KISS1R Membrane Protein Introduction

Introduction of KISS1R

KISS1R is a galanin-like G-protein coupled receptor which has seven transmembrane domains, encoded by KISS1R gene. It is highly expressed in the pancreas, placenta, and spinal cord and lowly expressed in peripheral blood leukocytes, kidney, lung, fetal liver, stomach, small intestine, testes, spleen, thymus, adrenal glands and lymph nodes. Most studies indicate that KISS1R plays an essential role in the regulation of reproductive functions and puberty maturity.

Function of KISS1R Membrane Protein

KISS1R is a receptor for metastin that is a peptide encoded by the metastasis suppressor gene KISS1. KISS1R coupled to Gα_q/11 is activated by binding to its ligand, and then stimulates the activation of primary effector phospholipase C (PLC). The activated PLC further promotes the formation of inositol-(1,4,5)-trisphosphate (IP3) and diacylglycerol and activates protein kinase C (PKC) as well as extracellular signal-regulated kinases 1 and 2 (ERK1/2). The KISS1R signaling is associated with the regulation of endocrine function and reproductive maturation and function, involved in the onset of puberty, normal gonadotropin-released hormone physiology and ovulation. Besides, KISS1R signaling also regulates the tumor process through inhibiting metastases in numerous human cancers. Several studies have shown that KP/KISS1R pathway is associated with the pathological process of malignant melanomas and breast carcinomas. So, KP/KISS1R pathway can be regarded as a promising therapeutic target for cancer treatment. In addition, some findings also identify that KISS1R is involved in the regulation of lipid synthesis and obesity development.

Fig.1 Established and putative signaling pathways coupled to KISS1R. (Cvetković, 2013)

Application of KISS1R Membrane Protein in Literature

1. Wang T., et al. Kisspeptin receptor GPR54 promotes adipocyte differentiation and fat accumulation in mice. Frontiers in Physiology. 2018, 9:209. PubMed ID: 29593567
   
   

   The study indicates that GPR54 can promote lipid synthesis and obesity development possibly by activating MAP kinase pathway, thus providing a new drug target for metabolic diseases treatment.

2. Kostakis I.D., et al. KISS1 and KISS1R expression in gastric cancer. Journal of BUON. 2018, 23(1):79-84. PubMed ID: 29552764
   
   

   The authors detect the expression of KISS1 and KISS1R in both normal and cancer tissue using immunohistochemistry. Results suggest that the expression of KISS1 is decreased during carcinogenesis in gastric mucosa, with lower levels in more advanced tumors and more aggressive histological types. While KISS1R expression is not detected in cancer tissues except low levels in the normal gastric epithelium.

3. Ciaramella V., et al. Kisspeptin and cancer: molecular interaction, biological functions, and future perspectives. Frontiers in Endocrinology. 2018, 9:115. PubMed ID: 29662466
   
   

   In this review, authors highlight the latest data on the role of kisspeptin signaling in the suppression of metastasis in various cancer types and the use of KiSS/GPR54 signaling as potential novel therapeutic agents for the treatment of cancer.

4. Franssen D., et al. The kisspeptin receptor: a key G protein-coupled receptor in the control of the reproductive axis. Best Practice & Research Clinical Endocrinology & Metabolism. 2018:107-123. PubMed ID: 29678280
   
   

   KISS1R is a G protein-coupled receptor involved in regulation of pubertal maturation, gonadotropin secretion and ovulation, as well as reproductive maturation and function. In this review, authors summarize the role of KISS1R in the mediation of the reproductive axis.

5. Delmas S., et al. Altered aspects of anxiety-related behavior in kisspeptin receptor-deleted male mice. Sci Rep. 2018, 8(1):2794. PubMed ID: 29434234
   
   

   The study indicates that KISS1R signaling impacts upon anxiogenic neural circuits operative in the elevated plus maze, while gonadal steroids appear to be important for anxiety behavior observed in the open field test. The potential anxiogenic role of kisspeptin may need to be considered in the development of kisspeptin analogs for the clinic.

KISS1R Preparation Options

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Reference

1. Cvetković D, et al. (2013). Kisspeptin/KISS1R System in Breast Cancer. Journal of Cancer. 4(8), 653-61.

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