ReviewMolecules (Basel, Switzerland)2015
Thapsigargin--from Thapsia L. to mipsagargin.
Review in Molecules (Basel, Switzerland), 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 45 papers.
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Who cites it
45 citing papers in PubMed, 109 citations in OpenAlex.
- RLASON-CDR: a reinforcement learning-driven adaptive synergistic optimization network for cancer drug response prediction.Briefings in bioinformatics · 2026Article
- Exploring the common ferroptosis-related genes and molecular mechanisms in periodontitis and systemic sclerosis via integrated bioinformatics and experimental analysis.Frontiers in cell and developmental biology · 2026Article
- Thapsigargin suppresses porcine hemagglutinating encephalomyelitis virus replication by disrupting host energy metabolism.Virologica Sinica · 2025Article
- Fine-Tuning of the Endoplasmic Reticulum Stress Response Mechanism Plays a Key Role in Cellular Survival-A Mathematical Study.International journal of molecular sciences · 2025Article
- Nature-Inspired Pathogen and Cancer Protein Covalent Inhibitors: From Plants and Other Natural Sources to Drug Development.Pathogens (Basel, Switzerland) · 2025Review
- Advancements in the therapeutic potential of sesquiterpenoids for the treatment of hepatocellular carcinoma (Review).International journal of oncology · 2025Review
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- Article
- Research advances in natural sesquiterpene lactones: overcoming cancer drug resistance through modulation of key signaling pathways.Cancer drug resistance (Alhambra, Calif.) · 2025Review
- Autophagy modulators in type 2 diabetes: A new perspective.Journal of diabetes · 2024Review
- Thapsigargin and its prodrug derivatives: exploring novel approaches for targeted cancer therapy through calcium signaling disruption.Medical oncology (Northwood, London, England) · 2024Review
- STIM1 in tumor cell death: angel or devil?Cell death discovery · 2023Review
- Isolation and Biological Activity of Iezoside and Iezoside B, SERCA Inhibitors from Floridian Marine Cyanobacteria.Marine drugs · 2023Article
- Synergistic antitumor effect of a penicillin derivative combined with thapsigargin in melanoma cells.Journal of cancer research and clinical oncology · 2022Article
- Peptide-Drug Conjugates: A New Hope for Cancer Management.Molecules (Basel, Switzerland) · 2022Review
- Thapsigargin: key to new host-directed coronavirus antivirals?Trends in pharmacological sciences · 2022Review
- Development of novel bone targeting peptide-drug conjugate of 13-aminomethyl-15-thiomatrine for osteoporosis therapy.RSC advances · 2021Article
- Genetic landscape of T cells identifies synthetic lethality for T-ALL.Communications biology · 2021Article
- Multi-level inhibition of coronavirus replication by chemical ER stress.Nature communications · 2021Article
- Next Chapter in the Legend of Silphion: Preliminary Morphological, Chemical, Biological and Pharmacological Evaluations, Initial Conservation Studies, and Reassessment of the Regional Extinction Event.Plants (Basel, Switzerland) · 2021Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The sesquiterpene lactone thapsigargin is found in the plant Thapsia garganica L., and is one of the major constituents of the roots and fruits of this Mediterranean species. In 1978, the first pharmacological effects of thapsigargin were established and the full structure was elucidated in 1985. Shortly after, the overall mechanism of the Sarco-endoplasmic reticulum Ca2+-ATPase (SERCA) inhibition that leads to apoptosis was discovered. Thapsigargin has a potent antagonistic effect on the SERCA and is widely used to study Ca2+-signaling. The effect on SERCA has also been utilized in the treatment of solid tumors. A prodrug has been designed to target the blood vessels of cancer cells; the death of these blood vessels then leads to tumor necrosis. The first clinical trials of this drug were initiated in 2008, and the potent drug is expected to enter the market in the near future under the generic name Mipsagargin (G-202). This review will describe the discovery of the new drug, the on-going elucidation of the biosynthesis of thapsigargin in the plant and attempts to supply the global market with a novel potent anti-cancer drug.
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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.