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Study · Not a test of the peptide alone · 2004

4 results

A predictive pharmacophore model of human melanocortin-4 receptor as derived from the solution structures of cyclic peptides.

Sun H, Greeley DN, Chu XJ, Cheung A, Danho W, Swistok J, Wang Y, Zhao C, Chen L, Fry DC

Bioorganic & medicinal chemistry1 May 2004Cited by 17 (Europe PMC)

PMID15110848 (opens in a new tab)DOI10.1016/j.bmc.2004.03.017 (opens in a new tab)PepBankPUB-15110848
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 study4

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

Studies that did not test the peptide alone4

In this study, Melanotan II 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 II.

  1. 01LabNot a test of Melanotan II aloneIn vitro (cell-free)Other

    In NMR solution structures, a beta-turn structure was conserved among all the cyclic MT-II-based peptides studied.

    In plain wordsIn lab structure tests, all the cyclic MT-II-based peptides studied kept the same turn shape.

    Peptide
    Melanotan II
    Outcome
    Not applicableConserved beta-turn structure across cyclic MT-II-based peptides
    Study

    n: not reported in source

    Cyclic peptide analogs based on MT-II and the human MC4 receptor
    Outcome group
    Receptor activity and mechanism · Pharmacology

    Source sentences

    Summary
    A beta-turn structure was conserved among all of the cyclic peptides studied.
    1 context sentence
    Summary · context
    Using nuclear magnetic resonance (NMR) spectroscopy, we have determined the solution structures for a series of potent agonists for the human melanocortin-4 receptor (hMC4R), based on the cyclic peptide MT-II [Ac-Nle-cyclo-(Asp-Lys) (Asp-His-(D)Phe-Arg-Trp-Lys)-NH2].

    In this study, Melanotan II 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 II.

  2. 02LabNot a test of Melanotan II aloneOther designActivity measurement

    In lab tests, the most selective and rigid MT-II-based analog was a full agonist of the human melanocortin-4 receptor with an EC50 of 11 nM.

    In plain wordsIn lab tests, the most selective and rigid MT-II-based analog fully activated the human melanocortin-4 receptor at a low concentration.

    Peptide
    Melanotan II
    Outcome
    Not applicablehMC4R agonist potency of the most selective rigid analog (EC50)
    Study

    n: not reported in source

    Cyclic peptide analogs based on MT-II and the human MC4 receptor
    Outcome group
    Receptor activity and mechanism · Pharmacology

    Measurements

    EC50
    11 nM
    hMC4R

    Source sentences

    Summary
    was found to be a full agonist of hMC4R with an EC50 of 11nM against hMC4R
    1 context sentence
    Summary · context
    Using nuclear magnetic resonance (NMR) spectroscopy, we have determined the solution structures for a series of potent agonists for the human melanocortin-4 receptor (hMC4R), based on the cyclic peptide MT-II [Ac-Nle-cyclo-(Asp-Lys) (Asp-His-(D)Phe-Arg-Trp-Lys)-NH2].

    In this study, Melanotan II 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 II.

  3. 03LabNot a test of Melanotan II aloneOther designActivity measurement

    In lab tests, the most selective MT-II-based analog showed 65-fold selectivity for the human melanocortin-4 receptor over hMC1R.

    In plain wordsIn lab tests, the most selective MT-II-based analog acted 65-fold more strongly on the melanocortin-4 receptor than on the melanocortin-1 receptor.

    Peptide
    Melanotan II
    Outcome
    Not applicableSelectivity of the most selective analog for hMC4R over hMC1R
    Study

    n: not reported in source

    Cyclic peptide analogs based on MT-II and the human MC4 receptor
    Outcome group
    Receptor activity and mechanism · Pharmacology

    Measurements

    Selectivity
    65-fold
    hMC4R versus hMC1R

    Source sentences

    Summary
    and to exhibit 65-fold selectivity against hMC1R.
    1 context sentence
    Summary · context
    Using nuclear magnetic resonance (NMR) spectroscopy, we have determined the solution structures for a series of potent agonists for the human melanocortin-4 receptor (hMC4R), based on the cyclic peptide MT-II [Ac-Nle-cyclo-(Asp-Lys) (Asp-His-(D)Phe-Arg-Trp-Lys)-NH2].

    In this study, Melanotan II 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 II.

  4. 04Computer modelNot a test of Melanotan II aloneIn silicoOther

    In a virtual screen of a library of 1000 drug-like compounds, the pharmacophore model identified the known potent ligands that had been added to the library.

    In plain wordsIn a computer screen, the model picked out the known potent ligands from among 1000 compounds.

    Peptide
    Melanotan II
    Outcome
    Not applicableValidation of the pharmacophore model by virtual screen
    Study

    n: not reported in source

    Cyclic peptide analogs based on MT-II and the human MC4 receptor
    Outcome group
    Receptor activity and mechanism · Pharmacology

    Source sentences

    Summary
    The utility of the model was validated by its ability to identify the known ligands from among this large library.
    2 context sentences
    Summary · context
    This model was used to perform a virtual screen using a library of 1000 drug-like compounds, to which a small set of known potent ligands had been intentionally added.
    Summary · context
    Using nuclear magnetic resonance (NMR) spectroscopy, we have determined the solution structures for a series of potent agonists for the human melanocortin-4 receptor (hMC4R), based on the cyclic peptide MT-II [Ac-Nle-cyclo-(Asp-Lys) (Asp-His-(D)Phe-Arg-Trp-Lys)-NH2].

    In this study, Melanotan II 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 II.

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

    10 Oct 2026, 09:43 UTC

    Study results updated

  2. Version 1

    9 Oct 2026, 03:04 UTC

    First added · source update from Europe PMC

Subjects

Terms as the source lists them.

Publication types

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