Kisspeptin Receptor Antibodies

KISS1R (also known as GPR54 or the kisspeptin receptor) is a G protein–coupled receptor that binds kisspeptins, a family of peptides derived from the KISS1 gene. Pharmacologically, KISS1R primarily signals through Gq/11 proteins, activating phospholipase C, which increases intracellular Ca²⁺ and activates protein kinase C, leading to robust stimulation of gonadotropin-releasing hormone (GnRH) neurons. KISS1R is highly expressed in the hypothalamus, especially in GnRH neurons, but it is also found in the pituitary, gonads, placenta, and several peripheral tissues, indicating additional regulatory roles. Functionally, the KISS1–KISS1R pathway is indispensable for the onset of puberty and maintenance of reproductive function. Genetic inactivation of KISS1R results in hypogonadotropic hypogonadism, while activating mutations can cause precocious puberty, highlighting its pivotal role in reproductive timing. Emerging evidence also links KISS1R signaling to metabolic control, placental development, and tumor metastasis suppression. Overall, KISS1R serves as a key neuroendocrine receptor integrating reproductive, metabolic, and developmental signals essential for fertility and physiological homeostasis. For more information on KISS1R receptor pharmacology please refer to the IUPHAR database.