Global Patent Index - EP 0979407 A1

EP 0979407 A1 2000-02-16 - METHODS FOR IDENTIFYING LIGANDS FOR NUCLEAR HORMONE RECEPTORS

Title (en)

METHODS FOR IDENTIFYING LIGANDS FOR NUCLEAR HORMONE RECEPTORS

Title (de)

VERFAHREN ZUM IDENTIFIZIEREN VON LIGANDEN FÜR HORMONRECEPTOREN

Title (fr)

PROCEDE D'IDENTIFICATION DE LIGANDS POUR RECEPTEURS D'HORMONES NUCLEAIRES

Publication

EP 0979407 A1 (EN)

Application

EP 98915218 A

Priority

  • US 9806446 W
  • US 84662097 A

Abstract (en)

[origin: WO9849555A1] Fatty acids (FAs) and their derivatives are essential cellular metabolites whose concentations must be closely regulated. This implies that regulatory circuits exist which can sense changes in FA levels. Indeed, the peroxisome proliferator activated receptor alpha (PPAR alpha ) regulates lipid homeostasis and is transcriptionally activated by a variety of lipid-like compounds. It remains unclear as to how these structurally-diverse compounds can activate a single receptor. In accordance with the present invention, there are provided conformation-based assays which screen activators for their ability to bind to PPARs (i.e., PPAR alpha , PPAR delta and PPAR gamma ) and induce DNA binding. It is shown here that specific FAs, eicosanoids and lipomodulatory agents are ligands for PPAR alpha , PPAR delta and/or PPAR gamma . Since altered FA levels are associated with obesity, atherosclerosis, hypertension and diabetes, PPARs may serve as molecular sensors which are central to the development and treatment of these metabolic disorders.

IPC 1-7 (main, further and additional classification)

G01N 33/02; G01N 33/03; G01N 33/53; G01N 33/566

IPC 8 full level (invention and additional information)

G01N 33/566 (2006.01)

CPC (invention and additional information)

G01N 33/566 (2013.01)

Citation (search report)

See references of WO 9849555A1

Designated contracting state (EPC)

AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE

EPO simple patent family

WO 9849555 A1 19981105; AU 6945898 A 19981124; CA 2288978 A1 19981105; EP 0979407 A1 20000216

INPADOC legal status


2001-08-29 [18W] WITHDRAWN

- Date of withdrawal: 20010626

2000-02-16 [17P] REQUEST FOR EXAMINATION FILED

- Effective date: 19991125

2000-02-16 [AK] DESIGNATED CONTRACTING STATES:

- Kind Code of Ref Document: A1

- Designated State(s): AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE