Linked Life Data

16399409

Source:http://linkedlifedata.com/resource/pubmed/id/16399409

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:dateCreated
2006-1-9
pubmed:abstractText
The ecdysone receptor (EcR) belongs to the superfamily of nuclear receptors (NRs) that are ligand-dependent transcription factors. Ecdysone receptor is present only in invertebrates and plays a central role in regulating the expression of a vast array of genes during development and reproduction. The functional entity is a heterodimer composed of EcR and the ultraspiracle protein (USP)-the orthologue of the vertebrate retinoid X receptor (RXR). Ecdysone receptor is the molecular target of ecdysteroids-the endogenous steroidal molting hormones found in arthropods and nonarthropod invertebrates. In addition, EcR is the target of the environmentally safe bisacylhydrazine insecticides used against pests, such as caterpillars, that cause severe damage to agriculture. The crystal structures of the ligand-binding domains (LBDs) of the EcR/USP heterodimer, complexed to the ecdysteroid ponasterone A (ponA) and to the lepidopteran specific bisacylhydrazine BYI06830 used in the agrochemical pest control, provide the first insight at atomic level for these important functional complexes. The EcR/USP heterodimer has a shape similar to that seen for the known vertebrate heterodimer complexes with a conserved main interface, but with features, that are specific to this invertebrate heterodimer. The two EcR-LBD structures in complex with steroidal and nonsteroidal ligands reveal substantial differences. The adaptability of EcR to its ligand results in two radically different and only partially overlapping ligand-binding pockets with different residues involved in ligand recognition. The concept brought by these structural studies of a ligand-dependent binding pocket has potential applications for other NRs.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
0083-6729
pubmed:author
pubmed:issnType
Print
pubmed:volume
73
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
101-29
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
2005
pubmed:articleTitle
Ligand-binding pocket of the ecdysone receptor.
pubmed:affiliation
IGBMC, Laboratoire de génomique et Biologie Structurales, CNRS/INSERM/Université Louis Pasteur, Parc d'Innovation BP10142 67404 Illkirch cedex, France.
pubmed:publicationType
Journal Article, Review, Research Support, Non-U.S. Gov't