Abstract
A series of 30 RCO-HfR-NH(2) derivatives show preference for the mouse MC1R vs MC3-5Rs. trans-4-HOC(6)H(4)CH=CHCO-HfR-NH(2) (13) [EC(50) (nM): MC1R 83, MC3R 20500, MC4R 18130 and MC5R 935; ratio 1:246:217:11] is 11 times more potent than the lead compound LK-394 Ph(CH(2))(3)CO-HfR-NH(2) (2) and only 11 times less potent than the native tridecapeptide alpha-MSH at mMC1R. Differences in conformations of 2 and 13 are discussed.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Acid Sequence
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Animals
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Binding Sites
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Computer Simulation
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Mice
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Molecular Conformation
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Peptides / chemical synthesis
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Peptides / chemistry*
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Peptides / pharmacology
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Protein Isoforms / agonists
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Protein Isoforms / metabolism
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Receptors, Melanocortin / agonists*
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Receptors, Melanocortin / metabolism
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alpha-MSH / chemistry
Substances
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Peptides
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Protein Isoforms
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Receptors, Melanocortin
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alpha-MSH