Source:http://linkedlifedata.com/resource/pubmed/id/14971895
Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
5
|
pubmed:dateCreated |
2004-2-19
|
pubmed:abstractText |
The neuropeptides orexin A and B (also known as hypocretins) play an important role in many physiological and behavioral activities. Orexins are ligands of two closely related G-protein-coupled receptors, that are the named orexin 1 and orexin 2 receptors. To clearly identify the minimal ligand sequences required for receptor activation, we synthesized and analyzed different centrally, C- and N-terminally truncated analogues of orexins A and B. Furthermore, we used the shortest active analogue to screen for important amino acid residues by l-alanine and l-proline replacement scans. For orexin A, only full-length peptides were able to show the same activity as orexin A, but interestingly, reduced orexin A and natural orexin A, which contains the two disulfide bonds, had the same activity. The shortest highly active orexin B analogue was orexin B 6-28. In addition, we identified orexin A 2-33 as the first analogue with orexin 1 receptor preference and orexin B 10-28, [A27]orexin B 6-28, and [P11]orexin B 6-28 as being highly potent orexin 2 receptor selective (>1000-fold) peptides.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Calcium,
http://linkedlifedata.com/resource/pubmed/chemical/Carrier Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Intracellular Signaling Peptides...,
http://linkedlifedata.com/resource/pubmed/chemical/Neuropeptides,
http://linkedlifedata.com/resource/pubmed/chemical/Oligopeptides,
http://linkedlifedata.com/resource/pubmed/chemical/Peptide Fragments,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, G-Protein-Coupled,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Neuropeptide,
http://linkedlifedata.com/resource/pubmed/chemical/orexin receptors,
http://linkedlifedata.com/resource/pubmed/chemical/orexins
|
pubmed:status |
MEDLINE
|
pubmed:month |
Feb
|
pubmed:issn |
0022-2623
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:day |
26
|
pubmed:volume |
47
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1153-60
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:14971895-Calcium,
pubmed-meshheading:14971895-Carrier Proteins,
pubmed-meshheading:14971895-Cell Line,
pubmed-meshheading:14971895-Humans,
pubmed-meshheading:14971895-Intracellular Signaling Peptides and Proteins,
pubmed-meshheading:14971895-Neuropeptides,
pubmed-meshheading:14971895-Oligopeptides,
pubmed-meshheading:14971895-Peptide Fragments,
pubmed-meshheading:14971895-Receptors, G-Protein-Coupled,
pubmed-meshheading:14971895-Receptors, Neuropeptide,
pubmed-meshheading:14971895-Structure-Activity Relationship
|
pubmed:year |
2004
|
pubmed:articleTitle |
Structure-activity studies of orexin a and orexin B at the human orexin 1 and orexin 2 receptors led to orexin 2 receptor selective and orexin 1 receptor preferring ligands.
|
pubmed:affiliation |
Institute of Biochemistry, University of Leipzig, Germany.
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|