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rdf:type |
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lifeskim:mentions |
umls-concept:C0020205,
umls-concept:C0022914,
umls-concept:C0026667,
umls-concept:C0086418,
umls-concept:C0243071,
umls-concept:C0254370,
umls-concept:C0439282,
umls-concept:C0439596,
umls-concept:C0537521,
umls-concept:C1167622,
umls-concept:C1510827,
umls-concept:C1514721
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pubmed:issue |
10
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pubmed:dateCreated |
2011-5-2
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pubmed:abstractText |
A novel hybrid melanocortin pharmacophore was designed based on the topographical similarities between the pharmacophores of Agouti related protein (AGRP) an endogenous melanocortin antagonist, and ?-melanocyte-stimulating hormone (?-MSH), an endogenous melanocortin agonist. When employed in two different 23-membered macrocyclic lactam peptide templates, the designed hybrid AGRP/MSH pharmacophore yielded non-competitive ligands with nanomolar range binding affinities. The topography-based pharmacophore hybridization strategy will prove useful in development of unique non-competitive melanocortin receptor modulators.
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pubmed:grant |
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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 |
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
1464-3405
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pubmed:author |
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pubmed:copyrightInfo |
Published by Elsevier Ltd.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
21
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3099-102
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pubmed:dateRevised |
2011-10-21
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pubmed:meshHeading |
pubmed-meshheading:21486697-Agouti-Related Protein,
pubmed-meshheading:21486697-Amino Acid Sequence,
pubmed-meshheading:21486697-Binding, Competitive,
pubmed-meshheading:21486697-Cyclization,
pubmed-meshheading:21486697-Drug Design,
pubmed-meshheading:21486697-Humans,
pubmed-meshheading:21486697-Inhibitory Concentration 50,
pubmed-meshheading:21486697-Lactams,
pubmed-meshheading:21486697-Ligands,
pubmed-meshheading:21486697-Molecular Sequence Data,
pubmed-meshheading:21486697-Protein Binding,
pubmed-meshheading:21486697-Receptors, Melanocortin,
pubmed-meshheading:21486697-alpha-MSH
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pubmed:year |
2011
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pubmed:articleTitle |
Cyclic lactam hybrid ?-MSH/Agouti-related protein (AGRP) analogues with nanomolar range binding affinities at the human melanocortin receptors.
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pubmed:affiliation |
Department of Chemistry and Biochemistry, University of Arizona, Tucson, AZ 85721, USA.
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pubmed:publicationType |
Journal Article,
Research Support, N.I.H., Extramural
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