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An Update on Patents Covering Agents That Interfere with the Cancer Glycolytic Cascade
ChemMedChem ( IF 3.4 ) Pub Date : 2018-10-09 , DOI: 10.1002/cmdc.201800447
Serena Fortunato 1 , Giulia Bononi 1 , Carlotta Granchi 1 , Filippo Minutolo 1
Affiliation  

Many tumors exhibit altered metabolic characteristics relative to normal and healthy tissues. Their metabolic profile highlights a strong prevalence of glycolysis over oxidative phosphorylation, regardless of their exposure to different oxygen levels (the Warburg effect). This condition originates from a set of gene regulations, consisting of the overexpression of some enzymes or transporters involved in the glycolytic pathway. Therefore, these effectors may constitute appealing targets for the implementation of selective therapeutic interventions against cancer. Recently, significant progress has been made in the discovery of molecules that act at various levels of the glycolytic pathway of tumor cells. So far, some of the most widely explored targets of the glycolytic cascade are represented by glucose transporters, hexokinase, 6‐phosphofructokinase, enolase, pyruvate kinase, lactate dehydrogenase, and monocarboxylate transporters. The purpose of this minireview is to provide an update on some of the most recently patented bioactive molecules that are able to interfere with cancer glycolysis, and on their use in specific combination therapies.

中文翻译:

干扰糖酵解级联反应的专利保护剂的更新

相对于正常组织和健康组织,许多肿瘤表现出改变的代谢特征。它们的代谢特征突显出糖酵解优于氧化磷酸化的普遍性,无论它们暴露在不同的氧气水平下(Warburg效应)。这种情况源于一系列基因调控,包括与糖酵解途径有关的某些酶或转运蛋白的过表达。因此,这些效应子可以构成用于实施针对癌症的选择性治疗干预的有吸引力的靶标。最近,在发现在肿瘤细胞糖酵解途径的各种水平上起作用的分子方面已经取得了重大进展。到目前为止,糖酵解级联的一些最广泛探索的靶标是葡萄糖转运蛋白,己糖激酶,6-磷酸果糖激酶,烯醇酶,丙酮酸激酶,乳酸脱氢酶和单羧酸盐转运蛋白。这项小型审查的目的是提供一些能够干扰癌症糖酵解的最新专利生物活性分子及其在特定联合疗法中的应用的更新。
更新日期:2018-10-09
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