Review Article

Revisiting the Warburg Effect: Diet-Based Strategies for Cancer Prevention

Table 2

Therapeutics targeting the Warburg effect in cancers.

TargetCompoundEffectStatusReferences

GLUT1WZB117, STF-31Inhibits CLUT1
Induces cell cycle arrest and inhibits cancer cell growth
Preclinical[30, 31]
HK2DGInhibits HK
Tolerable adverse effects
Clinical trials discontinued[78]
PKM2TEPP-46Activates PKM2
Tetramer formation and suppress tumorigenesis
Preclinical[79] [80]
LDHAFX11Inhibits LDHA
Oxidative stress and inhibits tumor progression
Preclinical[81]
G6PD6-ANInduces oxidative stress
Induces cell cycle arrest and apoptosis selectively in irradiated human malignant cells
Preclinical[82]
MCT1AZD3965Inhibits uptake of extracellular lactatePhase I[83]
PDK1DCAInhibits PDK1Phase I-II[84] [85]
PKBAZD5363Inhibits PKB activityPhase I-II[86]
GDC0068Phase I[87]
GSK2141795Phase I completed[88]
GSK2110183Phase I-II completed
Phase II
[88]
MK-2206Akt inhibitor enhances antitumor efficacy by standard chemotherapeutic agents or molecular targeted drugs in vitro and in vivoPhase I-II[89]

Adapted from [90].