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KiSS1-derived Peptide GPCR Assays

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Background of KiSS1-derived Peptide Receptors

KiSS1-derived peptide receptors, also known as GPR54 or kisspeptin receptors, is a G protein-coupled receptors (GPCR) binding to the peptide hormone kisspeptin. The human kisspeptin receptor gene is localized on chromosome 19p13.3. The KiSS1/KiSS1R system plays an important role in the regulation of puberty, gonadotropin secretion, as well as the metabolic and environmental modulation of fertility. The KiSS1-derived peptide receptor has served as an essential GPCR for the normal maturation and function of the reproductive axis.

Kiss1R cellular signaling pathways.Fig.1. Kiss1R cellular signaling pathways. (Franssen, 2018)

Distribution and Function of KiSS1-derived Peptide Receptors

High concentrations of kisspeptin receptors can be detected in the pancreas, placenta, and brain, whereas kisspeptin receptors are expressed at lower levels in the small intestine, kidney, lung, liver, and heart. Studies have shown that the kisspeptin receptor plays an important role in the neuroendocrine control of the gonadotrophin axis and is associated with inhibiting metastasis.

Mechanisms of KiSS1-derived Peptide Receptors

Receptor Gene Mechanism Agonists Antagonists
Kisspeptin receptor KISS1R
  • Kisspeptin receptor stimulating phospholipase C and resulting in Ca2+ mobilization.
  • Kisspeptin receptor signals through β-arrestin-1 and -2 to stimulate phosphorylation of ERK1/2.
  • Kisspeptin
  • Kisspeptin-10
  • TAK-683
  • MVT-602
  • Kisspeptin-234

Assay List of KiSS1-derived Peptide Receptor

Creative Biolabs can provide a range of assays of KiSS1-derived peptide receptor. You can choose the assay in the list or contact us for more information:

KISS1R
Assay No. Assay Name Host Cell Assay Type Datasheet
Calcium Flux Assay
S01YF-1122-KX555 Magic™ Rat KISS1R In Vitro Calcium Flux Assay CHO-K1-Gα16 Calcium Flux Assay
Radioligand Binding Assay
S01YF-1122-KX554 Magic™ Human KISS1R In Vitro Radioligand Binding Assay CHO-K1 Radioligand Binding Assay

Published Data

Paper Title Increased serum levels of KiSS1-derived peptides in non-small cell lung cancer patient liquid biopsies and biological relevance
Journal Translational lung cancer research
Published 2022
Abstract Studies have shown that the expression of KiSS1 can reduce the invasive ability of NSCLC drug-resistant cells. However, the levels of secreted products of the metastasis suppressor gene KiSS1 in patients are still poorly studied. We therefore carried out a series of studies to analyze the level of KiSS1 in liquid biopsy and explore the function of KiSS1. The expression levels of KiSS1-derived peptides were detected in 60 NSCLC patients by ELISA. The results showed that specific modulation of KiSS1 levels in liquid biopsies from NSCLC patients and modulation of cisplatin-induced apoptosis by KiSS1-derived peptides support the involvement of KiSS1 in cellular response to therapy and may serve as a potential biomarker in NSCLC.
Result

In this study, we found that elevated levels of KiSS1 could be detected in liquid biopsies from NSCLC patients compared with healthy donors. Release of soluble KiSS1 in the media of NSCLC cells and regulation of apoptosis by KiSS1-derived peptides following exposure to anticancer drugs. The experimental results indicated that KiSS1 may serve as a biomarker for NSCLC. However, more research is needed to validate our clinical findings and conjectures.

KiSS1 production by neurons.Fig.2. KiSS1 production by neurons. (Gatti, et al., 2022)

References

  1. Franssen, D.; Tena-Sempere, M. The kisspeptin receptor: A key G-protein-coupled receptor in the control of the reproductive axis. Best Practice & Research Clinical Endocrinology & Metabolism. 2018, 32(2): 107-123.
  2. Gatti, L.; et al. Increased serum levels of KiSS1-derived peptides in non-small cell lung cancer patient liquid biopsies and biological relevance. Translational lung cancer research. 2022, 11(7): 1315.
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