ERB-26 (original) (raw)
ERB-26 is a synthetic estrogen and a selective agonist of the ERβ. It is the active enantiomer of the racemic mixture ERB-79. Whereas ERB-79 shows 484-fold selectivity for the ERβ over the ERα, ERB-26 differs slightly in that it is even more selective, showing greater than 1,000-fold selectivity for transactivation of the ERβ relative to the ERα. Its EC50 value for the ERβ is 0.21 nM (4-fold weaker than estradiol) and for the ERα is 260 nM (10,000-fold weaker than estradiol). It has no antagonistic activity at either receptor. ERB-26 is active in prevention of prostate cancer development in preclinical models. In contrast to ERB-26, the selective ERα agonist ERA-45 induced prostate cancer development in preclinical models when it was given in combination with testosterone, whereas testoste
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| dbo:abstract | ERB-26 is a synthetic estrogen and a selective agonist of the ERβ. It is the active enantiomer of the racemic mixture ERB-79. Whereas ERB-79 shows 484-fold selectivity for the ERβ over the ERα, ERB-26 differs slightly in that it is even more selective, showing greater than 1,000-fold selectivity for transactivation of the ERβ relative to the ERα. Its EC50 value for the ERβ is 0.21 nM (4-fold weaker than estradiol) and for the ERα is 260 nM (10,000-fold weaker than estradiol). It has no antagonistic activity at either receptor. ERB-26 is active in prevention of prostate cancer development in preclinical models. In contrast to ERB-26, the selective ERα agonist ERA-45 induced prostate cancer development in preclinical models when it was given in combination with testosterone, whereas testosterone alone did not do so. These findings suggest opposing roles of the ERα and ERβ in the prostate gland. The chemical structure of ERB-26 does not appear to have been disclosed. (en) |
| dbo:class | dbr:Estrogen_(medication) |
| dbo:wikiPageID | 52741283 (xsd:integer) |
| dbo:wikiPageLength | 4041 (xsd:nonNegativeInteger) |
| dbo:wikiPageRevisionID | 1086717558 (xsd:integer) |
| dbo:wikiPageWikiLink | dbr:Prinaberel dbr:Prostate_gland dbr:Enantiomer dbr:Transactivation dbr:EC50 dbr:ERA-45 dbr:ERB-79 dbr:Racemic_mixture dbc:Synthetic_estrogens dbr:Chemical_structure dbr:Erteberel dbr:Estrogen dbr:Estrogen_(medication) dbr:WAY-200070 dbr:WAY-214156 dbc:Selective_ERβ_agonists dbr:Animal_model dbr:Receptor_antagonist dbr:Prostate_cancer dbr:WAY-166818 dbr:Agonist dbr:ERB-196 dbr:Estradiol dbr:FERb_033 dbr:Testosterone_(medication) dbc:Drugs_with_undisclosed_chemical_structures dbr:Binding_selectivity dbr:Biological_activity dbr:Diarylpropionitrile dbr:Synthetic_compound dbr:ERβ dbr:Preclinical_research |
| dbp:class | Estrogen; Selective ERβ agonist (en) |
| dbp:wikiPageUsesTemplate | dbt:Drugbox dbt:Estrogen_receptor_modulators dbt:Genito-urinary-drug-stub dbt:Reflist dbt:Short_description |
| dct:subject | dbc:Synthetic_estrogens dbc:Selective_ERβ_agonists dbc:Drugs_with_undisclosed_chemical_structures |
| rdf:type | owl:Thing dul:ChemicalObject dbo:ChemicalSubstance wikidata:Q8386 dbo:Drug |
| rdfs:comment | ERB-26 is a synthetic estrogen and a selective agonist of the ERβ. It is the active enantiomer of the racemic mixture ERB-79. Whereas ERB-79 shows 484-fold selectivity for the ERβ over the ERα, ERB-26 differs slightly in that it is even more selective, showing greater than 1,000-fold selectivity for transactivation of the ERβ relative to the ERα. Its EC50 value for the ERβ is 0.21 nM (4-fold weaker than estradiol) and for the ERα is 260 nM (10,000-fold weaker than estradiol). It has no antagonistic activity at either receptor. ERB-26 is active in prevention of prostate cancer development in preclinical models. In contrast to ERB-26, the selective ERα agonist ERA-45 induced prostate cancer development in preclinical models when it was given in combination with testosterone, whereas testoste (en) |
| rdfs:label | ERB-26 (en) |
| owl:sameAs | yago-res:ERB-26 wikidata:ERB-26 https://global.dbpedia.org/id/2ct7o |
| prov:wasDerivedFrom | wikipedia-en:ERB-26?oldid=1086717558&ns=0 |
| foaf:isPrimaryTopicOf | wikipedia-en:ERB-26 |
| is dbo:wikiPageRedirects of | dbr:ERB26 dbr:ERB_26 |
| is dbo:wikiPageWikiLink of | dbr:ERA-45 dbr:ERB-79 dbr:Estrogen_receptor_beta dbr:ERB26 dbr:ERB_26 |
| is foaf:primaryTopic of | wikipedia-en:ERB-26 |