| Source: |
| Type: enzyme |
| PKM2 (Pyruvate Kinase, Muscle 2) is an enzyme that plays a crucial role in glycolysis, the process by which cells convert glucose into energy. PKM2 is a key regulatory enzyme in the glycolytic pathway, and it is primarily expressed in various tissues, including muscle, brain, and cancer cells. -C-myc is a common oncogene that enhances aerobic glycolysis in the cancer cells by transcriptionally activating GLUT1, HK2, PKM2 and LDH-A -PKM2 has been shown to be overexpressed in many types of tumors, including breast, lung, and colon cancer. This overexpression may contribute to the development and progression of cancer by promoting glycolysis and energy production in cancer cells. -inhibition of PKM2 may cause ATP depletion and inhibiting glycolysis. -PK exists in four isoforms: PKM1, PKM2, PKR, and PKL -PKM2 plays a role in the regulation of glucose metabolism in diabetes. -PKM2 is involved in the regulation of cell proliferation, apoptosis, and autophagy. – Pyruvate kinase catalyzes the final, rate-limiting step of glycolysis, converting phosphoenolpyruvate (PEP) to pyruvate with the production of ATP. – The PKM2 isoform is uniquely regulated and can exist in both highly active tetrameric and less active dimeric forms. – Cancer cells often favor the dimeric form of PKM2 to slow pyruvate production, thereby accumulating upstream glycolytic intermediates that can be diverted into anabolic pathways to support cell growth and proliferation. – Under low oxygen conditions, cancer cells rely on altered metabolic pathways in which PKM2 is a key player. – The shift to aerobic glycolysis (Warburg effect) orchestrated in part by PKM2 helps tumor cells survive and grow in hypoxic conditions. – Elevated expression of PKM2 is frequently observed in many cancer types, including lung, breast, colorectal, and pancreatic cancers. – High levels of PKM2 are often correlated with enhanced tumor aggressiveness, poor differentiation, and advanced clinical stage. PKM2 in carcinogenesis and oncotherapy Inhibitors of PKM2: -Shikonin, Resveratrol, Baicalein, EGCG, Apigenin, Curcumin, Ursolic Acid, Citrate (best known as an allosteric inhibitor of phosphofructokinase-1 (PFK-1), a key rate-limiting enzyme in glycolysis) potential to directly inhibit or modulate PKM2 is less well established Full List of PKM2 inhibitors from Database -key connected observations: Glycolysis↓, lactateProd↓, ROS↑ in cancer cell, while some result for opposite effect on normal cells. Tumor pyruvate kinase M2 modulators Flavonoids effect on PKM2 Compounds name IC50/AC50uM Effect Flavonols 1. Fisetin 0.90uM Inhibition 2. Rutin 7.80uM Inhibition 3. Galangin 8.27uM Inhibition 4. Quercetin 9.24uM Inhibition 5. Kaempferol 9.88uM Inhibition 6. Morin hydrate 37.20uM Inhibition 7. Myricetin 0.51uM Activation 8. Quercetin 3-b- D-glucoside 1.34uM Activation 9. Quercetin 3-D -galactoside 27-107uM Ineffective Flavanons 10. Neoeriocitrin 0.65uM Inhibition 11. Neohesperidin 14.20uM Inhibition 12. Naringin 16.60uM Inhibition 13. Hesperidin 17.30uM Inhibition 14. Hesperitin 29.10uM Inhibition 15. Naringenin 70.80uM Activation Flavanonols 16. (-)-Catechin gallateuM 0.85 Inhibition 17. (±)-Taxifolin 1.16uM Inhibition 18. (-)-Epicatechin 1.33uM Inhibition 19. (+)-Gallocatechin 4-16uM Ineffective Phenolic acids 20. Ferulic 11.4uM Inhibition 21. Syringic and 13.8uM Inhibition 22. Caffeic acid 36.3uM Inhibition 23. 