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ProteomicsIdentification of ubiquitination site in BCL-XL after PROTAC DT2216 treatment
The availability of a suitable lysine for PROTAC-mediated ubiquitination can also determine the degradative ability of a protein target and the selectivity of a PROTAC. PROTAC DT2216 selectively triggers ubiquitination and degradation of BCL-XL. In this study, we identify K87 is the key ubiquitinate...
ORGANISM(S): Homo sapiens (Human) 
2019-10-08 | PXD015454 | Pride
Bcl-xl Ubiquitination site K87 Protac Dt2216 
ProteomicsPiperlongumine (PL) conjugates induce targeted protein degradation
PROteolysis Targeting Chimeras (PROTACs) are bifunctional molecules that degrade target proteins through recruiting E3 ligases. However, their application is limited in part because few E3 ligases can be recruited by known E3 ligase ligands. In this study, we identified piperlongumine (PL), a natura...
ORGANISM(S): Homo sapiens (Human) 
2024-05-24 | PXD039385 | Pride
Piperlongumine Protac E3 ligase Cdk9 
ProteomicsIdentification of the E3 ligase(s) recruited by 955 to degrade CDK9
PROTACs induce the degradation of target proteins by hijacking an E3 ligase. However, it is usually difficult to directly identify the E3 ligase recruited by a new E3 ligase ligand in a PROTAC using the co-immunoprecipitation method because the formation of the complex is transient and very dynamic....
ORGANISM(S): Homo sapiens (Human) 
2024-05-24 | PXD039401 | Pride
Turboid Protac Pl Cdk9 E3 ligase 
ProteomicsDevelopment and crystal structures of a more potent second-generation dual degrader of BCL-2 and BCL-xL
Overexpression of BCL-xL and BCL-2 play key roles in tumorigenesis and cancer drug resistance. Advances in PROTAC technology facilitated recent development of the first BCL-xL/BCL-2 dual degrader, 753b, a VHL-based degrader with improved potency and reduced toxicity compared to previous small molec...
ORGANISM(S): Homo sapiens (Human) 
2024-03-12 | PXD049976 | Pride
Protac Crystal structure Ubiquitin Ternary complex Degrader E3 ligase Bcl-xl/bcl-2 
ProteomicsDT2216 is a specific BCL-XL PROTAC
To validate the specificity of DT2216, we used the stable isotope labeling with amino acids in cell culture (SILAC) and liquid chromatography-tandem mass spectrometry (LC-MS/MS)-based proteomics to analyze the changes in proteins in WI-38 normal human diploid fibroblasts after DT2216 and DT2216NC tr...
ORGANISM(S): Homo sapiens (Human) 
2019-10-08 | PXD010878 | Pride
Dt2216 bcl-xl protac silac lc-ms/ms 
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