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Study · Not a test of the peptide alone · 2000

3 results

Molecular determinants of ligand binding to the human melanocortin-4 receptor.

Yang YK, Fong TM, Dickinson CJ, Mao C, Li JY, Tota MR, Mosley R, Van Der Ploeg LH, Gantz I

Biochemistry1 Dec 2000Cited by 142 (Europe PMC)

PMID11101306 (opens in a new tab)DOI10.1021/bi001684q (opens in a new tab)PepBankPUB-11101306
Publisher pagePubMedAsk about this study
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Summary

The text of this summary is not shown here, because the article license does not allow reuse. Read it at the source (opens in a new tab)

Text rights: Publisher copyright. Results still quote short attributed sentences.

Results from this study3

No result from this study comes from a test of the peptide.

Studies that did not test the peptide alone3

In this study, Melanotan I (afamelanotide) was a lab tool or a carrier, part of a mix, or the subject of a lab method. These results are not evidence about taking Melanotan I (afamelanotide).

  1. 01LabNot a test of Melanotan I (afamelanotide) aloneIn vitro (cells)Mechanism

    In structure-activity studies at the human melanocortin-4 receptor, D-Phe7-Arg8-Trp9 was the minimal NDP-MSH fragment with full agonist efficacy.

    In plain wordsIn lab tests, a short three-amino-acid piece of NDP-MSH was enough to fully activate the human MC4 receptor.

    Peptide
    Melanotan I (afamelanotide)
    Outcome
    Not applicableMinimal NDP-MSH fragment with full agonist efficacy at hMC4R
    Study

    n: not reported in source

    Outcome group
    Receptor activity and mechanism · Pharmacology

    Source sentences

    Summary
    Structure-activity studies of [Nle(4), D-Phe(7)]-alpha-melanocyte stimulating hormone (NDP-MSH) identified D-Phe7-Arg8-Trp9 as the minimal NDP-MSH fragment that possesses full agonist efficacy at the hMC4R.
    1 context sentence
    Summary · context
    To elucidate the molecular basis for the interaction of ligands with the human melanocortin-4 receptor (hMC4R), agonist structure-activity studies and receptor point mutagenesis were performed.

    In this study, Melanotan I (afamelanotide) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Melanotan I (afamelanotide).

  2. 02LabNot a test of Melanotan I (afamelanotide) aloneIn vitro (cells)Mechanism

    In cells expressing mutant hMC4R, mutation of TM3 residues D122 and D126 and TM6 residues F261 and H264 decreased NDP-MSH binding affinity 5-fold or greater.

    In plain wordsIn lab tests, changing four sites in the human MC4 receptor made NDP-MSH bind at least five times less strongly.

    Peptide
    Melanotan I (afamelanotide)
    Outcome
    DecreaseNDP-MSH binding affinity at hMC4R mutants
    Study

    n: not reported in source

    Outcome group
    Receptor activity and mechanism · Pharmacology

    Measurements

    Binding affinity decrease
    ≥ 5 fold
    D122, D126, F261 and H264 mutants

    Source sentences

    Summary
    Mutation of TM3 residues D122 and D126 and TM6 residues F261 and H264 decreased the binding affinity of NDP-MSH 5-fold or greater, thereby identifying these receptor residues as sites potentially involved in the sought after ligand-receptor interactions.
    1 context sentence
    Summary · context
    To elucidate the molecular basis for the interaction of ligands with the human melanocortin-4 receptor (hMC4R), agonist structure-activity studies and receptor point mutagenesis were performed.

    In this study, Melanotan I (afamelanotide) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Melanotan I (afamelanotide).

  3. 03LabNot a test of Melanotan I (afamelanotide) aloneIn vitro (cells)Mechanism

    In studies of substituted NDP-MSH peptides at receptor mutants, evidence indicated that Arg8 of the core melanocortin sequence interacts with hMC4R TM3 residue D122.

    In plain wordsIn lab tests, one amino acid in NDP-MSH appeared to contact a specific site on the human MC4 receptor.

    Peptide
    Melanotan I (afamelanotide)
    Outcome
    Not applicableArg8 interaction with hMC4R TM3 residue D122
    Study

    n: not reported in source

    Outcome group
    Receptor activity and mechanism · Pharmacology

    Source sentences

    Summary
    By examination of the binding affinities and potencies of substituted NDP-MSH peptides at receptor mutants, evidence was found that core melanocortin peptide residue Arg8 interacts at a molecular level with hMC4R TM3 residue D122.
    1 context sentence
    Summary · context
    To elucidate the molecular basis for the interaction of ligands with the human melanocortin-4 receptor (hMC4R), agonist structure-activity studies and receptor point mutagenesis were performed.

    In this study, Melanotan I (afamelanotide) was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Melanotan I (afamelanotide).

AI wrote and checked these results. AI can make mistakes, so check important results against the source.

Version history

PepBank keeps every version of the data on this study. Status changes from Retraction Watch, Europe PMC and Crossref are listed with their source.

  1. Version 2Current

    13 Oct 2026, 21:44 UTC

    Study results updated

  2. Version 1

    13 Oct 2026, 16:31 UTC

    First added · source update from Europe PMC

Subjects

Terms as the source lists them.

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