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用葡萄糖偶联的乳酸脱氢酶抑制剂双重靶向瓦博格效应。

Dual targeting of the Warburg effect with a glucose-conjugated lactate dehydrogenase inhibitor.

机构信息

Department of Biochemistry, University of Illinois at Urbana-Champaign, 600 S. Mathews Avenue, Urbana, IL 61801 (USA).

出版信息

Chembiochem. 2013 Nov 25;14(17):2263-7. doi: 10.1002/cbic.201300562. Epub 2013 Oct 31.

DOI:10.1002/cbic.201300562
PMID:24174263
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3919968/
Abstract

Effective glucose diet: We report the development and activity of glucose-conjugated LDH-A inhibitors designed for dual targeting of the Warburg effect (elevated glucose uptake and glycolysis) in cancer cells. Glycoconjugation could be applied to inhibitors of many enzymes involved in glycolysis or tumor metabolism.

摘要

有效葡萄糖饮食

我们报告了葡萄糖缀合的 LDH-A 抑制剂的开发和活性，该抑制剂旨在双重靶向癌细胞中的瓦博格效应（葡萄糖摄取和糖酵解增加）。糖缀合可以应用于许多参与糖酵解或肿瘤代谢的酶的抑制剂。

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本文引用的文献

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Glucose conjugation for the specific targeting and treatment of cancer.用于癌症特异性靶向治疗的葡萄糖缀合。
Chem Sci. 2013 Jun;4(6):2319-2333. doi: 10.1039/C3SC22205E.
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Assessing the differential action on cancer cells of LDH-A inhibitors based on the N-hydroxyindole-2-carboxylate (NHI) and malonic (Mal) scaffolds.基于 N-羟基吲哚-2-羧酸酯 (NHI) 和丙二酸 (Mal) 骨架评估 LDH-A 抑制剂对癌细胞的差异作用。
Org Biomol Chem. 2013 Oct 14;11(38):6588-96. doi: 10.1039/c3ob40870a. Epub 2013 Aug 29.
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Tumor-derived lactate modifies antitumor immune response: effect on myeloid-derived suppressor cells and NK cells.肿瘤衍生的乳酸改变抗肿瘤免疫反应：对髓源性抑制细胞和 NK 细胞的影响。
J Immunol. 2013 Aug 1;191(3):1486-95. doi: 10.4049/jimmunol.1202702. Epub 2013 Jul 1.
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Evaluation of LDH-A and glutaminase inhibition in vivo by hyperpolarized 13C-pyruvate magnetic resonance spectroscopy of tumors.通过肿瘤的 13C-丙酮酸极化磁共振波谱技术评估体内 LDH-A 和谷氨酰胺酶的抑制作用。
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Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase.鉴定取代的 2-硫代-6-氧代-1,6-二氢嘧啶作为人乳酸脱氢酶抑制剂。
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Fragment growing and linking lead to novel nanomolar lactate dehydrogenase inhibitors.片段生长和连接导致新型纳摩尔乳酸脱氢酶抑制剂。
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Design, synthesis, and preliminary biological evaluation of 6-O-glucose-azomycin adducts for diagnosis and therapy of hypoxic tumors.设计、合成及初步生物学评价 6-O-葡萄糖-阿霉素加合物用于诊断和治疗缺氧肿瘤。
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Visualizing sweetness: increasingly diverse applications for fluorescent-tagged glucose bioprobes and their recent structural modifications.可视化甜味：荧光标记葡萄糖生物探针的应用日益多样化及其最近的结构修饰。
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Enhancement of cyclopamine via conjugation with nonmetabolic sugars.通过与非代谢糖缀合来增强环巴胺。
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Design and synthesis of novel lactate dehydrogenase A inhibitors by fragment-based lead generation.基于片段的先导化合物生成法设计与合成新型乳酸脱氢酶 A 抑制剂
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