Linked Life Data

17579384

Source:http://linkedlifedata.com/resource/pubmed/id/17579384

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
14
pubmed:dateCreated
2007-7-5
pubmed:abstractText
Kisspeptins (KPs) play important roles in the regulation of physiological and pathological states through activation of the cognate receptor GPR54. Our previous studies to downsize KP agonists to the essential GPR54 pharmacophore identified peptides 1-3 as low molecular weight GPR54 agonists. In this study, the effect of N-terminal acyl groups on the activity of a series of analogues (R-Phe-Gly-Leu-Arg-Trp-NH2) was investigated in order to develop novel potent GPR54 agonists. Among the compounds developed, the most potent agonistic activity for GPR54 was observed for N-terminal 4-fluorobenzoyl analogue 29. Using quantitative structure-activity relationship studies, it was demonstrated that the inductively negative and small substituents were preferred at the 4-position of N-terminal benzoyl groups.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jul
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:day
12
pubmed:volume
50
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
3222-8
pubmed:meshHeading
pubmed:year
2007
pubmed:articleTitle
SAR and QSAR studies on the N-terminally acylated pentapeptide agonists for GPR54.
pubmed:affiliation
Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't