EP 1141405 A1 20011010 - BIOASSAY FOR IDENTIFYING ESTROGEN RECEPTOR-BETA/ALPHA SELECTIVE MODULATORS
Title (en)
BIOASSAY FOR IDENTIFYING ESTROGEN RECEPTOR-BETA/ALPHA SELECTIVE MODULATORS
Title (de)
BIOLOGISCHES TESTVERFAHREN ZUR IDENTIFIZIERUNG VON ALPHA/BETA - SELEKTIVEN ÖSTROGENREZEPTORMODULATOREN
Title (fr)
DOSAGE BIOLOGIQUE PERMETTANT D'IDENTIFIER DES MODULATEURS SELECTIFS DES RECEPTEURS DES OESTROGENES BETA/ALPHA
Publication
Application
Priority
- US 9929856 W 19991217
- US 11279098 P 19981218
Abstract (en)
[origin: WO0037681A1] The present invention provides novel assay methods for identifying compounds that selectively activate estrogen receptors (ER) of the alpha or beta subtype. In particular, the results from two assays, one measuring ER- beta activity and the other measuring ER- alpha activity are interpreted. The assay measuring ER- beta activity uses cells comprising endogenous metallothionein-II as well as a DNA plasmid comprising a polynucleotide encoding human ER- beta . The assay monitors expression of metallothionein-II-mRNA in said cells, wherein the level of metallothionein-II expression is regulated when a potential ligand binds to ER- beta . The assay measuring ER- alpha activity uses cells comprising ER- alpha as well as DNA plasmid comprising a reporter gene linked to an estrogen response element. The assay monitors expression of the reporter gene, wherein the level of reporter gene is regulated when a potential ligand binds to ER- alpha . Compounds which modulate activity in one assay but have little or no activity in the other assay are defined as estrogen receptor subtype selective.
[origin: WO0037681A1] The present invention provides novel assay methods for identifying compounds that selectively activate estrogen receptors (ER) of the alpha or beta subtype. In particular, the results from two assays, one measuring ER- beta activity and the other measuring ER- alpha activity are interpreted. The assay measuring ER- beta activity uses cells comprising endogenous metallothionein-II as well as a DNA plasmid comprising a polynucleotide encoding human ER- beta . The assay monitors expression of metallothionein-II-mRNA in said cells, wherein the level of metallothionein-II expression is regulated when a potential ligand binds to ER- beta . The assay measuring ER- alpha activity uses cells comprising ER- alpha as well as DNA plasmid comprising a reporter gene linked to an estrogen response element. The assay monitors expression of the reporter gene, wherein the level of reporter gene is regulated when a potential ligand binds to ER- alpha . Compounds which modulate activity in one assay but have little or no activity in the other assay are defined as estrogen receptor subtype selective.
IPC 1-7
IPC 8 full level
C12Q 1/02 (2006.01); C12Q 1/68 (2006.01); C12N 15/09 (2006.01); C12Q 1/6897 (2018.01); G01N 33/74 (2006.01)
CPC (source: EP)
C12Q 1/6897 (2013.01); G01N 33/743 (2013.01); G01N 2333/723 (2013.01); G01N 2500/00 (2013.01)
Designated contracting state (EPC)
AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE
DOCDB simple family (publication)
WO 0037681 A1 20000629; AU 2187900 A 20000712; AU 760784 B2 20030522; CA 2352203 A1 20000629; CN 1352699 A 20020605; EP 1141405 A1 20011010; HU P0104719 A2 20020429; HU P0104719 A3 20040301; JP 2002533098 A 20021008; NO 20012999 D0 20010615; NO 20012999 L 20010815; NZ 512347 A 20031219
DOCDB simple family (application)
US 9929856 W 19991217; AU 2187900 A 19991217; CA 2352203 A 19991217; CN 99814685 A 19991217; EP 99966310 A 19991217; HU P0104719 A 19991217; JP 2000589734 A 19991217; NO 20012999 A 20010615; NZ 51234799 A 19991217