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ProteomicsDiscovery of dedicated EPHA2 inhibitors - Medicinal chemistry meets chemical proteomics
The receptor tyrosine kinase EPHA2 has gained interest as therapeutical drug target in cancer and infectious diseases in the past years. However, EPHA2 research and EPHA2 based therapies have been hampered by the lack of selective small molecule EPHA2 inhibitors. We report on the synthesis and evalu...
ORGANISM(S): Homo sapiens (Human) 
2017-05-30 | PXD006193 | Pride
Eph receptor Drug discovery Selectivity profiling Inhibitors Chemical proteomics 
ProteomicsDefining the landscape of EPHA2 Inhibition by Clinical Kinase Inhibitors
The receptor tyrosine kinase EPHA2 plays important roles in oncogenesis, metastasis and treatment resistance but therapeutic targeting, drug discovery or investigation of EPHA2 biology is hampered by the lack of appropriate inhibitors and structural information on how these interact with the protein...
ORGANISM(S): Homo sapiens (Human) 
2016-12-23 | PXD004112 | Pride
Epha2 co-crystals Selectivity profiling Chemical proteomics Residue categorization Drug protein interactions 
UnknownAURORA A interacts with DICER and SETD2 to promote S-phase progression
Not available
S-SCDT-10_1038-S44319-026-00850-0 | biostudies-other
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 
ProteomicsThe formation of a camalexin-biosynthetic metabolon
Arabidopsis thaliana efficiently synthesizes the antifungal phytoalexin camalexin without apparent release of bioactive intermediates, such as indole-3-acetaldoxime, suggesting channeling of the biosynthetic pathway involving an enzyme complex. To identify such protein interactions, two independent ...
ORGANISM(S): Arabidopsis thaliana (Mouse-ear cress) 
2019-08-26 | PXD008812 | Pride
Camalexin Cytochrome p450 
ProteomicsChemical phosphoproteomic approaches reveal substrate specificity of protein phosphatases-1 and -2
The phosphatases PP1 and PP2A are responsible for the majority of dephosphorylation reactions on phosphoserine (pS) and –threonine (pT), and are involved in basically all cellular processes and many related diseases. They are thought to have no appreciable intrinsic substrate specificity, but to gai...
ORGANISM(S): Homo sapiens (Human) 
2020-07-14 | PXD012026 | Pride
Co-immunoprecipitation Phosphatase substrates Quantitative phosphoproteomics 
TranscriptomicsFOXO1/3 and PTEN Depletion in Granulosa Cells Promotes Ovarian Granulosa Cell Tumor Development
The Forkhead Box, FOXO1 and FOXO3, transcription factors regulate multiple functions in mammalian cells. Selective inactivation of the Foxo1 and Foxo3 genes in murine ovarian granulosa cells severely impairs follicular development and apoptosis causing infertility, and as shown herein, granulosa cel...
ORGANISM(S): Mus musculus 
2015-06-17 | E-GEOD-67662 | biostudies-arrayexpress
ProteomicsPROTAC-triggered degradation of MYC
The oncogene MYC drives many cancers and is an outstanding therapeutic target. MYC is an intrinsically disordered protein, and therefore, targeting MYC remains a challenge. Here, we developed a proteolysis targeting chimera (PROTAC) degrading MYC: MDEG-541. The inhibitor is based on the MYC-MAX dim...
ORGANISM(S): Homo sapiens (Human) 
2022-05-12 | PXD018674 | Pride
Lc-ms3 Myc degradation Human 
ProteomicsDasatinib for the treatment of gastric cancer
Gastric cancer (GC) represents a major health problem, remaining the fifth most common type of cancer and the third leading cause of cancer-related death worldwide with only few targeted therapies available to date. The positive effect of kinase inhibitors on many different types of cancers has prom...
ORGANISM(S): Homo sapiens (Human) 
2020-05-26 | PXD012953 | Pride
Dasatinib Src kinases Gastric cancer Kinobeads 
ProteomicsSingle methyl group positioning opens new chemical space for EPH receptor kinase inhibition
EPHrin receptors (EPH) are transmembrane receptor tyrosine kinases. Their extracellular domains bind specifically to ephrin A/B ligands, and this binding modulates the intracellular kinase activity. EPHs are key players in bidirectional intercellular signalling, controlling cell morphology, adhesion...
ORGANISM(S): Homo sapiens (Human) 
2018-09-05 | PXD009188 | Pride
Eph receptor Selectivity profiling Kinase inhibitor Kinobeads 
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