期刊
TRENDS IN PHARMACOLOGICAL SCIENCES
卷 21, 期 10, 页码 381-388出版社
ELSEVIER SCIENCE LONDON
DOI: 10.1016/S0165-6147(00)01548-0
关键词
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Nuclear receptors are members of a large family of ligand-inducible transcription factors that regulate gene programs underlying a plethora of (patho)physiological phenomena. The recent determination of the crystal structures of nuclear receptor ligand-binding domains has provided an extremely detailed insight into the intra- and intermolecular mechanisms that constitute the initial events of receptor activation and signal transduction. Here, a comprehensive mechanistic view of agonist and antagonist action will be presented. Furthermore, the novel class of partial agonists-antagonists will be described and the multiple challenges and novel perspectives for nuclear-receptor-based drug design will be discussed.
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