Abstract
The understanding of the functions of the nuclear receptor peroxisome proliferator-activated receptor a (PPARalpha) as a regulator of lipid and lipoprotein homeostasis, and the rapid development of parallel high-throughput screening assays to evaluate the activity toward other PPAR subtypes (PPARdelta and PPARgamma), have provided an opportunity to develop novel PPARalpha-selective, PPARalpha/gamma dual and PPAR pan agonists for the treatment of various metabolic diseases. This review focuses on the molecular pharmacology of PPARalpha, and summarizes recent literature and patent applications disclosing medicinal chemistry strategies to identify new PPARalpha-selective agonists. The species selectivity of some classes of PPARalpha-selective agonists in response to in vitro PPARalpha transactivation activity is also reported.
| Original language | English |
|---|---|
| Pages (from-to) | 746-754 |
| Number of pages | 9 |
| Journal | IDrugs |
| Volume | 7 |
| Issue number | 8 |
| Publication status | Published - Aug 2004 |
| Externally published | Yes |
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Keywords
- Metabolic disorders
- Peroxisome proliferatoractivated receptorα
- Phenoxyacetic acid
- Species selectivity
ASJC Scopus subject areas
- Pharmacology
- Drug Discovery
Cite this
Recent progress of the research on peroxisome proliferator-activated receptor α-selective ligands. / Miyachi, Hiroyuki.
In: IDrugs, Vol. 7, No. 8, 08.2004, p. 746-754.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Recent progress of the research on peroxisome proliferator-activated receptor α-selective ligands
AU - Miyachi, Hiroyuki
PY - 2004/8
Y1 - 2004/8
N2 - The understanding of the functions of the nuclear receptor peroxisome proliferator-activated receptor a (PPARalpha) as a regulator of lipid and lipoprotein homeostasis, and the rapid development of parallel high-throughput screening assays to evaluate the activity toward other PPAR subtypes (PPARdelta and PPARgamma), have provided an opportunity to develop novel PPARalpha-selective, PPARalpha/gamma dual and PPAR pan agonists for the treatment of various metabolic diseases. This review focuses on the molecular pharmacology of PPARalpha, and summarizes recent literature and patent applications disclosing medicinal chemistry strategies to identify new PPARalpha-selective agonists. The species selectivity of some classes of PPARalpha-selective agonists in response to in vitro PPARalpha transactivation activity is also reported.
AB - The understanding of the functions of the nuclear receptor peroxisome proliferator-activated receptor a (PPARalpha) as a regulator of lipid and lipoprotein homeostasis, and the rapid development of parallel high-throughput screening assays to evaluate the activity toward other PPAR subtypes (PPARdelta and PPARgamma), have provided an opportunity to develop novel PPARalpha-selective, PPARalpha/gamma dual and PPAR pan agonists for the treatment of various metabolic diseases. This review focuses on the molecular pharmacology of PPARalpha, and summarizes recent literature and patent applications disclosing medicinal chemistry strategies to identify new PPARalpha-selective agonists. The species selectivity of some classes of PPARalpha-selective agonists in response to in vitro PPARalpha transactivation activity is also reported.
KW - Metabolic disorders
KW - Peroxisome proliferatoractivated receptorα
KW - Phenoxyacetic acid
KW - Species selectivity
UR - http://www.scopus.com/inward/record.url?scp=16544373479&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=16544373479&partnerID=8YFLogxK
M3 - Article
C2 - 15334308
AN - SCOPUS:16544373479
VL - 7
SP - 746
EP - 754
JO - IDrugs : the investigational drugs journal
JF - IDrugs : the investigational drugs journal
SN - 1369-7056
IS - 8
ER -