Linked Life Data

20307531

Source:http://linkedlifedata.com/resource/pubmed/id/20307531

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PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1-3
pubmed:dateCreated
2010-4-30
pubmed:abstractText
Neuropeptide S and its receptor represent a novel neurotransmitter system mainly expressed in the brain. A single nucleotide polymorphism in the first extracellular loop (I107) increases the potency of neuropeptide S and has been identified for both the human neuropeptide S receptor short (A) and long (B) C-terminal forms. Preliminary human genetic studies link this polymorphism to asthma, panic disorders and altered sleep behavior. No polymorphism or splice variants have been reported for the rat neuropeptide S receptor, however it carries an isoleucine at position 107. To identify a suitable tracer for neuropeptide S receptor binding and investigate the role of specific amino acids within neuropeptide S we carried out mutagenesis of the peptide and assessed the ability of the mutations to stimulate calcium release in HEK293 cells expressing human neuropeptide S receptor variants (A, B, AI(107), BI(107)) and rat neuropeptide S receptor. Replacement of threonine at position 8 by arginine and methionine at position 10 by tyrosine resulted in a mutant peptide slightly more potent on all neuropeptide S receptor variants compared to neuropeptide S and more importantly the iodinated mutant peptide was found to be a suitable tracer for binding studies with improved signal to noise ratio and stability compared to [(125)I-Y(10)] neuropeptide S. Replacement of serine at position 1 of neuropeptide S peptide by arginine resulted in a complete loss of potency for the neuropeptide S receptor (long and short form) but not for the I(107) receptor variants (long and short) or rat neuropeptide S receptor.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
1879-0712
pubmed:author
pubmed:issnType
Electronic
pubmed:day
10
pubmed:volume
635
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
27-33
pubmed:meshHeading
pubmed:year
2010
pubmed:articleTitle
Mutagenesis studies of neuropeptide S identify a suitable peptide tracer for neuropeptide S receptor binding studies and peptides selectively activating the I(107) variant of human neuropeptide S receptor.
pubmed:affiliation
Johnson & Johnson Pharmaceutical Research & Development, L.L.C., San Diego, CA 92121, USA. dnepomuc@its.jnj.com
pubmed:publicationType
Journal Article