PMID- 10198642
OWN - NLM
STAT- MEDLINE
DCOM- 19990426
LR  - 20220330
IS  - 1097-2765 (Print)
IS  - 1097-2765 (Linking)
VI  - 3
IP  - 3
DP  - 1999 Mar
TI  - Molecular recognition of fatty acids by peroxisome proliferator-activated
      receptors.
PG  - 397-403
AB  - 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.
FAU - Xu, H E
AU  - Xu HE
AD  - Glaxo Wellcome Research and Development, Research Triangle Park, North Carolina
      27709, USA.
FAU - Lambert, M H
AU  - Lambert MH
FAU - Montana, V G
AU  - Montana VG
FAU - Parks, D J
AU  - Parks DJ
FAU - Blanchard, S G
AU  - Blanchard SG
FAU - Brown, P J
AU  - Brown PJ
FAU - Sternbach, D D
AU  - Sternbach DD
FAU - Lehmann, J M
AU  - Lehmann JM
FAU - Wisely, G B
AU  - Wisely GB
FAU - Willson, T M
AU  - Willson TM
FAU - Kliewer, S A
AU  - Kliewer SA
FAU - Milburn, M V
AU  - Milburn MV
LA  - eng
PT  - Journal Article
PL  - United States
TA  - Mol Cell
JT  - Molecular cell
JID - 9802571
RN  - 0 (Butyrates)
RN  - 0 (Fatty Acids)
RN  - 0 (GW 2433)
RN  - 0 (Ligands)
RN  - 0 (Phenylurea Compounds)
RN  - 0 (Receptors, Cytoplasmic and Nuclear)
RN  - 0 (Transcription Factors)
RN  - AAN7QOV9EA (Eicosapentaenoic Acid)
SB  - IM
MH  - Animals
MH  - Binding Sites
MH  - Butyrates/chemistry/metabolism
MH  - Crystallization
MH  - Crystallography, X-Ray
MH  - Eicosapentaenoic Acid/chemistry/metabolism
MH  - Fatty Acids/chemistry/*metabolism
MH  - Humans
MH  - Hydrogen Bonding
MH  - Inhibitory Concentration 50
MH  - Ligands
MH  - Models, Molecular
MH  - Molecular Conformation
MH  - Phenylurea Compounds/chemistry/metabolism
MH  - Protein Binding
MH  - Protein Conformation
MH  - Protein Structure, Secondary
MH  - Receptors, Cytoplasmic and Nuclear/*chemistry/*metabolism
MH  - Transcription Factors/*chemistry/*metabolism
EDAT- 1999/04/13 00:00
MHDA- 1999/04/13 00:01
CRDT- 1999/04/13 00:00
PHST- 1999/04/13 00:00 [pubmed]
PHST- 1999/04/13 00:01 [medline]
PHST- 1999/04/13 00:00 [entrez]
AID - S1097-2765(00)80467-0 [pii]
AID - 10.1016/s1097-2765(00)80467-0 [doi]
PST - ppublish
SO  - Mol Cell. 1999 Mar;3(3):397-403. doi: 10.1016/s1097-2765(00)80467-0.