Linked Life Data

19746979

Source:http://linkedlifedata.com/resource/pubmed/id/19746979

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
19
pubmed:dateCreated
2009-10-1
pubmed:abstractText
The neurokinin NK2 receptor is known to pre-exist in equilibrium between at least three states: resting-inactive, calcium-triggering, and cAMP-producing. Its endogeneous ligand, NKA, mainly induces the calcium response. Using a FRET-based assay, we have previously discovered an allosteric modulator of the NK2 receptor that has the unique ability to discriminate among the two signaling pathways: calcium-signaling is not affected while cAMP signaling is significantly decreased. A series of compounds have been prepared and studied in order to better understand the structural determinants of this allosteric functional switch of a GPCR. Most of them display the same allosteric profile, with smooth pharmacomodulation. One compound however exhibits significantly improved modulatory properties of NKA induced signaling when compared to the original modulator.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Oct
pubmed:issn
1520-4804
pubmed:author
pubmed:issnType
Electronic
pubmed:day
8
pubmed:volume
52
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
5999-6011
pubmed:meshHeading
pubmed:year
2009
pubmed:articleTitle
Allosteric functional switch of neurokinin A-mediated signaling at the neurokinin NK2 receptor: structural exploration.
pubmed:affiliation
UMR UdS/CNRS 7200, Laboratoire d'Innovation Thérapeutique, Faculté de Pharmacie, Illkirch, France.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't