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Ghrelin (mouse, rat) TFA是一种胃肠道分泌生成的、由28个氨基酸组成的内源性脑肠肽，具有包括刺激食欲在内的多种生理功能，同时也是ghrelin（GHS）受体的内源性激动剂肽。

Ghrelin is a 28 amino acid peptide hormone that has various effects on the body, including stimulating appetite, nutrient sensing and meal initiation. It has also been found to regulate insulin resistance, diabetes and obesity and asserts its functional affects through acting as an endogenous ligand for the growth hormone secretagogue receptor (GHS-R). Its wider functions such as glucose homeostasis, energy homeostasis, cardio-protective effects, its role in bone metabolism and its potential to be a target for cancer means that it can be used to develop therapies for a whole spectrum of diseases. This product is available in the trifluoroacetate salt form and as a 0.1mg vial.

胃饥饿素\生长素释放肽(Ghrelin)的定义

生长素释放肽是生长激素促分泌素受体（GHSR）的内源性配体，其主要在胃中合成，并响应营养状态的急性和慢性变化而释放【1】。

Ghrelin is an endogenous ligand for the growth hormone secretagogue receptor (GHSR), which is synthesized principally in the stomach and is released in response to acute and chronic changes in nutritional state 【1】.

胃饥饿素\生长素释放肽(Ghrelin)的相关肽

生长素释放肽基因编码前体蛋白preproghrelin。替代mRNA剪接和/或蛋白水解加工产生生长素释放肽和其他潜在活性肽。肽obestatin来源于preproghrelin的C末端区域，对细胞增殖有直接影响【2】。配体des-Gln14-ghrelin是一种27个氨基酸的肽，在Ser3处具有正辛酰基修饰，除了缺失一个谷氨酰胺外，与ghrelin相同，并且是通过大鼠ghrelin基因的可变剪接产生的。Des-Gln14-ghrelin具有与ghrelin相同的效力。另一方面，未修饰的去正辛酰基形式的生长素释放肽（去酰基生长素释放肽）对细胞内Ca2+和GH分泌的升高没有影响1。来自肠道，大脑和其他组织的其他肽激素（即胃动素，TRH，PACAP，GnRH，瘦素，FMRF酰胺，甘丙肽，NPY，NPW）也在调节家畜和低等脊椎动物的GH分泌中发挥作用【3】。

The ghrelin gene encodes a precursor protein, preproghrelin. Alternative mRNA splicing and/or proteolytic processing derives ghrelin and other potentially active peptides. The peptide obestatin is derived from the C-terminal region of preproghrelin and has direct effects on cell proliferation【2】. The ligand des-Gln14-ghrelin, a 27-amino acid peptide with an n-octanoyl modification at Ser3, is identical to ghrelin except for the deletion of one glutamine, and is produced through alternative splicing of the rat ghrelin gene. Des-Gln14-ghrelin has the same potency as ghrelin. On the other hand, the unmodified, des-n-octanoyl form of ghrelin (desacyl ghrelin) has no effect on the elevation of intracellular Ca2+ and GH secretion1. Other peptide hormones (i.e., motilin, TRH, PACAP, GnRH, leptin, FMRF amide, galanin, NPY, NPW) from gut, brain and other tissues also play a role in modulating GH secretion in livestock and lower vertebrate species 【3】.

胃饥饿素\生长素释放肽(Ghrelin)的发现

Masayasu Kojima及其同事于1999年报道了生长素释放肽的发现【4】。

The discovery of ghrelin was reported by Masayasu Kojima and colleagues in 1999 【4】.

胃饥饿素\生长素释放肽(Ghrelin)的结构特征

生长素释放肽被合成为前激素（13kDa），然后经过蛋白水解处理产生28个氨基酸的肽（3kDa），在其第三个丝氨酸残基处具有正辛酰基修饰，这对其生物活性至关重要【5】。

Ghrelin is synthesized as a preprohormone (13kDa), and then proteolytically processed to yield a 28 amino acid peptide (3kDa) with an n-octanoyl modification at its third serine residue, which is essential for its biological activity【5】.

 
胃饥饿素\生长素释放肽(Ghrelin)的作用机制

生长素释放肽受体在生长素释放肽被发现之前就已为人所知。垂体前叶内的细胞带有生长激素分泌受体（GHS-R）。生长素释放肽与GHS-R结合并刺激生长激素（GH）的释放。

The ghrelin receptor was known well before ghrelin was discovered. Cells within the anterior pituitary bear a growth hormone secretagoue receptor (GHS-R). Ghrelin bind to the GHS-R and stimulates the release of the growth hormone (GH).

 胃饥饿素\生长素释放肽(Ghrelin)的功能

生长素释放肽在大鼠和人类中有效诱导GH释放。生长素释放肽主要产生于胃中不同的内分泌细胞。产生生长素释放肽的神经元也存在于下丘脑弓状核中，该区域调节GH的释放和食物摄入。生长素释放肽还参与刺激进食和调节能量代谢【5】。

Ghrelin potently induces GH release both in rats and humans. Ghrelin is primarily produced in distinct endocrine cells in the stomach. Ghrelin-producing neurons are also present in the hypothalamic arcuate nucleus, a region that regulates GH release and food intake. Ghrelin is also involved in the stimulation of feeding and the regulation of energy metabolism【5】.

胃饥饿素\生长素释放肽(Ghrelin)的相关文献

1. Hosoda H, Kojima M, Kangawa K (2002). Ghrelin and the Regulation of Food Intake and Energy Balance. Molecular Interventions, 2(8):494-503.

2. Seim I, Amorim L, Walpole C, Carter S, Chopin LK, Herington AC (2009). Ghrelin gene-related peptides: multi-functional endocrine/autocrine modulators in health and disease. Clin Exp Pharmacol Physiol .

3. Anderson LL, Jeftinija S, Scanes CG, Stromer MH, Lee JS, Jeftinija K, Glavaski-Joksimovic A. (2005). Physiology of ghrelin and related peptides. Domestic Animal Endocrinology, 29(1):111-144.

4. Book: Ghrelin. Chapter 2: Discovery of Ghrelin, an Endogenous Ligand for the Growth-Hormone Secret Agogue Receptor. By Masayasu Kojima, Hiroshi Hosoda, Hiroyuki Kaiya and Kenji Kangawa.

5. Kangawa K, Kojima M, Hosoda H (2004). Ghrelin: discovery and physiological significance. Nippon Rinsho. 62 (9):317-323.