Enantio-dependent binding and transactivation of optically active phenylpropanoic acid derivatives at human peroxisome proliferator-activated receptor alpha.

Enantio-dependent binding and transactivation of optically active phenylpropanoic acid derivatives at human peroxisome proliferator-activated receptor alpha.
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光学活性苯丙酸衍生物在人过氧化物酶体增殖物激活受体α上的对映依赖性结合和反式激活。

DOI:
10.1016/s0960-894x(01)00732-6
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发表时间:
2002
影响因子:
2.7
通讯作者:
K. Awano
K. Awano
中科院分区:
医学4区
文献类型:
--
作者:
H. Miyachi;M. Nomura;T. Tanase;Masahiro Suzuki;K. Murakami;K. Awano

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制备光学活性苯丙酸衍生物[(S)-5和(R)-5],并评估它们与过氧化物酶体增殖物激活受体(PPAR)α和PPARγ的亲和力。结合测定和基于细胞的报告基因测定表明这些化合物的活性是对映体依赖性的,并且仅存在于(S)-异构体上。
Optically active phenylpropanoic acid derivatives [(S)-5, and (R)-5] were prepared, and their affinities for peroxisome proliferator-activated receptor (PPAR)α and PPARγ 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.
DOI: 10.1038/347645a0
发表时间: 1990-10-18
期刊: NATURE
影响因子: 64.8
作者:
ISSEMANN, I;GREEN, S
通讯作者: GREEN, S