Nuclear receptor ligand-binding domains: three-dimensional structures, molecular interactions and pharmacological implications.

Content Provider	Semantic Scholar
Author	Bourguet, William Germain, Philippe Gronemeyer, Hinrich
Copyright Year	2000
Abstract	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.
File Format	PDF HTM / HTML
DOI	10.1016/S0165-6147(00)01548-0
PubMed reference number	11050318
Journal	Medline
Volume Number	21
Issue Number	10
Alternate Webpage(s)	http://www.cmbi.ru.nl/edu/bioinf4/articles/pdf/nre_Bourguet.pdf
Alternate Webpage(s)	https://doi.org/10.1016/S0165-6147%2800%2901548-0
Journal	Trends in pharmacological sciences
Language	English
Access Restriction	Open
Content Type	Text
Resource Type	Article