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Study · Not a test of the peptide alone · 2021

3 results

Structural insights into ligand recognition and activation of the melanocortin-4 receptor.

Zhang H, Chen LN, Yang D, Mao C, Shen Q, Feng W, Shen DD, Dai A, Xie S, Zhou Y, Qin J, Sun JP and 5 more

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Scharf DH, Hou T, Zhou T, Wang MW, Zhang Y

Cell research25 Aug 2021Cited by 59 (Europe PMC)

PMID34433901 (opens in a new tab)PMCIDPMC8563965 (opens in a new tab)DOI10.1038/s41422-021-00552-3 (opens in a new tab)PepBankPUB-34433901
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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, the peptide 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 the peptide.

  1. 01LabNot a test of Bremelanotide (PT-141) aloneIn vitro (cell-free)Mechanism

    A high-resolution structure of full-length MC4R in complex with Gs protein and bremelanotide, with pharmacological studies, showed a conserved binding mode of peptidic agonists.

    In plain wordsIn lab tests, the structure of bremelanotide bound to its receptor showed a binding mode shared with other peptide agonists.

    Peptide
    Bremelanotide (PT-141)
    Outcome
    Not applicableStructure of MC4R-Gs complex bound to bremelanotide
    Study

    n: not reported in source

    Outcome group
    Receptor activity and mechanism · Pharmacology

    Source sentences

    Summary
    Together with pharmacological studies, our results reveal the conserved binding mode of peptidic agonists, the distinctive molecular details of small-molecule agonist recognition underlying receptor subtype selectivity, and a distinct activation mechanism for MC4R, thereby offering new insights into G protein coupling.
    1 context sentence
    Summary · context
    Here, we report four high-resolution structures of full-length MC4R in complex with the heterotrimeric Gs protein stimulated by the endogenous peptide ligand α-MSH, FDA-approved drugs afamelanotide (Scenesse™) and bremelanotide (Vyleesi™), and a selective small-molecule ligand THIQ, respectively.

    In this study, Bremelanotide (PT-141) 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 Bremelanotide (PT-141).

  2. 02LabNot a test of Melanotan I (afamelanotide) aloneIn vitro (cell-free)Mechanism

    Four high-resolution structures of full-length MC4R in complex with the Gs protein were reported, each stimulated by one ligand: alpha-MSH, afamelanotide, bremelanotide or THIQ.

    In plain wordsIn lab tests, researchers solved four detailed structures of the MC4R receptor bound to different ligands, including afamelanotide.

    Peptide
    Melanotan I (afamelanotide)
    Outcome
    Not applicableStructure of MC4R-Gs complex with afamelanotide
    Study

    n: not reported in source

    full-length MC4R in complex with heterotrimeric Gs protein
    Outcome group
    Receptor activity and mechanism · Pharmacology

    Source sentences

    Summary
    Here, we report four high-resolution structures of full-length MC4R in complex with the heterotrimeric Gs protein stimulated by the endogenous peptide ligand α-MSH, FDA-approved drugs afamelanotide (Scenesse™) and bremelanotide (Vyleesi™), and a selective small-molecule ligand THIQ, respectively.

    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 (cell-free)Mechanism

    The structures, with pharmacological studies, revealed a conserved binding mode of peptidic agonists at MC4R, shared across the peptide ligands.

    In plain wordsIn lab tests, peptide drugs including afamelanotide bind MC4R in a similar way.

    Peptide
    Melanotan I (afamelanotide)
    Outcome
    Not applicableConserved binding mode of peptidic agonists at MC4R
    Study

    n: not reported in source

    full-length MC4R in complex with heterotrimeric Gs protein
    Outcome group
    Receptor activity and mechanism · Pharmacology

    Source sentences

    Summary
    our results reveal the conserved binding mode of peptidic agonists, the distinctive molecular details of small-molecule agonist recognition underlying receptor subtype selectivity, and a distinct activation mechanism for MC4R, thereby offering new insights into G protein coupling
    1 context sentence
    Summary · context
    Here, we report four high-resolution structures of full-length MC4R in complex with the heterotrimeric Gs protein stimulated by the endogenous peptide ligand α-MSH, FDA-approved drugs afamelanotide (Scenesse™) and bremelanotide (Vyleesi™), and a selective small-molecule ligand THIQ, respectively.

    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. Versions 4 to 18Current

    28 Oct 2026, 02:02 UTC

    The same notice was added 15 times, first on 13 Oct 2026, 21:44 UTC. The status did not change between them.

    Study results updated

  2. Version 3

    13 Oct 2026, 16:31 UTC

    Study data updated · source update from Europe PMC

  3. Version 2

    9 Oct 2026, 18:17 UTC

    Study results updated

  4. Version 1

    9 Oct 2026, 03:04 UTC

    First added · source update from Europe PMC

Subjects

Terms as the source lists them.

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