ArticleBiochemical pharmacology2010
Identification and characterization of a novel estrogenic ligand actinopolymorphol A.
Article in Biochemical pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed.
- New Zosteropenillines and Pallidopenillines from the Seagrass-Derived FungusMarine drugs · 2024Article
- Antiestrogenic Activity and Possible Mode of Action of Certain New Nonsteroidal Coumarin-4-acetamides.Molecules (Basel, Switzerland) · 2020Article
- A Computational-Based Approach to Identify Estrogen ReceptorMolecular pharmacology · 2018Article
- Flexible small molecular anti-estrogens with N,N-dialkylated-2,5-diethoxy-4-morpholinoaniline scaffold targets multiple estrogen receptor conformations.Cell cycle (Georgetown, Tex.) · 2017Article
- Biosynthetic potential-based strain prioritization for natural product discovery: a showcase for diterpenoid-producing actinomycetes.Journal of natural products · 2014Article
- Δ(9)-Tetrahydrocannabinol disrupts estrogen-signaling through up-regulation of estrogen receptor β (ERβ).Chemical research in toxicology · 2013Article
- Differential action of monohydroxylated polycyclic aromatic hydrocarbons with estrogen receptors α and β.Toxicological sciences : an official journal of the Society of Toxicology · 2013Article
- Homologous NRPS-like gene clusters mediate redundant small-molecule biosynthesis in Aspergillus flavus.Angewandte Chemie (International ed. in English) · 2013Article
- Identification of estrogen receptor dimer selective ligands reveals growth-inhibitory effects on cells that co-express ERα and ERβ.PloS one · 2012Article
- Generation of stable reporter breast cancer cell lines for the identification of ER subtype selective ligands.Biochemical pharmacology · 2011Article
- Actinopolysporins A-C and tubercidin as a Pdcd4 stabilizer from the halophilic actinomycete Actinopolyspora erythraea YIM 90600.Journal of natural products · 2011Article
- Endocrine disrupting chemicals targeting estrogen receptor signaling: identification and mechanisms of action.Chemical research in toxicology · 2011Review
- Cycloheximide and congeners as inhibitors of eukaryotic protein synthesis from endophytic actinomycetes Streptomyces sps. YIM56132 and YIM56141.The Journal of antibiotics · 2011Article
- Bafilomycins produced by an endophytic actinomycete Streptomyces sp. YIM56209.The Journal of antibiotics · 2011Article
- Discovery and total synthesis of a new estrogen receptor heterodimerizing actinopolymorphol A from Actinopolymorpha rutilus.Organic letters · 2010Article
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Authors and funding
11 authors.
Funding
Abstract
Xenoestrogenic compounds are abundant in the modern environment including phytoestrogens from plants, chemical by-products from industry, and secondary metabolites from microbes; all can profoundly affect human health. Consequently mechanism-based screens are urgently needed to improve the rate at which the xenoestrogens are discovered. Estrogen Receptor (ER) dimerization is required for target gene transcription. The three ER dimer pairs (ERalpha/alpha homodimers, ERbeta/beta homodimers, and ERalpha/beta heterodimers) exhibit diverse physiological responses in response to ligand-dependent activation with ERalpha/alpha homodimers being pro-proliferative and ERbeta/beta homodimers being anti-proliferative. The biological role of the ERalpha/beta heterodimer remains unclear. We previously developed a cell-based, bioluminescence resonance energy transfer (BRET) assay that can distinguish natural estrogenic compounds based on their abilities to activate the three diverse ER dimer pairs. Using BRET assays, we sought to identify novel xenoestrogens from soil bacteria that preferentially activate ERalpha/beta heterodimer with hopes of shedding light on the biological function of this elusive dimer pair. Here we describe the application of BRET assays in high throughput screens of crude bacterial extracts not previously screened for ER modulatory function and originating from unique ecological niches. Here we report the discovery and biological evaluation of a new natural product, actinopolymorphol A (1), that preferentially induces ERalpha/beta dimerization. Actinopolymorphol A represents the first representative of a new ER modulatory scaffold.
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Registered trials
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