cholera toxin

Cholera toxin, a multifunctional protein produced by Vibrio cholera, does not just cause cholera but also able to influence the immune system in many ways.

霍乱毒素B （来源于霍乱弧菌） 对细胞无毒，且不具备内在腺苷酸环化酶活性。它通过与神经节苷脂 GM1.8 结合附着于细胞。研究表明，Cholera toxin B subunit 是小胶质细胞的可靠标记物（因为其细胞表面神经节苷脂 GM1 丰富），但不适用于标记少突胶质细胞或星形胶质细胞。Cholera toxin B subunit 也被报告为一种利用免疫组织化学研究轴突运输的极佳示踪剂，并已被广泛用作膜脂筏的标记物。

Iobenguane sulfate (MIBG sulfate) 是一种具有抗肿瘤活性的神经递质去甲肾上腺素的类似物。Iobenguane sulfate 是一种高亲和力的霍乱毒素底物，干扰细胞单核(ADP-核糖基化)。放射性碘代 Iobenguane sulfate 可用于肾上腺肿瘤诊断和肿瘤靶向药物的研究。

Ganglioside GM1is a monosialylated ganglioside and the prototypic ganglioside for those containing one sialic acid residue.1,2It is found in a large variety of cells, including immune cells and neurons, and is enriched in lipid rafts in the cell membrane.3It associates with growth factor receptors, including TrkA, TrkB, and the GDNF receptor complex containing Ret and GFRα, and is required for TrkA expression on the cell surface. Ganglioside GM1interacts with other proteins to increase calcium influx, affecting various calcium-dependent processes, including inducing neuronal outgrowth during differentiation. Ganglioside GM1acts as a receptor for cholera toxin, which binds to its oligosaccharide group, facilitating toxin cell entry into epithelial cells of the jejunum.4,5Similarly, it is bound by the heat-labile enterotoxin fromE. coliin the pathogenesis of traveler's diarrhea.6Ganglioside GM1gangliosidosis, characterized by a deficiency in GM1-β-galactosidase, the enzyme that degrades ganglioside GM1, leads to accumulation of the gangliosides GM1and GA1in neurons and can be fatal in infants.1Levels of ganglioside GM1are decreased in the substantia nigra pars compacta in postmortem brain from patients with Parkinson's disease.3Ganglioside GM1mixture contains a mixture of ovine ganglioside GM1molecular species with primarily C18:0 fatty acyl chain lengths, among various others. [Matreya, LLC. Catalog No. 1544] 1.Kolter, T.Ganglioside biochemistryISRN Biochem.506160(2012) 2.Mocchetti, I.Exogenous gangliosides, neuronal plasticity and repair, and the neurotrophinsCell Mol. Life Sci.62(19-20)2283-2294(2005) 3.Ledeen, R.W., and Wu, G.The multi-tasked life of GM1 ganglioside, a true factotum of natureTrends Biochem. Sci.40(7)407-418(2015) 4.Turnbull, W.B., Precious, B.L., and Homans, S.W.Dissecting the cholera toxin-ganglioside GM1 interaction by isothermal titration calorimetryJ. Am. Chem. Soc.126(4)1047-1054(2004) 5.Blank, N., Schiller, M., Krienke, S., et al.Cholera toxin binds to lipid rafts but has a limited specificity for ganglioside GM1Immunol. Cell Biol.85(5)378-382(2007) 6.Minke, W.E., Roach, C., Hol, W.G., et al.Structure-based exploration of the ganglioside GM1 binding sites of Escherichia coli heat-labile enterotoxin and cholera toxin for the discovery of receptor antagonistsBiochemistry38(18)5684-5692(1999)

GM1a Ganglioside oligosaccharide为ganglioside GM1的半合成形式，后者作为霍乱毒素的天然受体，在生长调节及激素诱导反应的耦合中具有关键功能。

Endo CNTinh-03 具有抑制作用，可阻止 cAMP 和 cGMP 通过 G 蛋白偶联受体、腺苷酸环化酶及鸟苷酸环化酶的激动剂而升高（IC50为 4 μM）。此外，该化合物能够抑制霍乱毒素与Escherichia coli(STa) 毒素导致的氯离子电流，有效改善小鼠分泌性腹泻的症状，并在多囊肾病模型中防止囊肿的形成。

CTB (Cholera Toxin B subunit) 是一种 p300 组蛋白乙酰转移酶的激活剂，可诱导 MCF-7 细胞凋亡。

Ganglioside GM1-bindingpeptidesp3 为一种人工合成多肽，具备与GM1神经节苷脂的五糖部分进行特异性结合的能力。该多肽的动态转变对于理解GM1在多种受体功能中的作用至关重要，特别是在霍乱毒素感染的常见途径上。此外，Ganglioside GM1-bindingpeptidesp3 还常被应用于研究GM1与其配体之间的相互作用。