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Study · In vitro (cell-free) · 2023

4 results

Molecular insights into peptide agonist engagement with the PTH receptor.

Cary BP, Gerrard EJ, Belousoff MJ, Fletcher MM, Jiang Y, Russell IC, Piper SJ, Wootten D, Sexton PM

Structure (London, England : 1993)5 May 2023Cited by 17 (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 study4

1 result from studies that gave the peptide. No result from this study comes from people.

  1. 01LabIn vitro (cell-free)Activity measurement

    In laboratory assays, abaloparatide and other studied agonists showed similarities in Gαs activation measures.

    In plain wordsIn lab tests, abaloparatide and other studied agonists showed similar activation of Gαs.

    Outcome
    Not applicableGαs activation
    Study

    n: not reported in source

    PTH1R agonist complexes
    Comparator
    Other studied PTH1R agonists
    Outcome group
    Receptor activity and mechanism · Pharmacology
    Studied dose
    Dose not stated

    Source sentences

    Summary
    We found that the critical N terminus of each agonist engages the transmembrane bundle in a topologically similar fashion, reflecting similarities in measures of Gαs activation.
    1 context sentence
    Summary · context
    Here, we describe cryo-EM structures of the PTH1R in complex with fragments of the two hormones, PTH and PTH-related protein, the drug abaloparatide, as well as the engineered tool compounds, long-acting PTH (LA-PTH) and the truncated peptide, M-PTH(1-14).

Studies that did not test the peptide alone3

In this study, Abaloparatide (Tymlos) 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 Abaloparatide (Tymlos).

  1. 02LabNot a test of Abaloparatide (Tymlos) aloneIn vitro (cell-free)Mechanism

    In PTH1R structures, abaloparatide and other studied agonists engaged the transmembrane bundle with topologically similar N termini.

    In plain wordsIn lab tests, abaloparatide and other studied agonists contacted the receptor's membrane-spanning region in a similar way.

    Outcome
    Not applicableN-terminal receptor engagement
    Study

    n: not reported in source

    PTH1R agonist complexes
    Comparator
    Other studied PTH1R agonists
    Outcome group
    Receptor activity and mechanism · Pharmacology

    Source sentences

    Summary
    We found that the critical N terminus of each agonist engages the transmembrane bundle in a topologically similar fashion, reflecting similarities in measures of Gαs activation.
    1 context sentence
    Summary · context
    Here, we describe cryo-EM structures of the PTH1R in complex with fragments of the two hormones, PTH and PTH-related protein, the drug abaloparatide, as well as the engineered tool compounds, long-acting PTH (LA-PTH) and the truncated peptide, M-PTH(1-14).

    In this study, Abaloparatide (Tymlos) 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 Abaloparatide (Tymlos).

  2. 03LabNot a test of Abaloparatide (Tymlos) aloneIn vitro (cell-free)Mechanism

    In PTH1R structures, full-length agonists including abaloparatide induced subtly different extracellular domain orientations relative to the transmembrane domain.

    In plain wordsIn lab tests, full-length agonists including abaloparatide produced small differences in the receptor's outer-domain orientation.

    Outcome
    Direction not reportedExtracellular domain orientation
    Study

    n: not reported in source

    PTH1R agonist complexes
    Comparator
    Other studied PTH1R agonists
    Outcome group
    Receptor activity and mechanism · Pharmacology

    Source sentences

    Summary
    The full-length peptides induce subtly different extracellular domain (ECD) orientations relative to the transmembrane domain.
    1 context sentence
    Summary · context
    Here, we describe cryo-EM structures of the PTH1R in complex with fragments of the two hormones, PTH and PTH-related protein, the drug abaloparatide, as well as the engineered tool compounds, long-acting PTH (LA-PTH) and the truncated peptide, M-PTH(1-14).

    In this study, Abaloparatide (Tymlos) 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 Abaloparatide (Tymlos).

  3. 04LabNot a test of Abaloparatide (Tymlos) aloneIn vitro (cell-free)Mechanism

    In PTH1R complex structures, high resolution allowed identification of water molecules near peptide and G protein binding sites.

    In plain wordsIn lab tests, detailed receptor structures identified water molecules near peptide and G protein binding sites.

    Outcome
    Not applicableBinding-site water molecules
    Study

    n: not reported in source

    PTH1R agonist complexes
    Outcome group
    Receptor activity and mechanism · Pharmacology

    Source sentences

    Summary
    High resolutions enabled identification of water molecules near peptide and G protein binding sites.
    1 context sentence
    Summary · context
    Here, we describe cryo-EM structures of the PTH1R in complex with fragments of the two hormones, PTH and PTH-related protein, the drug abaloparatide, as well as the engineered tool compounds, long-acting PTH (LA-PTH) and the truncated peptide, M-PTH(1-14).

    In this study, Abaloparatide (Tymlos) 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 Abaloparatide (Tymlos).

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

    22 Oct 2026, 02:25 UTC

    Study results updated

  2. Version 1

    21 Oct 2026, 18:59 UTC

    First added · source update from Europe PMC

Subjects

Terms as the source lists them.

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