Target intelligence / Profile preview

Relaxin 1 (RLN1)

Target
RLN1
Molecular classification
Hormone, Secreted protein, Endocrine/autocrine hormone, Insulin-like peptide
01

Overview

Relaxin 1 (RLN1) is an endocrine hormone of the insulin superfamily synthesized as a preprohormone that is processed to a 6 kDa dimer comprised of an A and a B chain linked by disulfide bonds[2][5]. Its canonical action is via activation of the relaxin family peptide receptor 1 (RXFP1), a G protein-coupled receptor[1][2]. RLN1 is predominantly expressed in reproductive tissues such as the prostate, decidua, placenta, and endometrium, with lower levels in the myocardium[2][5]. It plays a key role in reproductive biology, including preparing the birth canal (cervical ripening, pubic symphysis elongation), suppressing uterine contractions, and modulating sperm motility[5][6]. It is also implicated in connective tissue remodeling, blood pressure regulation, heart rate control, and neuroendocrine hormone release[3][5]. In pathology, RLN1 is associated with reproductive disorders, prostate and thyroid neoplasia, germ cell tumors, spermatogenic failure, and may contribute to changes in lung tissue function[3][5]. Therapeutically, RLN1 and its pathway have drawn interest for potential application in heart failure and tissue remodeling, though clinical development is currently experimental with few direct drugs[1][2][4]. The safety profile for interventions targeting RLN1 remains to be fully elucidated, though risks may include effects on connective tissue and hormone-sensitive cancers[3][5].

Other names
Prorelaxin H1Relaxin B chainRelaxin A chainH1 relaxinH1H1RLXRLXH1bA12D24.3.1bA12D24.3.2preprorelaxin H1prorelaxin H1
02

Mechanism of action

Activates relaxin family peptide receptor 1 (RXFP1), a G protein-coupled receptor, increases cAMP signaling, activates ERK1/2, MAPK, tyrosine kinases, and nitric oxide pathways, drives tissue remodeling and relaxation responses[1][2][4]

03

Biological functions

Reproductive system modulation (cervical ripening, elongation of the pubic symphysis, inhibition of uterine contraction)Regulation of connective tissue remodelingRegulation of blood pressureModulation of heart rateEnhancement of sperm motilityRegulation of oxytocin and vasopressin releasePotential regulation of cell proliferation and differentiation
04

Disease associations

Reproductive disordersMale fertility and spermatogenic failureCancer (prostate cancer, medullary thyroid carcinoma, germ cell tumors)Cardiovascular diseaseLung function modulationOther
05

Safety considerations

Possible effects on connective tissue remodeling and cardiovascular systempotential implications in hormone-dependent cancersexperimental and safety profile for therapeutics targeting RLN1/RXFP1 axis not fully established
06

Interacting drugs

relaxin analogs and mimetics (experimental therapeutics)

1 more in the full profile.

07

Biomarkers

Potentially relevant as a marker for prostate and thyroid neoplasmsearly endocrine changes in some tumorscertain reproductive states

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