ArticleClinical cancer research : an official journal of the American Association for Cancer Research2007
Preclinical studies of celastrol and acetyl isogambogic acid in melanoma.
Article in Clinical cancer research : an official journal of the American Association for Cancer Research, 2007. 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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Who cites it
36 citing papers in PubMed, 93 citations in OpenAlex.
- Celastrol in Rheumatoid Arthritis: Immunomodulatory Mechanisms, Multicellular Convergence, and Translational Challenges.International journal of molecular sciences · 2026Review
- Review
- Progress in Antimelanoma Research of Natural Triterpenoids and Their Derivatives: Mechanisms of Action, Bioavailability Enhancement and Structure Modifications.Molecules (Basel, Switzerland) · 2023Review
- Celastrol impairs tumor growth by modulating the CIP2A-GSK3β-MCL-1 axis in gastric cancer cells.Aging · 2023Article
- Effect of Celastrol on LncRNAs and mRNAs Profiles of Cerebral Ischemia-Reperfusion Injury in Transient Middle Cerebral Artery Occlusion Mice Model.Frontiers in neuroscience · 2022Article
- The disruption of protein-protein interactions with co-chaperones and client substrates as a strategy towards Hsp90 inhibition.Acta pharmaceutica Sinica. B · 2021Review
- Nanotechnology-Based Celastrol Formulations and Their Therapeutic Applications.Frontiers in pharmacology · 2021Review
- Nuclear Mechanisms Involved in Endocrine Resistance.Frontiers in oncology · 2021Review
- Celastrol Self-Stabilized Nanoparticles for Effective Treatment of Melanoma.International journal of nanomedicine · 2020Article
- Review
- Autophagy flux inhibition mediated by celastrol sensitized lung cancer cells to TRAIL‑induced apoptosis via regulation of mitochondrial transmembrane potential and reactive oxygen species.Molecular medicine reports · 2019Article
- Inhibition of IKKβ by celastrol and its analogues - an in silico and in vitro approach.Pharmaceutical biology · 2017Article
- AlCl₃·6H₂O-Catalyzed Friedel-Crafts Alkylation of Indoles by the para-Quinone Methide Moiety of Celastrol.Molecules (Basel, Switzerland) · 2017Article
- Celastrol: A Spectrum of Treatment Opportunities in Chronic Diseases.Frontiers in medicine · 2017Review
- Inhibiting inducible miR-223 further reduces viable cells in human cancer cell lines MCF-7 and PC3 treated by celastrol.BMC cancer · 2015Article
- Direct inhibition of c-Myc-Max heterodimers by celastrol and celastrol-inspired triterpenoids.Oncotarget · 2015Article
- Celastrol induces unfolded protein response-dependent cell death in head and neck cancer.Experimental cell research · 2015Article
- Effect of celastrol on growth inhibition of prostate cancer cells through the regulation of hERG channel in vitro.BioMed research international · 2015Article
- Cancerous inhibitor of PP2A is targeted by natural compound celastrol for degradation in non-small-cell lung cancer.Carcinogenesis · 2014Article
- Celastrol analogues as inducers of the heat shock response. Design and synthesis of affinity probes for the identification of protein targets.ACS chemical biology · 2012Article
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
Abstract
purposeSensitize melanomas to apoptosis and inhibit their growth and metastatic potential by compounds that mimic the activities of activating transcription factor 2 (ATF2)-driven peptides. EXPERIMENTAL
designSmall-molecule chemical library consisting of 3,280 compounds was screened to identify compounds that elicit properties identified for ATF2 peptide, including (a) sensitization of melanoma cells to apoptosis, (b) inhibition of ATF2 transcriptional activity, (c) activation of c-Jun NH(2)-terminal kinase (JNK) and c-Jun transcriptional activity, and (d) inhibition of melanoma growth and metastasis in mouse models.
resultsTwo compounds, celastrol (CSL) and acetyl isogambogic acid, could, within a low micromolar range, efficiently elicit cell death in melanoma cells. Both compounds efficiently inhibit ATF2 transcriptional activities, activate JNK, and increase c-Jun transcriptional activities. Similar to the ATF2 peptide, both compounds require JNK activity for their ability to inhibit melanoma cell viability. Derivatives of CSL were identified as potent inducers of cell death in mouse and human melanomas. CSL and a derivative (CA19) could also efficiently inhibit growth of human and mouse melanoma tumors and reduce the number of lung metastases in syngeneic and xenograft mouse models.
conclusionsThese studies show for the first time the effect of CSL and acetyl isogambogic acid on melanoma. These compounds elicit activities that resemble the well-characterized ATF2 peptide and may therefore offer new approaches for the treatment of this tumor type.
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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.