The Warburg effect provides attributes that facilitate tumor-cell resistance.

The metabolic reprogramming known as the Warburg effect, in which cancer cells preferentially convert glucose to lactate even in the presence of oxygen, is a defining hallmark of malignant transformation. Rather than reflecting defective mitochondria or a simple adaptation to hypoxia, aerobic glycolysis now emerges as a central hub that integrates glycolysis, the tricarboxylic acid cycle, the pentose phosphate pathway, and lactate metabolism to sustain the bioenergetic, biosynthetic, and redox demands of cancer cells. Enhanced glycolytic flux supports rapid ATP generation, nucleotide and lipid biosynthesis, NADPH production, and acetyl-CoA-dependent epigenetic regulation, thereby promoting DNA repair, antioxidant defense, chromatin remodeling, and proliferation. Beyond these metabolic outputs, many glycolytic enzymes, such as hexokinase 2, phosphoglycerate mutase 1, pyruvate kinase M2, phosphoglucose isomerase/autocrine motility factor, and aldolase A, exert non-enzymatic "moonlighting" functions that regulate apoptosis, checkpoint signaling, transcriptional programs, cytoskeletal remodeling, and epithelial-mesenchymal transition. Through this combination of enzymatic and non-enzymatic activities, the Warburg effect reinforces multiple dimensions of therapeutic resistance, including ATP-dependent drug efflux, resistance to DNA-damaging therapies, immune evasion, and invasive, EMT-associated phenotypes. In this review, we summarize current evidence linking aerobic glycolysis, lactate metabolism, and the pentose phosphate pathway to resistance against chemotherapy, radiotherapy, targeted therapy, and immunotherapy, with a particular focus on the non-metabolic functions of glycolytic enzymes. We further discuss how targeting glucose uptake, glycolysis, lactate transport, or pentose phosphate pathway flux, alone or in combination with conventional therapies and immune checkpoint blockade, may provide metabolism-informed strategies to overcome drug resistance in cancer.

Authors

Institutions

Publication Details

Journal
PubMed
Published
2026-06-18
DOI
https://doi.org/10.14670/hh-25-109
Primary Topic
Cancer, Hypoxia, and Metabolism
Type
article
Field-Weighted Citation Impact
0.00
Controls
|||
ALL TIME
JAN
FEB
MAR
APR
MAY
JUN
JUL
AUG
SEP
OCT
article

The Warburg effect provides attributes that facilitate tumor-cell resistance.

Takumi Mikawa, Matilde E. Lleonart, Hiroshi Kondoh, Hiroshi Seno et al.
PubMed
Cancer, Hypoxia, and Metabolism
article

The Warburg effect provides attributes that facilitate tumor-cell resistance.

Takumi Mikawa, Matilde E. Lleonart, Hiroshi Kondoh, Hiroshi Seno, Zhining Zhang
article en

Abstract

The metabolic reprogramming known as the Warburg effect, in which cancer cells preferentially convert glucose to lactate even in the presence of oxygen, is a defining hallmark of malignant transformation. Rather than reflecting defective mitochondria or a simple adaptation to hypoxia, aerobic glycolysis now emerges as a central hub that integrates glycolysis, the tricarboxylic acid cycle, the pentose phosphate pathway, and lactate metabolism to sustain the bioenergetic, biosynthetic, and redox demands of cancer cells. Enhanced glycolytic flux supports rapid ATP generation, nucleotide and lipid biosynthesis, NADPH production, and acetyl-CoA-dependent epigenetic regulation, thereby promoting DNA repair, antioxidant defense, chromatin remodeling, and proliferation. Beyond these metabolic outputs, many glycolytic enzymes, such as hexokinase 2, phosphoglycerate mutase 1, pyruvate kinase M2, phosphoglucose isomerase/autocrine motility factor, and aldolase A, exert non-enzymatic "moonlighting" functions that regulate apoptosis, checkpoint signaling, transcriptional programs, cytoskeletal remodeling, and epithelial-mesenchymal transition. Through this combination of enzymatic and non-enzymatic activities, the Warburg effect reinforces multiple dimensions of therapeutic resistance, including ATP-dependent drug efflux, resistance to DNA-damaging therapies, immune evasion, and invasive, EMT-associated phenotypes. In this review, we summarize current evidence linking aerobic glycolysis, lactate metabolism, and the pentose phosphate pathway to resistance against chemotherapy, radiotherapy, targeted therapy, and immunotherapy, with a particular focus on the non-metabolic functions of glycolytic enzymes. We further discuss how targeting glucose uptake, glycolysis, lactate transport, or pentose phosphate pathway flux, alone or in combination with conventional therapies and immune checkpoint blockade, may provide metabolism-informed strategies to overcome drug resistance in cancer.

PubMed
Universitat Autònoma de Barcelona (ES), Kyoto University (JP), Vall d'Hebron Institut de Recerca (ES), Kyoto University Hospital (JP), Centro de Investigación Biomédica en Red de Cáncer (ES)
Good health and well-being
Openalex Percentile: Top 7%
Cancer, Hypoxia, and Metabolism
AI Navigator

Ask Laika to Summarize, Analyze, and Connect papers live on the map.

Summarize Papers & Methodologies

Extract key findings, datasets, and comparative methods across publications.

Benchmark Rankings & Visual Analytics

Rank top research institutions, authors, funders, topics, and journals by Field-Weighted Citation Impact (FWCI) and paper volume with instant charts.

Connect Distant Disciplines

Bridge topological clusters on the map to find hidden collaborative intersections.