Nuclear receptor ligand-binding domains: three-dimensional structures, molecular interactions and pharmacological implications.
Trends Pharmacol Sci
; 21(10): 381-8, 2000 Oct.
Article
in En
| MEDLINE
| ID: mdl-11050318
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.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Receptors, Cytoplasmic and Nuclear
Limits:
Animals
/
Humans
Language:
En
Journal:
Trends Pharmacol Sci
Year:
2000
Document type:
Article
Affiliation country:
France