Allosteric pathways in nuclear receptors - Potential targets for drug design.
Allosteric pathways in nuclear receptors - Potential targets for drug design.
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DOI：
10.1016/j.pharmthera.2017.10.014
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发表时间：
2018-03
影响因子：
13.5
通讯作者：
Fernandez EJ
中科院分区：
文献类型：
--
作者：
Fernandez EJ
核受体家族的转录因子蛋白介导内分泌功能，并在发育，生理和药理学中发挥关键作用。核受体功能障碍与几种疾病状态有关。核受体的功能活性由小分子激素和合成分子调节。多种证据来源已经确定并区分了由配体、DNA和辅因子（如辅激活子和辅抑制子）启动的不同变构途径。此外，这些生物物理学研究正试图确定这些调节辅激活因子和DNA识别的途径如何控制基因转录。因此，有越来越多的兴趣在确定核受体变构的基因组规模的影响。今天，人们普遍认为，详细了解核受体分子复合物内的变构调节途径将能够长期开发有效的药物疗法。
The nuclear receptor family of transcription factor proteins mediate endocrine function and play critical roles in development, physiology and pharmacology. Malfunctioning nuclear receptors are associated with several disease states. The functional activity of nuclear receptors is regulated by small molecular hormonal and synthetic molecules. Multiple sources of evidence have identified and distinguished between the different allosteric pathways initiated by ligands, DNA and cofactors such as co-activators and co-repressors. Also, these biophysical studies are attempting to determine how these pathways that regulate co-activator and DNA recognition can control gene transcription. Thus, there is a growing interest in determining the genome-scale impact of allostery in nuclear receptors. Today, it is accepted that a detailed understanding of the allosteric regulatory pathways within the nuclear receptor molecular complex will enable the development of efficient drug therapies in the long term.
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影响因子：
4.8
作者：
Ding, Xunshan;Lichti, Kristin;Staudinger, Jeff L.
通讯作者：
Staudinger, Jeff L.
影响因子：
10.5
作者：
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影响因子：
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作者：
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通讯作者：
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DOI：
10.1073/pnas.95.21.12208
发表时间：
1998-10-13
影响因子：
11.1
作者：
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通讯作者：
Berkenstam, A
影响因子：
4.8
作者：
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通讯作者：
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