Table 1.
Inhibitors of selected proteins involved in the Warburg effect
| Target | Agent | State of development |
|---|---|---|
| GLUT-1 | WZB 117 | In vivo [109] |
| Cytochalasin B | In vivo [110] | |
| Glupin | In vitro [111] | |
| Silybin | Clinical phase II [112] | |
| RNAi | Early clinical phase I [113] | |
| Hexokinase | 2-Deoxyglucose | Clinical phase II [114] |
| Lonidamine [115] | Clinical phase III [116] | |
| 3-Bromopyruvic acid [117] | Clinical phase I [118] | |
| Methyl Jasmonate | In vitro [119] | |
| BNBZ | In vivo [120] | |
| Astragalin | In vitro and in vivo [121] | |
| Resveratrol [122] | Clinical phase II [123] | |
| Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) | Asperphenin B | In vivo and in vitro [124] |
| Koningic acid | In vitro [125] | |
| Iodoacetate | In vitro [126] and in vivo[127] | |
| Lactate dehydrogenase A (LDHA) | 5-ALA | Clinical phase II study record | Beta ClinicalTrials.gov. https://beta.clinicaltrials.gov/study/NCT05101798 |
| Oxalate | In vivo [128] | |
| FX 11 | In vitro [129, 130] | |
| PSTMB | In vitro [131] | |
| Pyruvate kinase isoform M2 (PKM2) | miRNA | In vitro [132] |
| Shikonin | Clinical phase I [133] | |
| PFKFB3 | PFK-158 | Clinical phase I [134] |
| 3PO | Preclinical phase [134] | |
| MCT1 | AZD3965 | Clinical phase I [135] |
| MCT4 | AZD0095 | Preclinical phase [136] |
| Lactate | Lactate oxidase/catalase | Preclinical phase [103] |
BNBZ benitrobenrazide, PSTMB 1-(phenylseleno)-4-(trifluoromethyl) benzene, 5-ALA 5-aminolevulinic acid, 3PO 3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one, RNAi RNA interference, miRNA microRNA