3,4-Dihydroxybenzoic acid 78.7uM Inhibition 24. Gallic acid 332.6uM Inhibition 25. Shikimic acid 990uM Inhibition 26. p-Coumaric acid 22.2uM Activation 27. Sinapinic acids 26.2uM Activation 28. Vanillic 607.9uM Activation |
| 2325- | 2DG, | Research Progress of Warburg Effect in Hepatocellular Carcinoma |
| - | Review, | Var, | NA |
| 2326- | 2DG, | Caloric Restriction Mimetic 2-Deoxyglucose Alleviated Inflammatory Lung Injury via Suppressing Nuclear Pyruvate Kinase M2–Signal Transducer and Activator of Transcription 3 Pathway |
| - | in-vivo, | Nor, | NA |
| 3434- | ALA, | Alpha lipoic acid modulates metabolic reprogramming in breast cancer stem cells enriched 3D spheroids by targeting phosphoinositide 3-kinase: In silico and in vitro insights |
| - | in-vitro, | BC, | MCF-7 | - | in-vitro, | BC, | MDA-MB-231 |
| - | in-vitro, | BC, | MCF-7 |
| 1548- | Api, | A comprehensive view on the apigenin impact on colorectal cancer: Focusing on cellular and molecular mechanisms |
| - | Review, | Colon, | NA |
| 2319- | Api, | Apigenin sensitizes radiotherapy of mouse subcutaneous glioma through attenuations of cell stemness and DNA damage repair by inhibiting NF-κB/HIF-1α-mediated glycolysis |
| - | in-vitro, | GBM, | NA |
| 2318- | Api, | Apigenin as a multifaceted antifibrotic agent: Therapeutic potential across organ systems |
| - | Review, | Nor, | NA |
| 2317- | Api, | Apigenin intervenes in liver fibrosis by regulating PKM2-HIF-1α mediated oxidative stress |
| - | in-vivo, | Nor, | NA |
| 2299- | Api, | Flavonoids Targeting HIF-1: Implications on Cancer Metabolism |
| - | Review, | Var, | NA |
| 2316- | Api, | The interaction between apigenin and PKM2 restrains progression of colorectal cancer |
| - | in-vitro, | CRC, | LS174T | - | in-vitro, | CRC, | HCT8 | - | in-vivo, | CRC, | NA |
| 3383- | ART/DHA, | Dihydroartemisinin: A Potential Natural Anticancer Drug |
| - | Review, | Var, | NA |
| 2323- | ART/DHA, | Dihydroartemisinin represses esophageal cancer glycolysis by down-regulating pyruvate kinase M2 |
| - | in-vitro, | ESCC, | Eca109 | - | in-vitro, | ESCC, | EC9706 |
| 2322- | ART/DHA, | Dihydroartemisinin Regulates Self-Renewal of Human Melanoma-Initiating Cells by Targeting PKM2/LDHARelated Glycolysis |
| - | in-vitro, | Melanoma, | NA |
| 2321- | ART/DHA, | Dihydroartemisinin mediating PKM2-caspase-8/3-GSDME axis for pyroptosis in esophageal squamous cell carcinoma |
| - | in-vitro, | ESCC, | Eca109 | - | in-vitro, | ESCC, | EC9706 |
| 2320- | ART/DHA, | Dihydroartemisinin Inhibits the Proliferation of Leukemia Cells K562 by Suppressing PKM2 and GLUT1 Mediated Aerobic Glycolysis |
| - | in-vitro, | AML, | K562 | - | in-vitro, | Liver, | HepG2 |
| 2324- | ART/DHA, | Research Progress of Warburg Effect in Hepatocellular Carcinoma |
| - | Review, | Var, | NA |
