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ProteomicsOff-target based drug repurposing opportunities for tivantinib in acute myeloid leukemia
GSK3alpha has been identified as a new target in the treatment of acute myeloid leukemia (AML). However, most GSK3 inhibitors lack specificity for GSK3alpha over GSK3beta and other kinases. We have previously shown in lung cancer cells that GSK3alpha and to a lesser extent GSK3beta are inhibited by ...
ORGANISM(S): Homo sapiens (Human) 
2019-01-29 | PXD010217 | Pride
Aml Tivantinib Drug pulldowns 
ProteomicsProject Name: Functional proteomics of midostaurin in lung cancer cells: Chemical Proteomics
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) 
2018-09-24 | PXD010787 | Pride
Drug pulldown Midostaurin Chemical proteomics Lung cancer 
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 
ProteomicsTarget deconvolution in Plasmodium falciparum using pulldowns
Parasite lysates were centrifuged (20,000 g, 4°C, 15 min). Beads (blank and with linker attached) were washed 3× with water then twice with lysis buffer. The lysate (~2 mg total protein) was first incubated with 2 mg blank beads for 30 min at 4°C with rotating agitation. The lysate was divided into ...
ORGANISM(S): Plasmodium falciparum (isolate 3D7) 
2022-10-15 | PXD033740 | Pride
Pulldown Plasmodium falciparum Drug target Chemical proteomics 
ProteomicsDivergent polypharmacology-driven cellular activity of structurally similar multi-kinase inhibitors through cumulative differential effects on individual targets: Drug Pulldowns
Despite recent successes of precision and immunotherapies there is a persisting need for novel targeted or multi-targeted approaches in complex diseases. Through a systems pharmacology approach including phenotypic screening, chemical and phosphoproteomics and RNA-Seq, we elucidated the targets and ...
ORGANISM(S): Homo sapiens (Human) 
2019-06-24 | PXD012961 | Pride
Cabozantinib Chemical proteomics Polypharmacology Foretinib Lung cancer 
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 
ProteomicsThermal proteome profiling of MMV897615
The target deconvolution of MMV897615 was evaluated using thermal proteome profiling (TPP), a chemical proteomics approach based on the stabilisation of protein targets upon ligand binding. In these TPP experiments we used a whole-cell strategy, exposing cells rather than lysates to the drug
ORGANISM(S): Plasmodium falciparum (isolate 3D7) 
2023-03-09 | PXD034937 | Pride
Acyl-coa synthetases Drug target Thermal proteome profiling Plasmodium falciparum 
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 
ProteomicsDiazirine photo-immobilisation for target profiling of natural products and co-factors: pulldown data
Finding the targets of natural products is of key importance in both chemical biology and drug discovery, and deconvolution of cofactor interactomes contribute to the functional annotation of the proteome. Identifying the proteins that underlie natural compound activity in phenotypic screens help to...
ORGANISM(S): Homo sapiens (Human) Escherichia coli 
2022-10-06 | PXD033292 | Pride
Photo-immobilisation Pulldowns Natural products profiling Natural products targets 
ProteomicsProbing tyrosine kinase inhibitors specificity
Using a three-pronged MS-based proteomic approach, we assessed the mode-of-action of four clinically-relevant tyrosine kinase inhibitors in an epithelial cancer cell line. Here we defined the: (I) semi-quantitative tyrosine kinome; (II) drug interactome; and (III) drug-induced effects on the tyrosin...
ORGANISM(S): Homo sapiens (Human) 
2014-05-12 | PXD000681 | Pride
Human Tyrosine kinase inhibitors Chemical proteomics Phosphoproteomics Phosphotyrosine Lc-ms/ms 
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