Target intelligence / Profile preview

FSH receptor and LH receptor (FSHR and LHR/LHCGR)

Target
FSHR and LHR/LHCGR
Molecular classification
G protein-coupled receptor (GPCR), Glycoprotein hormone receptor family, Transmembrane receptor
01

Overview

The Follicle-stimulating hormone receptor (FSHR) and Luteinizing hormone/choriogonadotropin receptor (LHCGR or LHR) are structurally related glycoprotein hormone receptors, both belonging to the G protein-coupled receptor superfamily and predominantly expressed in the gonads. FSHR is essential for mediating the actions of FSH in regulating ovarian follicle maturation, granulosa cell proliferation, and spermatogenesis via Sertoli cells. LHCGR recognizes both LH and hCG to mediate ovulation, luteinization, and androgen production by Leydig cells. Both receptors transduce hormone binding signals primarily through the Gs/cAMP/PKA pathway but can activate additional cellular signaling cascades and sometimes form functional heteromers with each other, which can modulate their signaling output. Their critical roles make them central targets for drug development in reproductive medicine, especially in the treatment of infertility and assisted reproductive technologies. Note: The query provided both receptors as a single entity; however, they are distinct molecular targets that are closely related, frequently co-expressed, and sometimes physically interact through heteromerization, which can modulate signaling properties relevant to ovarian physiology.

Other names
FSHRFSH receptorfollicle-stimulating hormone receptorLHCGRLH receptorluteinizing hormone receptorchoriogonadotropin receptorLHR
02

Mechanism of action

Agonists (hormones or drugs) bind the extracellular domain, inducing conformational changes that activate the intracellular G protein-dependent pathways (mainly Gs/cAMP/PKA, but also Gq/PLC and β-arrestin pathways) Allosteric modulators can enhance or alter signaling

03

Biological functions

Signal transductionGonadal development and functionRegulation of gametogenesis (oogenesis/spermatogenesis)Regulation of steroidogenesis (sex steroid hormone production)Cell proliferationCell differentiation
04

Disease associations

Infertility (male and female)Ovarian dysfunctionPolycystic ovary syndrome (PCOS)Gonadal tumorsSome genetic and developmental disorders impacting sexual differentiationOvarian hyperstimulation syndrome (OHSS, iatrogenic/therapeutic risk)
05

Safety considerations

Ovarian hyperstimulation syndrome (especially with exogenous FSH/LH or hCG use)Multiple pregnancy (in fertility treatments)Tumorigenesis risk (rare, with chronic overstimulation)Potential cardiovascular or thromboembolic events with high-dose use in susceptible patients
06

Interacting drugs

Recombinant and urinary FSH formulations (e.g., follitropin alfa)

4 more in the full profile.

07

Biomarkers

Serum FSH and LH levels (for patient selection/monitoring in fertility treatments)Receptor expression in granulosa and Sertoli cells (tissue diagnostic)Genetic variations in FSHR/LHCGR for predicting ovarian response

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