusion-positive cancer cells
RET fusions (e.g., with KIF5B, CCDC6, and NCOA4) drive subsets of non-small cell lung cancer (NSCLC) and papillary thyroid carcinoma (PTC). Despite improvements in precision therapy using selective RET tyrosine kinase inhibitors (TKIs), resistance occurs and is often driven by RET-independent bypass...
ORGANISM(S): Homo sapiens (Human) 
2025-10-22 | PXD063113 | Pride
Phosphoproteomics Lung cancer Expression proteomics Thyroid cancer Kinase inhibition Src Ret 
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