EP 1297175 A2 20030402 - METHODS AND COMPOUNDS FOR MODULATING NUCLEAR RECEPTOR COACTIVATOR BINDING
Title (en)
METHODS AND COMPOUNDS FOR MODULATING NUCLEAR RECEPTOR COACTIVATOR BINDING
Title (de)
VERFAHREN UND VERBINDUNGEN ZUR MODULATION DER BINDUNG VON NUKLEÄREM REZEPTOR AM KOAKTIVATOR
Title (fr)
PROCEDES ET COMPOSES POUR MODULER LA FIXATION DE COACTIVATEURS A DES RECEPTEURS NUCLEAIRES
Publication
Application
Priority
- US 0120969 W 20010629
- US 60936100 A 20000630
Abstract (en)
[origin: WO0202488A2] The present invention relates to methods and agonist/antagonist compounds for modulating nuclear receptor coactivator binding. The invention includes a method for identifying residues comprising a coactivator binding site for a nuclear receptor of interest. Also included is a method of identifying agonists and/or antagonists that bind to a coactivator binding site of a nuclear receptor of interest. Agonists and antagonists of coactivator binding to nuclear receptors also are provided. The invention is exemplified by identification and manipulation of the coactivator binding site of the thyroid receptor (TR), and compounds that bind to this sites. The methods can be applied to other nuclear receptors including RAR, RXR, PPAR, VDR, ER, GR, PR, MR, and AR.
IPC 1-7
C12Q 1/00; G01N 33/53; G01N 33/543; G01N 33/566; G01N 33/567; A61K 38/04; C07K 5/00; G01N 33/68; C07B 61/00; C07D 209/82; C07D 209/88; C07D 225/08; C07D 403/06; C07D 403/14; C07K 1/04; C07K 7/08; C07K 7/56; B01J 19/00
IPC 8 full level
C07B 61/00 (2006.01); C07D 209/82 (2006.01); C07D 209/88 (2006.01); C07D 225/08 (2006.01); C07D 403/06 (2006.01); C07D 403/14 (2006.01); C07K 1/04 (2006.01); C07K 7/08 (2006.01); C07K 7/56 (2006.01); G01N 33/68 (2006.01); G16B 15/30 (2019.01); G16B 20/30 (2019.01)
CPC (source: EP US)
C07D 209/82 (2013.01 - EP); C07D 209/88 (2013.01 - EP); C07D 225/08 (2013.01 - EP); C07D 403/06 (2013.01 - EP); C07D 403/14 (2013.01 - EP); C07K 1/047 (2013.01 - EP); C07K 7/08 (2013.01 - EP); C07K 7/56 (2013.01 - EP); G01N 33/6875 (2013.01 - EP); G16B 15/00 (2019.01 - EP); G16B 15/30 (2019.01 - EP US); G16B 20/30 (2019.01 - EP US); C07K 2299/00 (2013.01 - EP); C40B 40/00 (2013.01 - EP); G16B 20/00 (2019.01 - EP)
Designated contracting state (EPC)
AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE TR
DOCDB simple family (publication)
WO 0202488 A2 20020110; WO 0202488 A3 20020418; WO 0202488 A9 20030912; CA 2415103 A1 20020110; EP 1297175 A2 20030402; EP 1297175 A4 20050202
DOCDB simple family (application)
US 0120969 W 20010629; CA 2415103 A 20010629; EP 01950770 A 20010629