期刊
PHARMACOLOGY & THERAPEUTICS
卷 183, 期 -, 页码 152-159出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.pharmthera.2017.10.014
关键词
Allostery; Nuclear receptor; Transcription; Drug design; Endocrine; Genome-scale
资金
- NIH [GM123469]
- NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES [R15GM123469] Funding Source: NIH RePORTER
The nuclear receptor family of transcription factor proteins mediates endocrine function and plays critical roles in the 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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