ArticleOrganic & biomolecular chemistry2014
Rare Streptomyces sp. polyketides as modulators of K-Ras localisation.
Article in Organic & biomolecular chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 17 citations in OpenAlex.
- Extracting Value from Marine and Microbial Natural Product Artifacts and Chemical Reactivity.Marine drugs · 2025Review
- RAS Function in cancer cells: translating membrane biology and biochemistry into new therapeutics.The Biochemical journal · 2020Review
- Depletion of phosphatidylinositol 4-phosphate at the Golgi translocates K-Ras to mitochondria.Journal of cell science · 2019Article
- Acylpeptide hydrolase is a novel regulator of KRAS plasma membrane localization and function.Journal of cell science · 2019Article
- An oxanthroquinone derivative that disrupts RAS plasma membrane localization inhibits cancer cell growth.The Journal of biological chemistry · 2018Article
- Deciphering lipid codes: K-Ras as a paradigm.Traffic (Copenhagen, Denmark) · 2018Review
- AMPK and Endothelial Nitric Oxide Synthase Signaling Regulates K-Ras Plasma Membrane Interactions via Cyclic GMP-Dependent Protein Kinase 2.Molecular and cellular biology · 2016Article
- Conserved molecular mechanisms underlying the effects of small molecule xenobiotic chemotherapeutics on cells.Molecular and clinical oncology · 2016Article
- Oligomycins as inhibitors of K-Ras plasma membrane localisation.Organic & biomolecular chemistry · 2016Article
- Rare Streptomyces N-formyl amino-salicylamides inhibit oncogenic K-Ras.Organic letters · 2014Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 4 countries.
Funding
Abstract
Chemical investigations of a soil-derived Streptomyces sp. led to the isolation of five new polyketides, (+)-oxanthromicin, (±)-hemi-oxanthromicins A/B, (±)-spiro-oxanthromicin A and oxanthroquinone, and the known alkaloid staurosporine, and the detection of four new metastable analogues, (±)-spiro-oxanthromicins B1/B2/C1/C2. Among the compounds tested, SAR investigations established that the synthetic oxanthroquinone ethyl ester and 3-O-methyl-oxanthroquinone ethyl ester were optimal at mislocalising oncogenic mutant K-Ras from the plasma membrane of intact Madin-Darby canine kidney (MDCK) cells (IC50 4.6 and 1.2 μM), while a sub-EC50 dose of (±)-spiro-oxanthromicin A was optimal at potentiating (750%) the K-Ras inhibitory activity of staurosporine (IC50 60 pM). These studies demonstrate that a rare class of Streptomyces polyketide modulates K-Ras plasma membrane localisation, with implications for the future treatment of K-Ras dependent cancers.
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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.