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ProteomicsProteomics analysis with the Aurora-A PROTAC, JB170
The mitotic kinase Aurora-A is essential for cell cycle progression and considered a priority cancer target. Dozens of ongoing clinical trials are testing the anti-cancer potential of Aurora-A kinase inhibitors. While the catalytic activity of Aurora-A is essential for its function during mitosis, a...
ORGANISM(S): Homo sapiens (Human) 
2020-09-28 | PXD019585 | Pride
Proteomics analysis with the aurora-a protac Jb170 
ProteomicsProteomics analysis with the Aurora-A PROTAC, JB170
To determine specificity of Aurora-A PROTAC (JB170), MV4-11 cells were labeled with medium containing different stable isotopes (SILAC), treated them with JB170 or Alisertib and subsequently compared their protein content to untreated cells by quantitative mass spectrometry.
ORGANISM(S): Homo sapiens (Human) 
2020-09-28 | PXD017342 | Pride
Aurora-a Protac Mv4-11 Degronimid Jb170 
ProteomicsIdentification of AURORA A interaction partners
The oncogenic kinase AURORA A is essential for mitotic progression, and its catalytic inhibition arrests cells at the G2/M-transition. Unexpectedly, partial degradation of AURORA A by PROTACs (proteolysis targeting chimeras) induces profound S-phase defects, revealing a non-catalytic scaffolding fun...
ORGANISM(S): Homo sapiens (Human) 
2026-06-03 | PXD069843 | Pride
Coip Interactome 
ProteomicsNovel, highly potent PROTACs targeting AURORA-A kinase
The family of AURORA kinases is essential for cell cycle progression and dysregulation of AURORA-A in cancer led to a large number of clinical and pre-clinical inhibitors. However, ATP competitive AURORA-A inhibitors usually do not target non-catalytic functions that have also been identified as mec...
ORGANISM(S): Homo sapiens (Human) 
2023-09-14 | PXD033239 | Pride
Lc-msms Aurka Protac Protein degrader 
ProteomicsTargeted AURKA degradation: Towards new therapeutic agents for neuroblastoma
Aurora kinase A (AURKA) is a well-established target in neuroblastoma (NB) due to both its catalytic functions during mitosis and its kinase-independent functions, including stabilization of the key oncoprotein MYCN. We present a structure-activity relationship (SAR) study of MK-5108-derived PROTACs...
ORGANISM(S): Homo sapiens (Human) 
2023-02-27 | PXD040389 | Pride
Aurka  mycn  neuroblastoma  protac  targeted protein degradation 
ProteomicsDCAF1-based PROTACs with activity against clinically validated targets overcoming intrinsic- and acquired-degrader resistance
Targeted protein degradation (TPD) mediates protein level through small molecule induced redirection of E3 ligases to ubiquitinate neo-substrates and mark them for proteasomal degradation. TPD has recently emerged as a key modality in drug discovery. So far only a few ligases have been utilized for ...
ORGANISM(S): Homo sapiens (Human) 
2023-12-18 | PXD046286 | Pride
Tmt Dcaf1 Tpd Protac 
ProteomicsTargeted AURKA degradation: Towards new therapeutic agents for neuroblastoma
Aurora kinase A (AURKA) is a well-established target in neuroblastoma (NB) due to both its catalytic functions during mitosis and its kinase-independent functions, including stabilization of the key oncoprotein MYCN. We present a structure-activity relationship (SAR) study of MK-5108-derived PROTACs...
ORGANISM(S): Homo sapiens (Human) 
2023-02-27 | PXD040391 | Pride
Aurka  mycn  neuroblastoma  protac  targeted protein degradation 
ProteomicsSystematic Proteome-Wide Target Interrogation of PROTAC activity by High-Throughput DIA-MS on the Orbitrap Astral Platform
An efficient degradation-based proteomics workflow was established using data-independent acquisition-mass spectrometry (DIA-MS) and the Orbitrap Astral platform to investigate the mode of actions (MOA) and on target specificity of bromodomain and extra-terminal (BET) protein-targeting PROTACs, MZ1 ...
ORGANISM(S): Homo sapiens (Human) 
2026-03-05 | PXD069438 | Pride
Proteomics Dia-ms Bromodomain containing proteins Orbitrap astral Proteolysis targeting chimeras 
ProteomicsA Gold-PROTAC degrades the oncogenic tyrosine kinase MERKT: Insights into the degradome from a steady-state system
Targeted protein degradation is a valuable strategy to eliminate disease-relevant proteins. Among other classes, proteolysis targeting chimeras (PROTACs) are bifunctional molecules that induce the proximity of a recruiter E3 ligase and the target protein of interest for ubiquitination and subsequent...
ORGANISM(S): Homo sapiens (Human) 
2026-07-27 | PXD067054 | Pride
Cancer  degradome  metallo-protac  protac  protein half-life  targeted protein degradation 
ProteomicsccRCC cells treated with DMSO or UNC8209
Clear cell renal cell carcinoma (ccRCC), the most common kidney cancer subtype, often features inactivation of the VHL tumor suppressor, creating therapeutic vulnerabilities. Although HIF2α inhibitors have shown promise, many VHL-deficient tumors remain resistant. TANK-binding kinase 1 (TBK1) has be...
ORGANISM(S): Homo sapiens (Human) 
2026-03-10 | PXD071969 | Pride
Lc-msms Protac Tbk1 Ccrcc 
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