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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
17
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pubmed:dateCreated |
1994-9-22
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pubmed:abstractText |
Screening a diverse, combinatorial library of ca. 5000 synthetic dimer and trimer N-(substituted)glycine "peptides" yielded novel, high-affinity ligands for 7-transmembrane G-protein-coupled receptors. The peptoid library was efficiently assembled using readily available chemical building blocks. The choice of side chains was biased to resemble known ligands to 7-transmembrane G-protein-coupled receptors. All peptides were screened in solution-phase, competitive radioligand-binding assays. Peptoid trimer CHIR 2279 binds to the alpha 1-adrenergic receptor with a Ki of 5 nM, and trimer CHIR 4531 binds to the mu-opiate receptor with a Ki of 6 nM. This represents the first example of the discovery of high-affinity receptor ligands from a combinatorial library of non-natural chemical entities.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Dipeptides,
http://linkedlifedata.com/resource/pubmed/chemical/Enkephalin, Ala(2)-MePhe(4)-Gly(5)-,
http://linkedlifedata.com/resource/pubmed/chemical/Enkephalins,
http://linkedlifedata.com/resource/pubmed/chemical/GTP-Binding Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Glycine,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Oligopeptides,
http://linkedlifedata.com/resource/pubmed/chemical/Peptoids,
http://linkedlifedata.com/resource/pubmed/chemical/Prazosin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, alpha-1,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Cell Surface,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Opioid, mu
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
19
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pubmed:volume |
37
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pubmed:owner |
NLM
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pubmed:authorsComplete |
N
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pubmed:pagination |
2678-85
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:8064796-Amino Acid Sequence,
pubmed-meshheading:8064796-Animals,
pubmed-meshheading:8064796-Binding, Competitive,
pubmed-meshheading:8064796-Brain,
pubmed-meshheading:8064796-Databases, Factual,
pubmed-meshheading:8064796-Dipeptides,
pubmed-meshheading:8064796-Enkephalin, Ala(2)-MePhe(4)-Gly(5)-,
pubmed-meshheading:8064796-Enkephalins,
pubmed-meshheading:8064796-GTP-Binding Proteins,
pubmed-meshheading:8064796-Glycine,
pubmed-meshheading:8064796-Ligands,
pubmed-meshheading:8064796-Molecular Sequence Data,
pubmed-meshheading:8064796-Molecular Structure,
pubmed-meshheading:8064796-Oligopeptides,
pubmed-meshheading:8064796-Peptoids,
pubmed-meshheading:8064796-Prazosin,
pubmed-meshheading:8064796-Radioligand Assay,
pubmed-meshheading:8064796-Rats,
pubmed-meshheading:8064796-Receptors, Adrenergic, alpha-1,
pubmed-meshheading:8064796-Receptors, Cell Surface,
pubmed-meshheading:8064796-Receptors, Opioid, mu,
pubmed-meshheading:8064796-Structure-Activity Relationship
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pubmed:year |
1994
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pubmed:articleTitle |
Discovery of nanomolar ligands for 7-transmembrane G-protein-coupled receptors from a diverse N-(substituted)glycine peptoid library.
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pubmed:affiliation |
Chiron Corporation, Emeryville, California 94608.
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pubmed:publicationType |
Journal Article,
Comparative Study
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