2-Deoxy-D-glucose (2DG), is a glucose analogue, act as competitive glycolytic inhibitor [1].
2-Deoxy-d-glucose (2DG) has been demonstrated to be a powerful agent for blocking and probing increased sugar metabolism in cancer cells [2]. Because of its similarity to glucose, 2-Deoxy-D-glucose inhibits glycolysis, but as chemically it is also 2-deoxymannose it is able to compete with mannose in the growing lipid-linked oligosaccharide chain during the initial steps of N-linked glycosylation. This mannose-like property of 2-Deoxy-D-glucose results in misfolded proteins leading to endoplasmic reticulum (ER) stress [3].
2-Deoxy-D-glucose delivered in the diet produces cardiac toxicity in rats at doses ranging from 0.02 to 0.3 g/kg (0.04-0.6% 2-Deoxy-D-glucose by weight in the diet) and hastens mortality at doses above 0.2 g/kg (0.4% in the diet) [4]. 2-Deoxy-D-glucose evoked increases in plasma adrenaline and glucose at 20 and 60 min [5].
References:
[1]. Mühlenberg T, Grunewald S, Treckmann J, et al. Inhibition of KIT-glycosylation by 2-deoxyglucose abrogates KIT-signaling and combination with ABT-263 synergistically induces apoptosis in gastrointestinal stromal tumor[J]. PloS one, 2015, 10(3): e0120531.
[2]. El Mjiyad N, Caro-Maldonado A, Ramirez-Peinado S, Munoz-Pinedo C. Sugar-free approaches to cancer cell killing. Oncogene. 2011 Jan;30(3):253-64.
[3]. Kurtoglu, Metin, Johnathan C. Maher, and Theodore J. Lampidis. "Differential toxic mechanisms of 2-deoxy-D-glucose versus 2-fluorodeoxy-D-glucose in hypoxic and normoxic tumor cells." Antioxidants & redox signaling 9.9 (2007): 1383-1390.
[4]. Minor R K, Smith Jr D L, Sossong A M, et al. Chronic ingestion of 2-deoxy-D-glucose induces cardiac vacuolization and increases mortality in rats[J]. Toxicology and applied pharmacology, 2010, 243(3): 332-339.
[5]. Bobrovskaya L, Damanhuri H A, Ong L K, et al. Signal transduction pathways and tyrosine hydroxylase regulation in the adrenal medulla following glucoprivation: an in vivo analysis[J]. Neurochemistry international, 2010, 57(2): 162-167.
2-Deoxy-D-glucose (2DG)，是一种葡萄糖类似物，作为竞争性糖酵解抑制剂[1]。
2-脱氧-d-葡萄糖 (2DG) 已被证明是一种强大的药物，可阻断和探测癌细胞中增加的糖代谢[2]。由于其与葡萄糖的相似性，2-脱氧-D-葡萄糖抑制糖酵解，但在化学上它也是 2-脱氧甘露糖，它能够在 N-连接糖基化的初始步骤中与生长的脂质连接的寡糖链中的甘露糖竞争. 2-脱氧-D-葡萄糖的这种类似甘露糖的特性导致错误折叠的蛋白质导致内质网 (ER) 应激 [3]。
饮食中提供的 2-脱氧-D-葡萄糖在 0.02 至 0.3 g/kg 的剂量范围内（饮食中 0.04-0.6% 2-脱氧-D-葡萄糖按重量计）对大鼠产生心脏毒性并加速死亡率剂量超过 0.2 g/kg（饮食中的 0.4%）[4]。 2-脱氧-D-葡萄糖在 20 分钟和 60 分钟时引起血浆肾上腺素和葡萄糖的增加[5]。