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The natural cyclopeptide Callyaerin B (CalB) exhibits highly specific antitubercular activity. The aim of this project is to study the protein binding partner of this compound using either activity-based protein profiling (ABPP) (ACE_0721) or affinity-based protein profiling (AfBPP) (ACE_0682 & ACE_...
ORGANISM(S): Mycobacterium tuberculosis H37Rv 
2024-07-25 | PXD050770 | Pride
The cytotoxic and antifungal peptolides vioprolide A-D were discovered in 1996, however their mode-of-action has so far been unsolved. Anti-cancer effect of the most potent cytotoxic derivative vioprolide A (VioA) were evaluated, showing a prominent potency against human acute lymphoblastic leukemia...
ORGANISM(S): Homo sapiens (Human) 
2020-01-13 | PXD015196 | Pride
To combat methicillin-resistant Staphylococcus aureus (MRSA) infections novel drugs are desperately needed. From a screen, we found that the anti-cancer drug sorafenib effectively kills MRSA strains. By synthetic variation of key structural features, we identified a potent analog, PK150, exhibiting ...
ORGANISM(S): Staphylococcus aureus 
2019-09-09 | PXD012946 | Pride
Screening large molecule libraries against pathogenic bacteria is often challenged by a low hit rate due to limited uptake, underrepresentation of antibiotic structural motifs and assays which do not resemble the infection conditions. To address these limitations, we here screen a library focused on...
ORGANISM(S): Staphylococcus aureus 
2024-07-17 | PXD051986 | Pride
Navtemadlin is a potent small moeclule inhibitor of the p53-MDM2 protein-protein interaction, that is being tested in Phase II/III clinical trials for the treatment of cancer. The selectivity of this molecule is poorly understood. So we synthesised and validated two photoactivatable clickable probes...
ORGANISM(S): Homo sapiens (Human) 
2025-04-28 | PXD058033 | Pride
Navtemadlin is a potent small moeclule inhibitor of the p53-MDM2 protein-protein interaction, that is being tested in Phase II/III clinical trials for the treatment of cancer. The selectivity of this molecule is poorly understood. So we synthesised and validated two photoactivatable clickable probes...
ORGANISM(S): Homo sapiens (Human) 
2025-04-28 | PXD058036 | Pride
Staphylococcus aureus is a major bacterial pathogen that invades and damages host tissue by the expression of devastating toxins. We here performed a phenotypic screen of 35 molecules that were structurally inspired by previous hydroxyamide-based S. aureus virulence inhibitors compiled from commerci...
ORGANISM(S): Staphylococcus aureus 
2018-03-05 | PXD008067 | Pride
A wide range of small molecule scaffolds capable of mimicking protein α-helices to modulate protein-protein interactions have been reported, yet their target selectivity is poorly understood. Here, we report the affinity-based protein profiling of three structurally distinct classes of α-helix mimet...
ORGANISM(S): Homo sapiens (Human) 
2026-08-05 | PXD063432 | Pride
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