Abstract
The identification of the nuclear receptor peroxisome proliferator-activated receptor-alpha (PPARα) as a molecular target of the fibrate class of anti-dyslipidaemic agents and the rapid development of the parallel high-through-put approach to evaluate activity towards other PPAR subtypes (PPARδ and PPARΥ) has provided an opportunity to develop novel PPARα-selective, PPARα/Υ dual and pan-PPAR agonists. This review outlines the molecular pharmacology of PPARα and summarises recent patents (from 2000 to 2003) disclosing medicinal chemical strategies to identify new PPARα agonists. These developments will help us to understand the structure-activity relationship and the interaction between the ligands and PPARα and also help to create novel therapeutic choices for the treatment of metabolic disorders, such as dyslipidaemia, obesity, diabetes and other PPARα-related diseases. 2004
| Original language | English |
|---|---|
| Pages (from-to) | 607-618 |
| Number of pages | 12 |
| Journal | Expert Opinion on Therapeutic Patents |
| Volume | 14 |
| Issue number | 5 |
| DOIs | |
| Publication status | Published - May 2004 |
| Externally published | Yes |
Keywords
- Carboxylic acid
- Dyslipidaemia
- Peroxisome proliferator-activated receptor-α (PPARα)
- Phenoxyacetic acid
- Thiazolidine-2,4-dione
- α-substituted phenylpropanoic acid
ASJC Scopus subject areas
- Pharmacology
- Drug Discovery
