Linked Life Data

19513650

Source:http://linkedlifedata.com/resource/pubmed/id/19513650

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:dateCreated
2009-6-10
pubmed:abstractText
G protein-coupled receptors (GPCRs) represent the largest class of targets in drug discovery, one-third of all marketed drugs are active at GPCRs and drugs targeted at GPCRs are marketed in virtually every therapeutic area. GPCRs can be classified by virtue of their coupling to second messenger signaling systems. In the last decade functional evaluation of Galphaq-coupled GPCRs has been enabled by advances in fluorescence dye-based methodologies and detection instrumentation. Investigations into the bioluminescence of jelly fish in the early 1960s isolated the photoprotein aequorin that required only the addition of calcium to generate a luminescent signal. The recent development of sensitive detection platforms with integrated fluidics for liquid handling has revived interest in bioluminescence as an alternative to chemical fluorophore-based detection for characterizing the pharmacology of this target class. In this chapter we describe a detailed methodology for the development and execution of bioluminescence apoprotein aequorin-based screens for hit identification and structure-activity relationship compound profiling and highlight the opportunities and challenges associated with this technique.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:issn
1064-3745
pubmed:author
pubmed:issnType
Print
pubmed:volume
552
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
181-98
pubmed:meshHeading
pubmed:year
2009
pubmed:articleTitle
Use of aequorin for G protein-coupled receptor hit identification and compound profiling.
pubmed:affiliation
Department of Screening and Compound Profiling, GlaxoSmithKline, Essex, UK.
pubmed:publicationType
Journal Article