Target intelligence / Profile preview

Insulin-like peptide 3 (INSL3)

Target
INSL3
Molecular classification
Peptide hormone, Insulin/relaxin superfamily, Ligand (for G protein-coupled receptor)
01

Overview

Insulin-like peptide 3 (INSL3) is a peptide hormone of the insulin/relaxin superfamily, produced primarily by Leydig cells of the testes and, to a lesser extent, in ovarian thecal cells. It acts as the physiological ligand for the G protein-coupled receptor RXFP2, and is critical for the initial phase of testicular descent in male fetuses by promoting gubernacular development. In adults, INSL3 continues to serve as a biomarker for Leydig cell differentiation and function, and its signaling is also implicated in ovarian follicle development and maintenance of normal bone characteristics. Mutations in INSL3 or its receptor RXFP2 are linked to disorders such as cryptorchidism and reduced bone density. INSL3 is under investigation as a diagnostic biomarker and as a potential therapeutic target, but no approved drugs currently modulate INSL3 signaling[1][2][4][5].

Other names
Insulin-like 3RLFRLNLLey-I-LLeydig insulin-like peptideRelaxin-like factorprepro-INSL3relaxin-like factor Bleydig insulin-like hormoneinsulin-like 3 B chaininsulin-like 3 A chain
02

Mechanism of action

Binds and activates Relaxin family peptide receptor 2 (RXFP2), a G protein-coupled receptor. Triggers cAMP signaling cascade in target cells

03

Biological functions

Hormonal signalingRegulation of testicular descentGonadal developmentRegulation of reproductive functions (male and female)Bone and skeletal muscle physiology
04

Disease associations

Cryptorchidism (undescended testes)Disorders of sexual developmentReduced bone density (osteopenia, osteoporosis in association with RXFP2 mutations)Potential biomarker for Leydig cell function and anti-androgen exposure
05

Safety considerations

Insufficient clinical experience with INSL3-targeted therapies; potential effects on reproductive and skeletal development if manipulatedAltered INSL3/RXFP2 signaling could disrupt testicular descent, fertility, or bone development
06

Interacting drugs

None currently approved or established; peptide analogs and antagonists under research
07

Biomarkers

INSL3 serum levels as biomarker for Leydig cell function and fetal testicular healthReduced INSL3 may be a biomarker for exposure to endocrine-disrupting chemicals

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