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Study · In vitro (cell-free) · 2023

1 result

A Lipidated Single-B-Chain Derivative of Relaxin Exhibits Improved In Vitro Serum Stability without Altering Activity.

Praveen P, Wang C, Handley TNG, Wu H, Samuel CS, Bathgate RAD, Hossain MA

International journal of molecular sciences1 Apr 2023Cited by 8 (Europe PMC)

PMID37047588 (opens in a new tab)PMCIDPMC10094921 (opens in a new tab)DOI10.3390/ijms24076616 (opens in a new tab)PepBankPUB-37047588
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Summary

Human relaxin-2 (H2 relaxin) is therapeutically very important due to its strong anti-fibrotic, vasodilatory, and cardioprotective effects. Therefore, relaxin's receptor, relaxin family peptide receptor 1 (RXFP1), is a potential target for the treatment of fibrosis and related disorders, including heart failure. H2 relaxin has a complex two-chain structure (A and B) and three disulfide bridges. Our laboratory has recently developed B7-33 peptide, a single-chain agonist based on the B-chain of H2 relaxin. However, the peptide B7-33 has a short circulation time in vitro in serum (t1/2 = ~6 min). In this study, we report structure-activity relationship studies on B7-33 utilizing different fatty-acid conjugations at different positions. We have shown that by fatty-acid conjugation with an appropriate spacer length, the in vitro half-life of B7-33 can be increased from 6 min to 60 min. In the future, the lead lipidated molecule will be studied in animal models to measure its PK/PD properties, which will lead to their pre-clinical applications.
CC BYText from Europe PMC. Highlighted sentences are the source of results.

Results from this study1

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

  1. 01LabIn vitro (cell-free)Pharmacokinetics

    In serum laboratory tests, native B7‑33 had a half-life of 6 minutes in the derivative comparison.

    In plain wordsIn lab tests, native B7‑33 had a serum half-life of 6 minutes.

    Peptide
    B7-33 (single-chain relaxin-2 analog)
    Outcome
    Not applicableSerum half-life
    Study

    n: not reported in source

    Serum incubation in vitro
    Outcome group
    Pharmacokinetics · Pharmacology
    Studied dose
    Dose not stated

    Measurements

    Half-life
    6 min
    native B7-33 comparator

    Source sentences

    Summary
    We have shown that by fatty-acid conjugation with an appropriate spacer length, the in vitro half-life of B7-33 can be increased from 6 min to 60 min.

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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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