Abstract
A series of pentapeptides, based on hMC4R pentapeptide agonist (Bu-His(6)-DPhe(7)-Arg(8)-Trp(9)-Gly(10)-NH(2)), was prepared in which either DPhe(7) or Trp(9) residue was systematically substituted. A number of interesting DPhe surrogates (D-Thi, D-3-CF(3)Phe, D-2-Nal and D-3,4-diClPhe) as well as Trp surrogates (2-Nal and Bta) were identified in this study.
MeSH terms
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Amino Acid Substitution
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Cell Line
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Humans
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Obesity / drug therapy
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Oligopeptides / chemistry
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Oligopeptides / pharmacology*
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Receptor, Melanocortin, Type 4 / agonists*
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Receptor, Melanocortin, Type 4 / genetics
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Receptors, Melanocortin / agonists*
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Receptors, Melanocortin / genetics
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Structure-Activity Relationship
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Transfection
Substances
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Bu-His(6)-Phe(7)-Arg(8)-Trp(9)-Gly(10)-NH(2)
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Oligopeptides
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Receptor, Melanocortin, Type 4
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Receptors, Melanocortin