| 957- | ART/DHA, | Artemisinin inhibits the development of esophageal cancer by targeting HIF-1α to reduce glycolysis levels |
| - | in-vitro, | ESCC, | KYSE150 | - | in-vitro, | ESCC, | KYSE170 |
| 1176- | Ash, | Metabolic Alterations in Mammary Cancer Prevention by Withaferin A in a Clinically Relevant Mouse Model |
| - | in-vivo, | NA, | NA |
| 2388- | Ash, | Withaferin A decreases glycolytic reprogramming in breast cancer |
| - | in-vitro, | BC, | MDA-MB-231 | - | in-vitro, | BC, | MDA-MB-468 | - | in-vitro, | BC, | MCF-7 | - | in-vitro, | BC, | MDA-MB-453 |
| 2289- | Ba, | Rad, | Baicalein Inhibits the Progression and Promotes Radiosensitivity of Esophageal Squamous Cell Carcinoma by Targeting HIF-1A |
| - | in-vitro, | ESCC, | KYSE150 |
| 2293- | Ba, | Baicalein suppresses inflammation and attenuates acute lung injury by inhibiting glycolysis via HIF‑1α signaling |
| - | in-vitro, | Nor, | MH-S | - | in-vivo, | NA, | NA |
| 2297- | Ba, | Significance of flavonoids targeting PI3K/Akt/HIF-1α signaling pathway in therapy-resistant cancer cells – A potential contribution to the predictive, preventive, and personalized medicine |
| - | Review, | Var, | NA |
| 2290- | Ba, | Research Progress of Scutellaria baicalensis in the Treatment of Gastrointestinal Cancer |
| - | Review, | GI, | NA |
| 2291- | Ba, | BA, | Baicalein and Baicalin Promote Melanoma Apoptosis and Senescence via Metabolic Inhibition |
| - | in-vitro, | Melanoma, | SK-MEL-28 | - | in-vitro, | Melanoma, | A375 |
| 2391- | Ba, | Scutellaria baicalensis and its flavonoids in the treatment of digestive system tumors |
| - | Review, | GC, | NA |
| 2335- | BBR, | Chemoproteomics reveals berberine directly binds to PKM2 to inhibit the progression of colorectal cancer |
| - | in-vitro, | CRC, | HT29 | - | in-vitro, | CRC, | HCT116 | - | in-vivo, | NA, | NA |
| 2336- | BBR, | Berberine Targets PKM2 to Activate the t-PA-Induced Fibrinolytic System and Improves Thrombosis |
| - | in-vivo, | Nor, | NA |
| 2337- | BBR, | Berberine Inhibited the Proliferation of Cancer Cells by Suppressing the Activity of Tumor Pyruvate Kinase M2 |
| - | in-vitro, | CRC, | HCT116 | - | in-vitro, | Cerv, | HeLa |
| 2709- | BBR, | Berberine inhibits the glycolysis and proliferation of hepatocellular carcinoma cells by down-regulating HIF-1α |
| - | in-vitro, | HCC, | HepG2 |
| 2710- | BBR, | Berberine inhibits the Warburg effect through TET3/miR-145/HK2 pathways in ovarian cancer cells |
| - | in-vitro, | Ovarian, | SKOV3 |
| 2740- | BetA, | Effects and mechanisms of fatty acid metabolism-mediated glycolysis regulated by betulinic acid-loaded nanoliposomes in colorectal cancer |
| - | in-vitro, | CRC, | HCT116 |
| - | in-vitro, | Cerv, | SiHa |
| 2394- | CAP, | Capsaicin acts as a novel NRF2 agonist to suppress ethanol induced gastric mucosa oxidative damage by directly disrupting the KEAP1-NRF2 interaction |
| - | in-vitro, | Nor, | GES-1 |
| 2347- | CAP, | Capsaicin ameliorates inflammation in a TRPV1-independent mechanism by inhibiting PKM2-LDHA-mediated Warburg effect in sepsis |
| - | in-vivo, | Nor, | NA | - | in-vitro, | Nor, | RAW264.7 |
