Nadal A, Ropero A B, Laribi O, Maillet M, Fuentes E, Soria B
Institute of Bioengineering, Department of Physiology, and Department of Applied Biology, Miguel Hernández University, San Juan Campus, Alicante 03550, Spain.
Proc Natl Acad Sci U S A. 2000 Oct 10;97(21):11603-8. doi: 10.1073/pnas.97.21.11603.
The molecular mechanism used by environmental chemicals to exert their hormone-like actions is still only partially resolved. Although it generally is accepted that xenoestrogens act at the genomic level by binding to intracellular estrogen receptors, we have shown here that they trigger nongenomic effects in pancreatic beta cells. Both xenoestrogens and the circulating hormone, 17beta-estradiol, bind with high affinity to a common membrane binding site unrelated to the intracellular estrogen receptors ERalpha and ERbeta. This binding site is shared by dopamine, epinephrine, and norepinephrine and has the pharmacological profile of the gammaadrenergic receptor. This study provides an outline of the membrane receptor involved in rapid xenoestrogen actions.
环境化学物质发挥其类激素作用所采用的分子机制目前仍仅得到部分解析。尽管人们普遍认为外源性雌激素通过与细胞内雌激素受体结合而在基因组水平发挥作用，但我们在此已表明，它们可在胰腺β细胞中引发非基因组效应。外源性雌激素和循环激素17β-雌二醇均以高亲和力与一个与细胞内雌激素受体ERα和ERβ无关的共同膜结合位点相结合。多巴胺、肾上腺素和去甲肾上腺素也共享这个结合位点，并且它具有γ肾上腺素能受体的药理学特征。本研究概述了参与外源性雌激素快速作用的膜受体。
