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Published on: September 27, 2015
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RXFP1, the relaxin receptor: Lost and found in translation.
Mark Lal1, Sean Eddy2, Anna Walentinsson3
1Bioscience, Cardiovascular, Renal and Metabolism, R&D Biopharmaceuticals, AstraZeneca, Gothenburg, Sweden.
Drug Discovery Today
|September 25, 2025
Summary
Relaxin is a hormone with cardiovascular and anti-fibrotic benefits. Understanding its receptor, RXFP1, and its varied expression across species is key to developing new therapies.
Area of Science:
- Endocrinology
- Cardiovascular Research
- Pharmacology
Background:
- Relaxin is a hormone with significant cardiovascular and anti-fibrotic properties.
- Species diversity in relaxin's effects and sources is well-established.
- A gap exists in understanding the relaxin family peptide receptor 1 (RXFP1).
Purpose of the Study:
- To review the tissue expression of RXFP1 across species.
- To highlight the translational gap in RXFP1 understanding.
- To emphasize the importance of RXFP1 target pharmacology for clinical applications.
Main Methods:
- Literature review focusing on RXFP1 tissue expression.
- Comparative analysis of RXFP1 expression in rodents versus humans.
- Discussion of RXFP1 pharmacology.
Main Results:
- Striking contrasts in RXFP1 tissue expression between rodents and humans were identified.
- The translational relevance of rodent models for human RXFP1 function is questioned.
- RXFP1 pharmacology presents a critical area for future research.
Conclusions:
- Understanding species-specific RXFP1 expression is crucial for therapeutic development.
- Targeting RXFP1 pharmacology is essential for clinical success.
- Further research into RXFP1 is needed to leverage relaxin's therapeutic potential.
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