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 their exposure to different oxygen levels (“Warburg effect”). This condition originates from a set of gene regulations, consisting in 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 acting 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 mini‐review is to provide an update about some of the most recently patented bioactive molecules, that are able to interfere with cancer glycolysis, as well as about their use in specific combination therapies.

An Update on Patents Covering Agents That Interfere with the Cancer Glycolytic Cascade

Fortunato, Serena
Primo
;
Bononi, Giulia;Granchi, Carlotta;Minutolo, Filippo
Ultimo
2018-01-01

Abstract

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 their exposure to different oxygen levels (“Warburg effect”). This condition originates from a set of gene regulations, consisting in 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 acting 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 mini‐review is to provide an update about some of the most recently patented bioactive molecules, that are able to interfere with cancer glycolysis, as well as about their use in specific combination therapies.
2018
Fortunato, Serena; Bononi, Giulia; Granchi, Carlotta; Minutolo, Filippo
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11568/929836
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