ArticleACS chemical biology2012
Celastrol analogues as inducers of the heat shock response. Design and synthesis of affinity probes for the identification of protein targets.
Article in ACS chemical biology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 36 papers.
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The trial behind it
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Who cites it
36 citing papers in PubMed, 71 citations in OpenAlex.
- Process-Induced Metabolite Remodeling ofMetabolites · 2026Article
- Synthesis of Bioconjugation Reagents for Use in Covalent Cross-Linking of Proteins by Azide-Alkyne Cycloaddition.Molecules (Basel, Switzerland) · 2025Article
- Emerging Target Discovery Strategies Drive the Decoding of Therapeutic Power of Natural Products and Further Drug Development: A Case Study of Celastrol.Exploration (Beijing, China) · 2025Review
- The cryoprotective effects of celastrol nanoemulsion on post-thawed attributes and fertilizing ability of cryopreserved buffalo semen.Veterinary research communications · 2025Article
- Celastrol targets CKB-mediated futile creatine cycle in human brown adipocytes thermogenesis.Metabolism open · 2025Article
- Prodrug-inspired adenosine triphosphate-activatable celastrol-Fe(III) chelate for cancer therapy.Science advances · 2024Article
- Recent Trends in anti-tumor mechanisms and molecular targets of celastrol.International journal of biological sciences · 2024Review
- Disruption of Proteostasis by Natural Products and Synthetic Compounds That Induce Pervasive Unfolding of Proteins: Therapeutic Implications.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Protein painting reveals pervasive remodeling of conserved proteostasis machinery in response to pharmacological stimuli.NPJ systems biology and applications · 2022Article
- Neuroprotective Effects of Celastrol in Neurodegenerative Diseases-Unscramble Its Major Mechanisms of Action and Targets.Aging and disease · 2022Review
- Antimalarial and antitumour activities of the steroidal quinone-methide celastrol and its combinations with artemiside, artemisone and methylene blue.Frontiers in pharmacology · 2022Article
- Celastrol exerts a neuroprotective effect by directly binding to HMGB1 protein in cerebral ischemia-reperfusion.Journal of neuroinflammation · 2021Article
- The Therapeutic Potential of Celastrol in Central Nervous System Disorders: Highlights from In Vitro and In Vivo Approaches.Molecules (Basel, Switzerland) · 2021Review
- Design, Synthesis and In Vitro Investigation of Novel Basic Celastrol Carboxamides as Bio-Inspired Leishmanicidal Agents Endowed with Inhibitory Activity againstBiomolecules · 2021Article
- Currently Available Strategies for Target Identification of Bioactive Natural Products.Frontiers in chemistry · 2021Review
- Heat shock protein 90 inhibition and multi-target approach to maximize cardioprotection in ischaemic injury.British journal of pharmacology · 2020Review
- Target identification of natural medicine with chemical proteomics approach: probe synthesis, target fishing and protein identification.Signal transduction and targeted therapy · 2020Review
- Chondro-protective effects of celastrol on osteoarthritis through autophagy activation and NF-κB signaling pathway inhibition.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2020Article
- Celastrol: A Review of Useful Strategies Overcoming its Limitation in Anticancer Application.Frontiers in pharmacology · 2020Review
- The plant triterpenoid celastrol blocks PINK1-dependent mitophagy by disrupting PINK1's association with the mitochondrial protein TOM20.The Journal of biological chemistry · 2019Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
The natural product celastrol (1) possesses numerous beneficial therapeutic properties and affects numerous cellular pathways. The mechanism of action and cellular target(s) of celastrol, however, remain unresolved. While a number of studies have proposed that the activity of celastrol is mediated through reaction with cysteine residues, these observations have been based on studies with specific proteins or by in vitro analysis of a small fraction of the proteome. In this study, we have investigated the spatial and structural requirements of celastrol for the design of suitable affinity probes to identify cellular binding partners of celastrol. Although celastrol has several potential sites for modification, some of these were not synthetically amenable or yielded unstable analogues. Conversion of the carboxylic acid functionality to amides and long-chain analogues, however, yielded bioactive compounds that induced the heat shock response (HSR) and antioxidant response and inhibited Hsp90 activity. This led to the synthesis of biotinylated celastrols (23 and 24) that were used as affinity reagents in extracts of human Panc-1 cells to identify Annexin II, eEF1A, and β-tubulin as potential targets of celastrol.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.