[D-Phe⁶, Des-Met¹⁴]bombesin (6-14) ethyl amide (DPDMB), bombesin receptor antagonist with IC₅₀ values for cellular secretion and growth approaching the picomolar region.
编号：180284
CAS号：124199-90-2
单字母：H2N-fQWAVGHL-NHEt
| 编号: | 180284 |
| 中文名称: | 蛙皮素(DPhe6, Leu-NHEt13, des-Met14)-Bombesin(6-14) |
| 英文名: | (DPhe6, Leu-NHEt13, des-Met14)-Bombesin(6-14) |
| CAS号: | 124199-90-2 |
| 单字母: | H2N-fQWAVGHL-NHEt |
| 三字母: | H2N N端氨基 -DPheD型笨丙氨酸 -Gln谷氨酰胺 -Trp色氨酸 -Ala丙氨酸 -Val缬氨酸 -Gly甘氨酸 -His组氨酸 -Leu亮氨酸 -NHEtC端乙胺基化修饰 |
| 氨基酸个数: | 8 |
| 分子式: | C49H69N12O9 |
| 平均分子量: | 970.15 |
| 精确分子量: | 969.53 |
| 等电点(PI): | - |
| pH=7.0时的净电荷数: | 1.21 |
| 平均亲水性: | -1.4285714285714 |
| 疏水性值: | 0.58 |
| 外观与性状: | 白色粉末状固体 |
| 消光系数: | 5500 |
| 来源: | 人工化学合成，仅限科学研究使用，不得用于人体。 |
| 纯度: | 95%、98% |
| 盐体系: | 可选TFA、HAc、HCl或其它 |
| 生成周期: | 2-3周 |
| 储存条件: | 负80℃至负20℃ |
| 标签: | D型氨基酸肽 蛙皮素(Bombesin) |
[D-Phe⁶, Des-Met¹⁴]bombesin (6-14) ethyl amide (DPDMB), bombesin receptor antagonist with IC₅₀ values for cellular secretion and growth approaching the picomolar region.
很多蛋白在细胞中非常容易被降解，或被标记，进而被选择性地破坏。但含有部分D型氨基酸的多肽则显示了很强的抵抗蛋白酶降解能力。
Definition
Bombesin is a polypeptide that is found in the brain and gastrointestinal tract. Experimentally it has shown to cause the secretion of various substances (as gastrin and cholecystokinin) and to inhibit intestinal motility.
Discovery
Bombesin was isolated from the skin of the frog Bombina bonmina by Anastasi and team in 19711.
Classification
Bombesin-like peptides are grouped into three families - 1) Bombesin group, viz., bombesin and alytesin, 2) Ranatensin group viz., ranatensins, litorin, and Rohdei litorin, 3) Phyllolitorin group viz., Leu(8)- and Phe(8)-phyllolitorins.
Structural characteristics
Bombesin is a small peptide of 14 amino acids.
Mode of action
The biological activity of bombesin is mediated by binding to specific receptors viz., gastrin releasing peptide receptor (GRPR; called also BB2 receptor), neuromedin B receptor (NMBR; called also BB1 receptor) and bombesin receptor subtype 3 (BRS-3; called also BB3 receptor). Bombesin induce Ca2+ release from intracellular stores2.
Functions
Bombesin and bombesin-like factors show a wide spectrum of biological activities. It regulates the contraction of smooth muscle cells, induction of the secretion of neuropeptides and hormones. It is one of the most powerful substances showing anorexic effects in the hypothalamus. It induces the release of gastrin and cholecystokinin in the intestines and the pancreas. They also posses activities of cytokines.
References
1. Anastasi A, Erspamer V, Bucci M (1971). Isolation and structure of bombesin and alytesin, 2 analogous active peptides from the skin of the European amphibians Bombina and Alytes. Experientia., 27(2):166-167.
2. Wang JL, Kalyanaraman S, Vivo MD, Gautam N (1996). Bombesin and thrombin affect discrete pools of intracellular calcium through different G-proteins. Biochem J., 320:87-91.
| DOI | 名称 | |
|---|---|---|
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| 10.1523/JNEUROSCI.3821-05.2005 | Gastrin-releasing peptide promotes suprachiasmatic nuclei cellular rhythmicity in the absence of vasoactive intestinal polypeptide-VPAC2 receptor signaling | 下载 |
| 10.1074/jbc.271.40.24684 | Spacial compartmentalization of Ca2+ signaling complexes in pancreatic acini | 下载 |
| 10.1016/s0196-9781(01)00368-0 | Proadrenomedullin N-terminal 20 peptide (PAMP) inhibits food intake and gastric emptying in mice | 下载 |
