Target intelligence / Profile preview

KISS1 receptor (KISS1R)

Target
KISS1R
Molecular classification
G protein-coupled receptor, GPCR, Class A peptide-GPCR
01

Overview

The KISS1 receptor (KISS1R), also known as GPR54, is a G protein-coupled receptor that plays a central role in reproductive physiology. Activation by kisspeptins triggers the release of GnRH, leading to the secretion of gonadotropins. It is also involved in metabolic regulation and acts as a metastasis suppressor in certain cancers. Mutations in KISS1R can cause hypogonadotropic hypogonadism.

Other names
GPR54Kisspeptin receptor
02

Mechanism of action

Activation of Gq/11 proteins, leading to PLC activation and downstream signaling cascades; β-arrestin-dependent ERK activation

03

Biological functions

Regulation of reproductive physiologyGnRH releaseGonadotropin secretionMetabolic regulation
04

Disease associations

Isolated hypogonadotropic hypogonadismPuberty disordersFertility disordersMetastasis in malignant melanomasBreast carcinoma
05

Interacting drugs

TAK448

1 more in the full profile.

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