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Study · Not a test of the peptide alone · 2021

2 results

Structure reveals the activation mechanism of the MC4 receptor to initiate satiation signaling.

Israeli H, Degtjarik O, Fierro F, Chunilal V, Gill AK, Roth NJ, Botta J, Prabahar V, Peleg Y, Chan LF, Ben-Zvi D, McCormick PJ, Niv MY, Shalev-Benami M

Science (New York, N.Y.)15 Apr 2021Cited by 81 (Europe PMC)

PMID33858992 (opens in a new tab)DOI10.1126/science.abf7958 (opens in a new tab)PepBankPUB-33858992
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 study2

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

Studies that did not test the peptide alone2

In this study, Setmelanotide 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 Setmelanotide.

  1. 01LabNot a test of Setmelanotide aloneIn vitro (cell-free)Mechanism

    In lab tests of the setmelanotide-bound human MC4R complex, structural work revealed a molecular switch that initiates satiation signaling.

    In plain wordsIn lab tests, the setmelanotide-bound receptor structure revealed a molecular switch that initiates satiation signaling.

    Peptide
    Setmelanotide
    Outcome
    Not applicableMC4R activation molecular switch
    Study

    humann: not reported in source

    MC4R-Gs signaling complex
    Outcome group
    Receptor activity and mechanism · Pharmacology

    Source sentences

    Summary
    The work reveals the mechanism of MC4R activation, highlighting a molecular switch that initiates satiation signaling.
    1 context sentence
    Summary · context
    Here, we present the cryo-electron microscopy (cryo-EM) structure of the human MC4R-Gs signaling complex bound to the agonist setmelanotide, a cyclic peptide recently approved for the treatment of obesity.

    In this study, Setmelanotide 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 Setmelanotide.

  2. 02LabNot a test of Setmelanotide aloneIn vitro (cell-free)Mechanism

    In lab tests of MC4R, calcium was required for agonist efficacy in the study of the setmelanotide-bound complex.

    In plain wordsIn lab tests of MC4R, calcium was required for agonist efficacy in the study of the setmelanotide-bound complex.

    Peptide
    Setmelanotide
    Outcome
    Not applicableCalcium requirement for agonist efficacy
    Study

    humann: not reported in source

    MC4R-Gs signaling complex
    Outcome group
    Receptor activity and mechanism · Pharmacology

    Source sentences

    Summary
    In addition, our findings indicate that calcium (Ca2+) is required for agonist, but not antagonist, efficacy.
    1 context sentence
    Summary · context
    Here, we present the cryo-electron microscopy (cryo-EM) structure of the human MC4R-Gs signaling complex bound to the agonist setmelanotide, a cyclic peptide recently approved for the treatment of obesity.

    In this study, Setmelanotide 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 Setmelanotide.

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

    28 Oct 2026, 02:03 UTC

    Study results updated

  2. Version 1

    27 Oct 2026, 16:36 UTC

    First added · source update from Europe PMC

Subjects

Terms as the source lists them.

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