Enantio-dependent binding and transactivation of optically active phenylpropanoic acid derivatives at human peroxisome proliferator-activated receptor alpha.
Optically active phenylpropanoic acid derivatives [(S)-5, and (R)-5] were prepared, and their affinities for peroxisome proliferator-activated receptor (PPAR)alpha and PPAR gamma were evaluated. Binding assay and cell-based reporter assay indicated that the activity of these compounds is enantio-dependent, and resides exclusively on the (S)-isomer.
Miyachi
Hiroyuki
H
Discovery Research Laboratories, Kyorin Pharmaceutical Co., Ltd., 2399-1Mitarai, Nogi-machi, Shimotsuga-gun, Tochigi 329-0114, Japan. hiroyuki.miyachi@mb2.kyorin-pharm.co.jp
Nomura
Masahiro
M
Tanase
Takahiro
T
Suzuki
Masahiro
M
Murakami
Koji
K
Awano
Katsuya
K
D018360:Crystallography, X-Ray; D006801:Humans; D008968:Molecular Conformation; D010666:Phenylpropionates / Q000138:chemical synthesis* / Q000494:pharmacology*; D011485:Protein Binding; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014157:Transcription Factors / Q000819:agonists*; D015533:Transcriptional Activation
D010666:Phenylpropionates; D018160:Receptors, Cytoplasmic and Nuclear; D014157:Transcription Factors