Abstract
A series of novel, disulfide-constrained human beta-melanocyte stimulating hormone (beta-MSH)-derived peptides were optimized for in vitro melanocortin-4 receptor (MC-4R) binding affinity, agonist efficacy, and selectivity. The most promising of these, analogue 18, was further studied in vivo using chronic rat food intake and body weight models.
MeSH terms
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Animals
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Anti-Obesity Agents / chemical synthesis*
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Anti-Obesity Agents / chemistry
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Anti-Obesity Agents / pharmacology
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Body Weight / drug effects
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Cell Line
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Eating / drug effects
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Humans
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Oligopeptides / chemical synthesis*
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Oligopeptides / chemistry
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Oligopeptides / pharmacology
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Radioligand Assay
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Rats
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Receptor, Melanocortin, Type 4 / agonists*
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Structure-Activity Relationship
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beta-MSH / chemistry*
Substances
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Anti-Obesity Agents
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Oligopeptides
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Receptor, Melanocortin, Type 4
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beta-MSH