Linked Life Data

14622968

Source:http://linkedlifedata.com/resource/pubmed/id/14622968

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
2003-11-18
pubmed:abstractText
The ligand-binding domain (LBD) of the human retinoic acid receptor-related orphan receptor (RORalpha-LBD), expressed in Sf9 cells, was purified and analyzed by electrospray ionization-mass spectrometry (ESI-MS). ESI-MS operated under native conditions showed the presence of a fortuitous ligand with molecular weight 386. Further analysis by gas chromatography-mass spectrometry (GC-MS) allowed the identification of the ligands bound to the LBD. Cholesterol (77%) and 7-dehydrocholesterol (provitamin D(3); 18%) were shown to be the major ligands. A monohydroxylated cholesterol derivative was identified as a minor ligand. In addition, ligand exchange experiments monitored by ESI-MS showed that cholesterol sulfate has a higher affinity for RORalpha-LBD than cholesterol and 25-hydroxycholesterol. Binding of coactivator (CoA) peptide GRIP1P was shown to occur in a stoichiometric manner. Therefore, monitoring of binding of CoAs by mass spectrometry could be used for classification of the ligands as agonist or antagonist molecules.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Dec
pubmed:issn
0003-2697
pubmed:author
pubmed:issnType
Print
pubmed:day
1
pubmed:volume
323
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
139-49
pubmed:dateRevised
2009-11-19
pubmed:meshHeading
pubmed-meshheading:14622968-Animals, pubmed-meshheading:14622968-Binding Sites, pubmed-meshheading:14622968-Carrier Proteins, pubmed-meshheading:14622968-Cell Line, pubmed-meshheading:14622968-Cholesterol, pubmed-meshheading:14622968-Cloning, Molecular, pubmed-meshheading:14622968-Gas Chromatography-Mass Spectrometry, pubmed-meshheading:14622968-Humans, pubmed-meshheading:14622968-Ligands, pubmed-meshheading:14622968-Nerve Tissue Proteins, pubmed-meshheading:14622968-Nuclear Receptor Subfamily 1, Group F, Member 1, pubmed-meshheading:14622968-Protein Structure, Tertiary, pubmed-meshheading:14622968-Receptors, AMPA, pubmed-meshheading:14622968-Receptors, Cytoplasmic and Nuclear, pubmed-meshheading:14622968-Spectrometry, Mass, Electrospray Ionization, pubmed-meshheading:14622968-Trans-Activators
pubmed:year
2003
pubmed:articleTitle
Identification of natural ligands of retinoic acid receptor-related orphan receptor alpha ligand-binding domain expressed in Sf9 cells--a mass spectrometry approach.
pubmed:affiliation
Central Technologies, Novartis Institutes for Biomedical Research, Lichtstrasse 35, CH-4002 Basel, Switzerland. francis.bitsch@pharma.novartis.com
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't