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Quantitative proteomics reveals cellular targets of celastrol
Jakob Hansen1, Johan Palmfeldt, Søren Vang
1Research Unit for Molecular Medicine, Aarhus University Hospital, Skejby, Aarhus, Denmark. Jakob.Hansen@ki.au.dk
Plos One
|November 3, 2011
Summary
Celastrol, a natural compound, significantly alters cellular protein levels, particularly those involved in stress response and endoplasmic reticulum function. This proteomic analysis provides potential biomarkers for monitoring celastrol-based therapies.
Area of Science:
- Proteomics
- Molecular Biology
- Pharmacology
Background:
- Celastrol, a natural product from traditional Chinese medicine, shows therapeutic potential for cancer, autoimmune, and protein misfolding diseases.
- Existing research on celastrol targets specific pathways, but a global view of its cellular effects is needed.
- Identifying celastrol's protein targets can aid in developing biomarkers for treatment monitoring.
Purpose of the Study:
- To globally assess the cellular effects of celastrol using quantitative proteomics.
- To identify potential protein biomarkers for monitoring celastrol treatment efficacy.
- To investigate celastrol's impact on cellular stress response pathways.
Main Methods:
- Large-scale quantitative proteomics was performed on cultured human lymphoblastoid cells.
- Proteomic analysis identified proteins with significant changes (≥1.5 fold) in response to celastrol.
- Analysis included specific examination of the mitochondrial proteome and selected mRNA transcripts.
Main Results:
- Celastrol significantly altered the proteome, with 158 out of ~1800 quantified proteins showing substantial changes.
- Upregulated proteins were involved in cytoprotection, endoplasmic reticulum protein processing, oxidative stress defense (e.g., heme oxygenase 1, peroxiredoxins, thioredoxins), and iron homeostasis.
- Celastrol increased mitochondrial association of antioxidant and apoptosis-regulating proteins, activated stress response pathways, and reduced cell viability at sub-micromolar concentrations.
Conclusions:
- Celastrol profoundly impacts cellular proteomes, particularly enhancing cytoprotective and stress response mechanisms.
- The identified protein changes serve as valuable biomarkers for developing and monitoring celastrol-based therapeutic strategies.
- This proteomic catalog offers a comprehensive understanding of celastrol's cellular effects.
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