Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 1999 Mar;3(3):397-403.
doi: 10.1016/s1097-2765(00)80467-0.

Molecular recognition of fatty acids by peroxisome proliferator-activated receptors

H E Xu  1 , M H Lambert, V G Montana, D J Parks, S G Blanchard, P J Brown, D D Sternbach, J M Lehmann, G B Wisely, T M Willson, S A Kliewer, M V Milburn
Affiliations
Free article

Molecular recognition of fatty acids by peroxisome proliferator-activated receptors

H E Xu et al. Mol Cell. 1999 Mar.
Free article

Abstract

The peroxisome proliferator-activated receptors (PPARs) are nuclear receptors for fatty acids (FAs) that regulate glucose and lipid homeostasis. We report the crystal structure of the PPAR delta ligand-binding domain (LBD) bound to either the FA eicosapentaenoic acid (EPA) or the synthetic fibrate GW2433. The carboxylic acids of EPA and GW2433 interact directly with the activation function 2 (AF-2) helix. The hydrophobic tail of EPA adopts two distinct conformations within the large hydrophobic cavity. GW2433 occupies essentially the same space as EPA bound in both conformations. These structures provide molecular insight into the propensity for PPARs to interact with a variety of synthetic and natural compounds, including FAs that vary in both chain length and degree of saturation.

PubMed Disclaimer

MeSH terms