ArticleInvestigational new drugs2015
The marine natural product microsclerodermin A is a novel inhibitor of the nuclear factor kappa B and induces apoptosis in pancreatic cancer cells.
Article in Investigational new drugs, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers, 2 of them syntheses that pooled it.
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Who cites it
29 citing papers in PubMed, 2 syntheses or guidelines pooled it, 46 citations in OpenAlex.
- Modulation of TLR/NF-κB/NLRP Signaling by Bioactive Phytocompounds: A Promising Strategy to Augment Cancer Chemotherapy and Immunotherapy.Frontiers in oncology · 2022Pooled it
- A Systematic Review of Recently Reported Marine Derived Natural Product Kinase Inhibitors.Marine drugs · 2019Pooled it
- Stereoselective Syntheses of Cyclic Microsclerodermin Derivatives.Chemistry (Weinheim an der Bergstrasse, Germany) · 2025Article
- Democratized Discovery of Microsclerodermin F as an Immunophilin Ligand.Marine drugs · 2025Article
- Repositioning Brusatol as a Transmission Blocker of Malaria Parasites.ACS infectious diseases · 2024Article
- The Microbiota of Moon Snail Egg Collars is Shaped by Host-Specific Factors.bioRxiv : the preprint server for biology · 2024Article
- The Marine Natural Compound Dragmacidin D Selectively Induces Apoptosis in Triple-Negative Breast Cancer Spheroids.Marine drugs · 2023Article
- Marine-Inspired Drugs and Biomaterials in the Perspective of Pancreatic Cancer Therapies.Marine drugs · 2022Review
- Anticancer effects of marine compounds blocking the nuclear factor kappa B signaling pathway.Molecular biology reports · 2022Review
- Natural Products of Marine Origin for the Treatment of Colorectal and Pancreatic Cancers: Mechanisms and Potential.International journal of molecular sciences · 2022Review
- Cancer and apoptosis: The apoptotic activity of plant and marine natural products and their potential as targeted cancer therapeutics.Frontiers in pharmacology · 2022Review
- Synthetic and Naturally Occurring Heterocyclic Anticancer Compounds with Multiple Biological Targets.Molecules (Basel, Switzerland) · 2021Review
- Myxobacteria as a Source of New Bioactive Compounds: A Perspective Study.Pharmaceutics · 2021Review
- Article
- Natural Cyclopeptides as Anticancer Agents in the Last 20 Years.International journal of molecular sciences · 2021Review
- Unfolding antifungals: as a new foe to pancreatic ductal adenocarcinoma-a mini-review.Molecular biology reports · 2021Review
- Recent Advances in Small Peptides of Marine Origin in Cancer Therapy.Marine drugs · 2021Review
- Review
- Isocorydine decrease gemcitabine-resistance by inhibiting epithelial-mesenchymal transition via STAT3 in pancreatic cancer cells.American journal of translational research · 2020Article
- Proapoptotic Index Evaluation of Two Synthetic Peptides Derived from the ConeshellMarine drugs · 2019Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
Pancreatic cancer, the 4th leading cause of cancer death in the US, is highly resistant to all current chemotherapies, and its growth is facilitated by chronic inflammation. An important mediator of inflammation is the nuclear factor kappa B (NFκB), a transcription factor that regulates over 500 genes including the regulation of anti-apoptotic proteins, cell cycle progression and cytokine production. NFκB is constitutively activated in pancreatic cancer cells contributing to their resistance to apoptosis and high metastatic potential. Although many small molecules that inhibit NFκB have been identified, none are currently used in the clinic, perhaps due to their lack of specificity. To identify novel inhibitors of NFκB, the HBOI library of enriched fractions from marine organisms was screened using a reporter cell line that produces luciferin under the transcriptional control of NFκB. Fractions from the sponge Amphibleptula were active in this screen and contained the antifungal cyclic peptide microsclerodermin A. Microsclerodermin A is shown here to inhibit NFκB transcriptional activity in a reporter cell line, to reduce levels of phosphorylated (active) NFκB in the AsPC-1 cell line, to have an IC50 for cytotoxicity in the low micromolar range against the AsPC-1, BxPC-3, MIA PaCa-2 and PANC-1 pancreatic cancer cell lines, and to induce significant apoptosis in the AsPC-1, BxPC-3 and the PANC-1 cell lines. Treatment of AsPC-1 cells with microsclerodermin A also resulted in an increase in IL-8 production without apparent induction of angiogenic factors and there is the possibility that inhibition of NFκB by microsclerodermin A is mediated by the glycogen synthase kinase 3β pathway.
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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.