Effects of the Anti‐Tumor Agent 3‐Bromopyruvate (3BrPA) on Glycolytic Energy Metabolism

Robey, R. Brooks; Hong, Richard; Zhong, Lihui; Feng, Lanfei; Zhang, Hongmei

doi:10.1096/fasebj.21.6.a1190-a

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In-vitro-Effekte von Dichloracetat in hypoxischen Tumorzellen

Gerhard¹

2015

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In-vitro-Effekte von Dichloracetat in hypoxischen Tumorzellen

Gerhard¹

2015

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Metabolic Targeting of Malignant Tumors: Small-Molecule Inhibitors of Bioenergetic Flux

Mathupala¹

2011

PRA

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Metabolism in tumors deviates significantly from that of normal tissues. Increasingly, the underlying aberrant metabolic pathways are being considered as novel targets for cancer therapy. Denoted “metabolic targeting”, small molecule drugs are under investigation for focused inhibition of key metabolic steps that are utilized by tumors, since such inhibitors should harbor minimal toxicity towards surrounding normal tissues.This review will examine the primary biochemical pathways that tumors harness to enhance their bioenergetic capacity, which in turn, help their rapid proliferation and metastasis within the host. It is hoped that “metabolite-mimetic” drugs can be utilized to interfere with metabolic flux pathways active within the tumor, and across tumor-microenvironment boundary. In fact, the major pathways of mammalian metabolism, i.e., the carbohydrate, amino-acid, and fatty-acid metabolic pathways have been examined as putative targets for drug development, with some drug candidates advancing to phase II/III stages. In this regard, glucose metabolism, i.e., the glycolytic pathway - that predominates the bio-energetic flux in tumors, and the associated mitochondrial metabolism have received the most attention as suitable “druggable” targets, focused either at the pathway enzymes or at the plasma-membrane-bound metabolite transporters. Outlined in this review are pre-clinical studies that have led to the discovery of promising drug candidates to target tumor-metabolic flux, and ensuing patents, with descriptions of the biochemical rationale for the combinatorial strategy of a particular metabolic pathway-drug candidate pair.

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Effects of the Anti‐Tumor Agent 3‐Bromopyruvate (3BrPA) on Glycolytic Energy Metabolism

Cited by 2 publications

References 0 publications

In-vitro-Effekte von Dichloracetat in hypoxischen Tumorzellen

In-vitro-Effekte von Dichloracetat in hypoxischen Tumorzellen

Metabolic Targeting of Malignant Tumors: Small-Molecule Inhibitors of Bioenergetic Flux

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