Linked Life Data

21623631

Source:http://linkedlifedata.com/resource/pubmed/id/21623631

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
13
pubmed:dateCreated
2011-7-7
pubmed:abstractText
26RFa is a new member of the RFamide peptide family that has been identified as the endogenous ligand of the orphan GPCR GPR103. As the C-terminal heptapeptide (26RFa((20-26))) mimics the action of the native peptide on food intake and gonadotropin secretion in rodents, we have synthesized a series of analogues of 26RFa((20-26)) and measured their potency to induce [Ca(2+)](i) mobilization in G?(16)-hGPR103-transfected CHO cells. Systematic replacement of each residue by an alanine (Ala scan) and its D-enantiomer (D scan) showed that the last three C-terminal residues were very sensitive to the substitutions while position 23 tolerated rather well both modifications. Most importantly, replacement of Ser(23) by a norvaline led to an analogue, [Nva(23)]26RFa((20-26)), that was 3-fold more potent than the native heptapeptide. These new pharmacological data, by providing the first information regarding the structure-activity relationships of 26RFa analogues, should prove useful for the rational design of potent GPR103 receptor ligands with potential therapeutic application.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jul
pubmed:issn
1520-4804
pubmed:author
pubmed:issnType
Electronic
pubmed:day
14
pubmed:volume
54
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
4806-14
pubmed:dateRevised
2011-10-13
pubmed:meshHeading
pubmed:year
2011
pubmed:articleTitle
Structure-activity relationships of a series of analogues of the RFamide-related peptide 26RFa.
pubmed:affiliation
INSERM U982, Laboratory of Neuronal and Neuroendocrine Differentiation and Communication, European Institute for Peptide Research (IFRMP 23), Cell Imaging Platform (PRIMACEN), University of Rouen, 76821 Mont-Saint-Aignan, France.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't