ArticleCancer biology & therapy2011
Proteasome inhibitory activity of thiazole antibiotics.
Article in Cancer biology & therapy, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 38 citations in OpenAlex.
- A Compact Reprogrammed Genetic Code for De Novo Discovery of Proteolytically Stable Thiopeptides.Journal of the American Chemical Society · 2024Article
- Regulation of Molecular Targets in Osteosarcoma Treatment.International journal of molecular sciences · 2022Review
- Mechanism of Action of Ribosomally Synthesized and Post-Translationally Modified Peptides.Chemical reviews · 2022Review
- High-throughput phenotypic screen and transcriptional analysis identify new compounds and targets for macrophage reprogramming.Nature communications · 2021Article
- Natural product scaffolds as inspiration for the design and synthesis of 20S human proteasome inhibitors.RSC chemical biology · 2020Article
- A preclinical evaluation of thiostrepton, a natural antibiotic, in nasopharyngeal carcinoma.Investigational new drugs · 2020Article
- Forkhead box M1 transcription factor: a novel target for pulmonary arterial hypertension therapy.World journal of pediatrics : WJP · 2020Review
- Proteasome inhibitors modulate anticancer and anti-proliferative properties via NF-kB signaling, and ubiquitin-proteasome pathways in cancer cell lines of different organs.Lipids in health and disease · 2018Article
- YcaO-Dependent Posttranslational Amide Activation: Biosynthesis, Structure, and Function.Chemical reviews · 2017Review
- Thiostrepton Variants Containing a Contracted Quinaldic Acid Macrocycle Result from Mutagenesis of the Second Residue.ACS chemical biology · 2016Article
- Saturation mutagenesis of TsrA Ala4 unveils a highly mutable residue of thiostrepton A.ACS chemical biology · 2015Article
- Gene silencing of NOB1 by lentivirus suppresses growth and migration of human osteosarcoma cells.Molecular medicine reports · 2014Article
- Review
- Thiostrepton is an inducer of oxidative and proteotoxic stress that impairs viability of human melanoma cells but not primary melanocytes.Biochemical pharmacology · 2012Article
- Proteasome inhibitors: an expanding army attacking a unique target.Chemistry & biology · 2012Review
- Micelle-encapsulated thiostrepton as an effective nanomedicine for inhibiting tumor growth and for suppressing FOXM1 in human xenografts.Molecular cancer therapeutics · 2011Article
- Thiazole antibiotic thiostrepton synergize with bortezomib to induce apoptosis in cancer cells.PloS one · 2011Article
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Thiopeptides are sulfur containing highly modified macrocyclic antibiotics with a central pyridine/tetrapyridine/dehydropiperidine ring with up to three thiazole substituents on positions 2, 3 and 6. Thiazole antibiotics with central pyridine nucleus have a macrocyclic loop connecting thiazole rings at position 2 and 3 described as ring A. In addition antibiotics with central tetrahydropyridine nucleus have a quinaldic acid macrocycle also connected to thiazole on position 2 described as ring B. We have demonstrated before that thiazole antibiotics thiostrepton and Siomycin A act as proteasome inhibitors in mammalian tumor cells. Here we decided to test whether other known thiazole antibiotics such as berninamycin, micrococcin P1 and P2, thiocillin and YM-266183 (lacking the quinaldic acid ring B) demonstrate this activity. We found that none of them act as proteasome inhibitors. Moreover, structural modification of thiostrepton to thiostrepton methyl ester (with open B ring) also did not demonstrate this activity. These data suggest that B ring of thiostrepton and Siomycin A that is absent in other thiazole antibiotics determines the proteasome inhibitory activity of these drugs.
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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.