Design of potent PPARalpha agonists.

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Sauerberg P, Mogensen JP, Jeppesen L, Bury PS, Fleckner J, Olsen GS, Jeppesen CB, Wulff EM, Pihera P, Havranek M, Polivka Z, Pettersson I

Design of potent PPARalpha agonists.

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3198-202. Epub 2007 Mar 12.

PubMed ID

17379517 [ View in PubMed

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Abstract

Computational analysis of the ligand binding pocket of the three PPAR receptor subtypes was utilized in the design of potent PPARalpha agonists. Optimum PPARalpha potency and selectivity were obtained with substituents having van der Waals volume around 260. Compound 6 had a PPARalpha potency of 0.002 microM and a selectivity ratio to PPARgamma and PPARdelta of 410 and 2000, respectively.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Rosiglitazone	Peroxisome proliferator-activated receptor alpha	EC 50 (nM)	4100	N/A	N/A	Details
Rosiglitazone	Peroxisome proliferator-activated receptor gamma	EC 50 (nM)	200	N/A	N/A	Details