Target intelligence / Profile preview

Gonadotropins and their receptors (Gn/GnR)

Target
Gn/GnR
Molecular classification
G protein-coupled receptor, Glycoprotein hormone family, Cystine knot family, Receptor
01

Overview

Gonadotropins, including follicle-stimulating hormone (FSH), luteinizing hormone (LH), and human chorionic gonadotropin (hCG), are a family of heterodimeric glycoprotein hormones that play a fundamental role in the regulation of vertebrate reproduction [8, 14]. These hormones exert their biological effects by binding to specific G protein-coupled receptors (GPCRs): the follicle-stimulating hormone receptor (FSHR) and the luteinizing hormone/choriogonadotropin receptor (LHCGR) [1, 9]. In the ovaries, these interactions stimulate folliculogenesis, ovulation, and the production of estrogen and progesterone, while in the testes, they regulate spermatogenesis and testosterone synthesis [2, 10]. Clinical applications of gonadotropins and their analogs are extensive, primarily focusing on the treatment of infertility through ovulation induction and assisted reproductive technologies [7, 12]. Additionally, the gonadotropin signaling axis is a target for managing conditions such as polycystic ovary syndrome (PCOS), hypogonadism, and certain hormone-sensitive malignancies like prostate and ovarian cancer [4, 16]. Safety considerations in therapeutic use include the risk of ovarian hyperstimulation syndrome (OHSS) and multiple gestations [14, 17].

Other names
Glycoprotein hormones and their receptorsGPHFollitropinLutropinChoriogonadotropinFSHRLHRLHCGRGonadotropin receptors
02

Mechanism of action

Agonism of the follicle-stimulating hormone receptor (FSHR) and the luteinizing hormone/choriogonadotropin receptor (LHCGR) to stimulate gametogenesis and steroidogenesis; modulation of the hypothalamic-pituitary-gonadal axis via GnRH analogs to indirectly regulate gonadotropin levels [7, 16].

03

Biological functions

Signal transductionReproductionGametogenesisSteroidogenesisCell proliferationCell differentiation
04

Disease associations

InfertilityPolycystic ovary syndrome (PCOS)HypogonadismOvarian cancerProstate cancerPrecocious pubertyEndometriosisOvarian hyperstimulation syndrome (OHSS)
05

Safety considerations

Ovarian hyperstimulation syndrome (OHSS)Multiple pregnancyEctopic pregnancyThromboembolismInjection site reactions
06

Interacting drugs

Follitropin alfa

7 more in the full profile.

07

Biomarkers

Follicle-stimulating hormone (FSH)Luteinizing hormone (LH)Human chorionic gonadotropin (hCG)EstradiolProgesteroneAnti-Müllerian hormone (AMH)Inhibin B

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