Global Patent Index - EP 1297175 A4

EP 1297175 A4 20050202 - 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

EP 1297175 A4 20050202 (EN)

Application

EP 01950770 A 20010629

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); G06F 19/00 (2006.01); G06F 19/16 (2011.01); G16B 15/30 (2019.01); G16B 20/30 (2019.01); G06F 19/18 (2011.01)

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)

Citation (search report)

  • [X] WO 9927365 A1 19990603 - TULARIK INC [US]
  • [X] WO 9960014 A2 19991125 - UNIV CALIFORNIA [US]
  • [X] WO 9950658 A2 19991007 - UNIV CALIFORNIA [US], et al
  • [X] DING XIU FEN ET AL: "Nuclear receptor-binding sites of coactivators glucocorticoid receptor interacting protein 1 (GRIP1) and steroid receptor coactivator 1 (SRC-1): Multiple motifs with different binding specificities", MOLECULAR ENDOCRINOLOGY, BALTIMORE, MD, US, vol. 12, no. 2, February 1998 (1998-02-01), pages 302 - 313, XP001040351, ISSN: 0888-8809
  • [X] DARIMONT B D ET AL: "STRUCTURE AND SPECIFICITY OF NUCLEAR RECEPTOR-COACTIVATOR INTERACTIONS", GENES AND DEVELOPMENT, COLD SPRING HARBOR LABORATORY PRESS, NEW YORK, US, vol. 12, no. 21, November 1998 (1998-11-01), pages 3343 - 3356, XP008026614, ISSN: 0890-9369
  • [A] POPE A J ET AL: "Homogeneous fluorescence readouts for miniaturized high-throughput screening: Theory and practice", DRUG DISCOVERY TODAY 1999 UNITED KINGDOM, vol. 4, no. 8, 1999, pages 350 - 362, XP002290440, ISSN: 1359-6446
  • [PA] BISSANTZ CATERINA ET AL: "Protein-based virtual screening of chemical databases. 1. Evaluation of different docking/scoring combinations", JOURNAL OF MEDICINAL CHEMISTRY, vol. 43, no. 25, 14 December 2000 (2000-12-14), pages 4759 - 4767, XP002307473, ISSN: 0022-2623
  • [A] SCHAPIRA MATTHIEU ET AL: "Rational discovery of novel nuclear hormone receptor antagonists", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, vol. 97, no. 3, 1 February 2000 (2000-02-01), pages 1008 - 1013, XP002307474, ISSN: 0027-8424
  • [A] CHANG C Y ET AL: "Dissection of the LXXLL nuclear receptor-coactivator interaction motif using combinatorial peptide libraries: discovery of peptide antagonists of estrogen receptors alpha and beta.", MOLECULAR AND CELLULAR BIOLOGY. DEC 1999, vol. 19, no. 12, December 1999 (1999-12-01), pages 8226 - 8239, XP001120691, ISSN: 0270-7306
  • [PX] GEISTLINGER T R ET AL: "An inhibitor of the interaction of thyroid hormone receptor beta and glucocorticoid interacting protein 1.", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY. 21 FEB 2001, vol. 123, no. 7, 21 February 2001 (2001-02-21), pages 1525 - 1526, XP002307472, ISSN: 0002-7863
  • See references of WO 0202488A2

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