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Design and Synthesis of a Structurally Stabilized B‑Chain Antagonist Targeting Relaxin Family Peptide Receptor 3

Hongkang Wu¹, Praveen Praveen¹, Isabelle Riches¹

¹The Florey, The University of Melbourne, Parkville, Victoria 3052, Australia.

ACS Medicinal Chemistry Letters

|November 19, 2025

Summary

Researchers developed a novel peptide antagonist, H3B10-22R-(13/17αF), targeting the relaxin-3 peptide receptor (RXFP3). This potent and stable molecule shows promise for treating feeding disorders like obesity.

Keywords:

Antagonist Peptides Peptides and Proteins RXFP3 Relaxin-3

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Area of Science:

Neuroendocrinology
Peptide Chemistry
Pharmacology

Background:

Relaxin-3 is a neuropeptide regulating motivated behaviors, including feeding.
Its complex structure hinders therapeutic development for metabolic and neuropsychiatric disorders.
Simplified B-chain analogues are being explored as potential drug candidates.

Purpose of the Study:

To develop and characterize a novel, simplified peptide antagonist for the relaxin-3 receptor (RXFP3).
To assess the antagonist's potency, selectivity, stability, and in vivo efficacy in a feeding behavior model.

Main Methods:

Design and synthesis of a stapled, single-chain peptide antagonist (H3B10-22R-(13/17αF)).
Biochemical assays to determine RXFP3 binding affinity, selectivity, and antagonist potency.
Assessment of serum stability and in vivo efficacy in a rat feeding model.

Main Results:

H3B10-22R-(13/17αF) demonstrated high RXFP3 selectivity and binding affinity.
The stapled peptide exhibited enhanced helicity and antagonist potency compared to linear analogues.
It showed a 12-fold improvement in serum stability and significantly inhibited RXFP3 agonist-induced feeding in rats.

Conclusions:

H3B10-22R-(13/17αF) is a potent, stable, and drug-like RXFP3 antagonist.
This novel peptide represents a promising therapeutic candidate for feeding disorders, including obesity.
Further development is warranted to explore its clinical potential.