メタスチン(45-54)アミド, ヒト 化学特性,用途語,生産方法
説明
Kisspeptin-10, also called Metastin (45-54), is a 10 amino acid peptide that corresponds to the bioactive C-terminal 45-54 amino acids of metastin, a metastasis suppressor gene product. It acts as a potent agonist of GPR54 (OT7T175, AXOR12), with approximately 8-fold higher binding affinity than metastin (Ki values of 0.042 and 0.34 nM, respectively, for displacement of metastin (40-54)). Metastin (45-54) induces calcium mobilization in GPR54-transfected cells (EC50 = 0.18-1.1 nM). It inhibits the migration of GPR54-transfected CHO cells at concentrations of 10-100 nM, equaling the potency of full length metastin.
使用
Kisspeptin 10 (human) is a powerful and specific activator for AXOR12 and hOT7T175 receptors. The Kisspeptin 10 (human) amide has been utilized in studies involving progesterone release from MA-10 cells and in experiments to induce gonadal differentiation in clownfish.
生物学の機能
Metastin serves as a tumor suppressor by hindering the growth of secondary tumors. When KISS1R (KISS1 receptor) is activated upon binding with KISS1, it boosts intracellular calcium levels and activates MAPKs, which in turn limit cell mobility and proliferation. Metastin is a potential therapeutic target for various cancers, including melanoma, thyroid, bladder, squamous cell carcinoma of the esophagus, gastric, hepatocellular, and breast cancers.
In addition to its role in cancer suppression, metastin plays a critical role in reproduction. It regulates the hypothalamic-pituitary-gonadal axis by modulating gonadotropin-releasing hormone (GnRH) secretion, which influences the onset of puberty. Gene mutations can lead to central precocious puberty (CPP) in males, while impaired metastin signaling can result in isolated hypogonadotropic hypogonadism (IHH) in both humans and mice. Metastin can also elevate plasma levels of gonadotropins (follicle-stimulating hormone and luteinizing hormone) and promote ovulation in prepubescent female rats.
一般的な説明
Metastin is also known as kisspeptin 1 (KISS1). It is encoded by KISS1 gene, that is mapped to human chromosome 1q32. Metastin is a tumor suppressor protein, made up of 145 amino acids. The protein fragments contain RFamide motif at the C- terminal end. The encoded protein is expressed in the human hypothalamus, gonads, placenta, liver and pancreas. This novel?peptide?is mainly isolated from the human placenta.
Biochem/physiol Actions
Kisspeptin 10 (human) is a highly effective natural ligand for the Kisspeptin receptor (KISS1, GPR54). It exhibits strong binding affinity to rat and human KISS1 receptors, with Ki values of 1.59 and 2.33 nM respectively. This peptide inhibits metastasis and invasion in mouse melanomas and triggers gonadotropin release upon intracerebroventricular administration.
Clinical claims and research
Kisspeptin-10 level is useful in assessing the severity of preeclampsia and can be a novel marker downregulated in pregnant women with preeclampsia, especially in those who also developed impaired uteroplacental perfusion or intrauterine growth restriction[2].
メタスチン(45-54)アミド, ヒト 上流と下流の製品情報
原材料
準備製品