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Study · Not a test of the peptide alone · 2007

3 results

Squalene-derived flexible linkers for bioactive peptides.

Jagadish B, Sankaranarayanan R, Xu L, Richards R, Vagner J, Hruby VJ, Gillies RJ, Mash EA

Bioorganic & medicinal chemistry letters6 Apr 2007Cited by 18 (Europe PMC)

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)Activity measurement

    In vitro, most linker-ligand constructs of NDP-alpha-MSH or MSH(4) bound the human melanocortin 4 receptor as well as the parental ligand.

    In plain wordsIn lab tests, most linked versions of the peptide bound the human MC4 receptor as well as the single peptide.

    Outcome
    No significant changeBinding affinity of linker-ligand constructs to hMC4R
    Study

    humann: not reported in source

    Comparator
    Parental ligand
    Outcome group
    Receptor activity and mechanism · Pharmacology

    Source sentences

    Summary
    In vitro biological evaluations showed that the binding affinity to the human melanocortin 4 receptor was not diminished for most linker-ligand combinations relative to the corresponding parental ligand.
    1 context sentence
    Summary · context
    A regiochemical and stereochemical mixture of flexible linkers bearing terminal azide functionality was synthesized in two steps from squalene and was used to connect two high affinity NDP-alpha-MSH ligands or two low affinity MSH(4) ligands.

    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)Activity measurement

    In vitro, dimeric constructs of the low affinity ligand MSH(4) showed statistical and cooperative binding effects.

    In plain wordsIn lab tests, linked pairs of the weak MSH(4) ligand showed cooperative binding effects.

    Outcome
    IncreaseCooperative binding of MSH(4) dimers
    Study

    humann: not reported in source

    Outcome group
    Receptor activity and mechanism · Pharmacology

    Source sentences

    Summary
    Statistical and cooperative binding effects were observed for dimeric constructs containing the low affinity ligand MSH(4), but not for dimeric NDP-alpha-MSH constructs, presumably due to slow off rates for this high affinity ligand.
    1 context sentence
    Summary · context
    A regiochemical and stereochemical mixture of flexible linkers bearing terminal azide functionality was synthesized in two steps from squalene and was used to connect two high affinity NDP-alpha-MSH ligands or two low affinity MSH(4) ligands.

    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)Activity measurement

    In vitro, dimeric NDP-alpha-MSH constructs showed no statistical or cooperative binding effects, probably because of slow off rates.

    In plain wordsIn lab tests, linked pairs of the strong NDP-alpha-MSH ligand showed no cooperative binding effects.

    Outcome
    No significant changeCooperative binding of NDP-alpha-MSH dimers
    Study

    humann: not reported in source

    Outcome group
    Receptor activity and mechanism · Pharmacology

    Source sentences

    Summary
    Statistical and cooperative binding effects were observed for dimeric constructs containing the low affinity ligand MSH(4), but not for dimeric NDP-alpha-MSH constructs, presumably due to slow off rates for this high affinity ligand.
    1 context sentence
    Summary · context
    A regiochemical and stereochemical mixture of flexible linkers bearing terminal azide functionality was synthesized in two steps from squalene and was used to connect two high affinity NDP-alpha-MSH ligands or two low affinity MSH(4) ligands.

    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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