Mastoparan acetate(72093-21-1 free base)

Mastoparan acetate is a peptide toxin from wasp venom. It has the chemical structure Ile-Asn-Leu-Lys-Ala-Leu-Ala-Ala-Leu-Ala-Lys-Lys-Ile-Leu-NH2.
In vitro, Mastoparan has an amphiphilic nature and is reported to exert a variety of pharmacological and biochemical effects. Mastoparan induces exocytosis of hormones from anterior pituitary cells. Mastoparan stimulation of prolactin secretion is dose-dependent, time-dependent, reversible and required the presence of calcium. Mastoparan causes translocation of protein kinase C activity from a soluble to a membrane-attached form. Mastoparan is able to increase the intracellular Ca2+ concentration in Fura-2-loaded individual lactotrophs. Mastoparan is also able to interact with GTP-bindmg proteins. Thus, Mastoparan has been shown to facilitate exchange of nucleotides and to stimulate GTPase activity on G-proteins. It has therefore been proposed that the cellular effects of Mastoparan are due to an ability to mimic G-protein-linked agonist-liganded receptors^[1].

References:
[1].Mau SE, et al. Mastoparan, a wasp venom peptide, stimulates release of prolactin from cultured rat anterior pituitary cells. J Endocrinol. 1994 Jul;142(1):9-18.

Mastoparan acetate(72093-21-1 free base) 是一种来自黄蜂毒液的肽毒素。它的化学结构为 Ile-Asn-Leu-Lys-Ala-Leu-Ala-Ala-Leu-Ala-Lys-Lys-Ile-Leu-NH2。
在体外，Mastoparan具有两亲性，已报道可产生多种药理学和生化效应。Mastoparan可诱导前叶垂体细胞的激素外泌。Mastoparan对催乳素分泌的刺激依赖于剂量、时间、可逆，并且需要钙的存在。Mastoparan导致蛋白激酶C活性从可溶形态向膜结合形态的转移。Mastoparan能够在Fura-2载体的单个泌乳细胞内增加Ca2+浓度。此外，Mastoparan还能与GTP结合蛋白互动。因此，研究表明Mastoparan能够促进核苷酸的交换，并刺激G蛋白的GTP酶活性。据此提出，Mastoparan对细胞的影响可能由于其模仿G蛋白偶联受体激动剂结合态的能力^[1]。