Linked Life Data

19664655

Source:http://linkedlifedata.com/resource/pubmed/id/19664655

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
2009-9-22
pubmed:abstractText
G protein-coupled receptors (GPCR) are targeted by many therapeutic drugs marketed to fight against a variety of diseases. Selection of novel lead compounds are based on pharmacological parameters obtained assuming that GPCR are monomers. However, many GPCR are expressed as dimers/oligomers. Therefore, drug development may consider GPCR as homo- and hetero-oligomers. A two-state dimer receptor model is now available to understand GPCR operation and to interpret data obtained from drugs interacting with dimers, and even from mixtures of monomers and dimers. Heteromers are distinct entities and therefore a given drug is expected to have different affinities and different efficacies depending on the heteromer. All these concepts would lead to broaden the therapeutic potential of drugs targeting GPCRs, including receptor heteromer-selective drugs with a lower incidence of side effects, or to identify novel pharmacological profiles using cell models expressing receptor heteromers.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Nov
pubmed:issn
1879-016X
pubmed:author
pubmed:issnType
Electronic
pubmed:volume
124
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
248-57
pubmed:meshHeading
pubmed:year
2009
pubmed:articleTitle
GPCR homomers and heteromers: a better choice as targets for drug development than GPCR monomers?
pubmed:affiliation
Departament de Bioquímica i Biologia Molecular, CIBERNED (Centro de Investigación en Red de Enfermedades Neurodegenerativas) and Institut d'Investigacions Biomèdiques August Pi i Sunyer (IDIBAPS) Universitat de Barcelona, 08028 Barcelona, Catalonia, Spain.
pubmed:publicationType
Journal Article, Comparative Study, Review, Research Support, Non-U.S. Gov't, Research Support, N.I.H., Intramural