ERA-45 is a synthetic estrogen and a selective agonist of the ERα. It shows 286-fold selectivity for transactivation of the ERα over the ERβ, with EC50 values of 0.37 nM for the ERα (7-fold weaker than estradiol) and 13 nM for the ERβ (20,000-fold weaker than estradiol). However, another found only about 35-fold potency for transactivation of the ERα over the ERβ. The drug has no antagonistic activity at either receptor. ERA-45 induced prostate cancer development in preclinical models when it was given in combination with testosterone, whereas testosterone alone did not do so. In contrast, the selective ERβ agonist ERB-26 was protective against the development of prostate cancer produced by these two drugs. These findings suggest opposing roles of the ERα and ERβ in the prostate gland. The
Property | Value |
---|---|
dbo:abstract |
|
dbo:casNumber |
|
dbo:class | |
dbo:wikiPageID |
|
dbo:wikiPageLength |
|
dbo:wikiPageRevisionID |
|
dbo:wikiPageWikiLink |
|
dbp:casNumber |
|
dbp:class |
|
dbp:wikiPageUsesTemplate | |
dcterms:subject | |
rdf:type | |
rdfs:comment |
|
rdfs:label |
|
owl:sameAs | |
prov:wasDerivedFrom | |
foaf:isPrimaryTopicOf | |
is dbo:wikiPageRedirects of | |
is dbo:wikiPageWikiLink of | |
is foaf:primaryTopic of |