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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
22
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pubmed:dateCreated |
2005-10-5
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pubmed:abstractText |
Linear pentapeptides (Penta-cis-Apc-DPhe-Arg-Trp-Gly-NH2) containing 1-amino-4-phenylcyclohexane-1-carboxylic acid (cis-Apc) and substituted Apc are potent hMC4R agonists and they are inactive or weakly active in hMC1R, hMC3R, and hMC5R agonist assays. This study, together with our earlier report on 5-BrAtc, demonstrated the importance of replacing His6 with phenyl-containing rigid templates in achieving good hMC4R agonist potency and selectivity against hMC1R in linear pentapeptides.
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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 |
Nov
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:BartkovitzDavidD,
pubmed-author:ChenLiL,
pubmed-author:CheungAdrian Wai-HingAW,
pubmed-author:ChuXin-JieXJ,
pubmed-author:DanhoWaleedW,
pubmed-author:FrancoLuciaL,
pubmed-author:KurylkoGrazynaG,
pubmed-author:QiLidaL,
pubmed-author:RowanKarenK,
pubmed-author:SwistokJosephJ,
pubmed-author:YagaloffKeithK,
pubmed-author:YeonMitchM
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pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
15
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4910-4
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pubmed:meshHeading |
pubmed-meshheading:16169218-Amino Acid Sequence,
pubmed-meshheading:16169218-Carboxylic Acids,
pubmed-meshheading:16169218-Cyclohexanes,
pubmed-meshheading:16169218-Humans,
pubmed-meshheading:16169218-Inhibitory Concentration 50,
pubmed-meshheading:16169218-Molecular Structure,
pubmed-meshheading:16169218-Receptor, Melanocortin, Type 1,
pubmed-meshheading:16169218-Receptor, Melanocortin, Type 4,
pubmed-meshheading:16169218-Sensitivity and Specificity,
pubmed-meshheading:16169218-Substrate Specificity
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pubmed:year |
2005
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pubmed:articleTitle |
Discovery of 1-amino-4-phenylcyclohexane-1-carboxylic acid and its influence on agonist selectivity between human melanocortin-4 and -1 receptors in linear pentapeptides.
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pubmed:affiliation |
Roche Research Center, Hoffmann-La Roche Inc., 340 Kingsland Street, Nutley, NJ 07110, USA. xin-jie.chu@roche.com
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pubmed:publicationType |
Journal Article
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