Kisspeptin-10Trifluoroacetate是Kisspeptin-10的三氟乙酸盐形式。Kisspeptin-10是具有全部生物活性的Kisspeptin最短多肽段，它是一种有效的GPR54内源性配体。
Kisspeptin-10 Trifluoroacetate is the trifluoroacetate salt form of Kisspeptin-10. Kisspeptin-10, the minimal kisspeptin sequence with biological activity, is a potent endogenous ligand for GPR54.
Kisspeptin-10 is the minimal kisspeptin sequence with full intrinsic bioactivity. Kisspeptins are a family of peptides encoded by the Kiss1 gene and are the natural ligands of the orphan g protein-coupled receptor GPR54[1]. Kisspeptins act as the principal positive regulator of the reproductive axis by directly stimulating gonadotropin-releasing hormone (GnRH) neuron activity. Kisspeptin-10 also has a direct stimulating effect on luteinizing hormone (LH) secretion in bovine anterior pituitary (AP) cells[2]. Different concentrations of Kisspeptin-10 have distinct effects on migration and proliferation of endothelial cells. Migration and proliferation of endothelial cells are increased at lower concentration of Kisspeptin-10 specially at 100 nM while higher concentration reduced both migration and proliferation[3].
Intravenous infusion of kisspeptin-10 (7.5, 35, and 100 nM) induces a dose-dependent increase in LH secretion. The stimulatory effect of kisspeptin-10 (100 n nM) on LH secretion is blocked by the GnRH antagonist cetrorelix, precluding a singular action on gonadotropes[4]. Kisspeptin-10 inhibits angiogenesis in vivo. Kp-10 inhibits tumor growth in SCID mice xenografted with human prostate cancer cells (PC-3) through inhibiting tumor angiogenesis[5].
[1]. Kotani M, et al. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. [2]. Kadokawa H, et al. Kisspeptin-10 stimulates the secretion of growth hormone and prolactin directly from cultured bovine anterior pituitary cells. Anim Reprod Sci. 2008 May;105(3-4):404-8. [3]. Golzar F, et al. The effects of kisspeptin-10 on migration and proliferation of endothelial cell. Adv Biomed Res. 2015 Feb 11;4:41. [4]. Kinsey-Jones JS, et al. Effects of kisspeptin-10 on the electrophysiological manifestation of gonadotropin-releasing hormone pulse generator activity in the female rat. Endocrinology. 2008 Mar;149(3):1004-8. [5]. Cho SG, et al. Kisspeptin-10, a KISS1-Derived Decapeptide, Inhibits Tumor Angiogenesis by Suppressing Sp1-Mediated VEGF Expression and FAK/Rho GTPase Activation. Cancer Res. 2009 Sep 1;69(17):7062-70.
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