Proteomics

Dataset Information

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DT2216 is a specific BCL-XL PROTAC

ABSTRACT: 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 treatment. The results show that DT2216, but not DT2216NC, reduced the levels of BCL-XL, but none of other proteins were significantly affected by either agent, demonstrating that DT2216 is a specific BCL-XL PROTAC.

INSTRUMENT(S): LTQ Orbitrap

ORGANISM(S): Homo Sapiens (human)

TISSUE(S): Cell Culture, Fibroblast

DISEASE(S): Disease Free

SUBMITTER: Dongwen Lv  

LAB HEAD: Daohong Zhou

PROVIDER: PXD010878 | Pride | 2019-10-08

REPOSITORIES: Pride

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Dataset's files

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Zhou_022818_SILAC3_FT.raw Raw
Zhou_022818_SILAC3_SF01.raw Raw
Zhou_022818_SILAC3_SF02.raw Raw
Zhou_022818_SILAC3_SF03.raw Raw
Zhou_022818_SILAC3_SF04.raw Raw
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Publications

B-cell lymphoma extra large (BCL-X<sub>L</sub>) is a well-validated cancer target. However, the on-target and dose-limiting thrombocytopenia limits the use of BCL-X<sub>L</sub> inhibitors, such as ABT263, as safe and effective anticancer agents. To reduce the toxicity of ABT263, we converted it into DT2216, a BCL-X<sub>L</sub> proteolysis-targeting chimera (PROTAC), that targets BCL-X<sub>L</sub> to the Von Hippel-Lindau (VHL) E3 ligase for degradation. We found that DT2216 was more potent again  ...[more]

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