| 2348- | CAP, | Recent advances in analysis of capsaicin and its effects on metabolic pathways by mass spectrometry |
| - | Analysis, | Nor, | NA |
| 2349- | CAP, | The TRPV1-PKM2-SREBP1 axis maintains microglial lipid homeostasis in Alzheimer’s disease |
| - | in-vivo, | AD, | NA |
| 2393- | Cela, | Celastrol mitigates inflammation in sepsis by inhibiting the PKM2-dependent Warburg effect |
| - | in-vivo, | Sepsis, | NA | - | in-vitro, | Nor, | RAW264.7 |
| 2392- | Cela, | The role of natural products targeting macrophage polarization in sepsis-induced lung injury |
| - | Review, | Sepsis, | NA |
| 2398- | CGA, | Polyphenol-rich diet mediates interplay between macrophage-neutrophil and gut microbiota to alleviate intestinal inflammation |
| - | in-vivo, | Col, | NA |
| 1576- | Citrate, | Targeting citrate as a novel therapeutic strategy in cancer treatment |
| - | Review, | Var, | NA |
| 2312- | CUR, | Dual Role of Reactive Oxygen Species and their Application in Cancer Therapy |
| - | Review, | Var, | NA |
| 2304- | CUR, | Curcumin decreases Warburg effect in cancer cells by down-regulating pyruvate kinase M2 via mTOR-HIF1α inhibition |
| - | in-vitro, | Lung, | H1299 | - | in-vitro, | BC, | MCF-7 | - | in-vitro, | Cerv, | HeLa | - | in-vitro, | Pca, | PC3 | - | in-vitro, | Nor, | HEK293 |
| 2305- | CUR, | Mitochondrial targeting nano-curcumin for attenuation on PKM2 and FASN |
| - | in-vitro, | BC, | MCF-7 |
| 2307- | CUR, | Cell-Type Specific Metabolic Response of Cancer Cells to Curcumin |
| - | in-vitro, | Colon, | HT29 | - | in-vitro, | Laryn, | FaDu |
| 2308- | CUR, | Counteracting Action of Curcumin on High Glucose-Induced Chemoresistance in Hepatic Carcinoma Cells |
| - | in-vitro, | Liver, | HepG2 |
| 2352- | dietFMD, | Glucose restriction reverses the Warburg effect and modulates PKM2 and mTOR expression in breast cancer cell lines |
| - | in-vitro, | BC, | MDA-MB-231 | - | in-vitro, | BC, | MCF-7 |
| 2302- | EGCG, | Flavonoids Targeting HIF-1: Implications on Cancer Metabolism |
| - | Review, | Var, | NA |
| 2309- | EGCG, | Chemo, | Targeting Glycolysis with Epigallocatechin-3-Gallate Enhances the Efficacy of Chemotherapeutics in Pancreatic Cancer Cells and Xenografts |
| - | in-vitro, | PC, | MIA PaCa-2 | - | in-vitro, | Nor, | HPNE | - | in-vitro, | PC, | PANC1 | - | in-vivo, | NA, | NA |
| 2422- | EMD, | Anti-Cancer Effects of Emodin on HepG2 Cells as Revealed by 1H NMR Based Metabolic Profiling |
| - | in-vitro, | HCC, | HepG2 |
| 2345- | EMD, | Emodin ameliorates antioxidant capacity and exerts neuroprotective effect via PKM2-mediated Nrf2 transactivation |
| - | in-vitro, | AD, | PC12 |
| 1654- | FA, | Molecular mechanism of ferulic acid and its derivatives in tumor progression |
| - | Review, | Var, | NA |
| 2401- | Flav, | In vitro effects of some flavonoids and phenolic acids on human pyruvate kinase isoenzyme M2 |
| - | in-vitro, | Nor, | NA |
| 2313- | Flav, | Flavonoids against the Warburg phenotype—concepts of predictive, preventive and personalised medicine to cut the Gordian knot of cancer cell metabolism |
| - | Review, | Var, | NA |
| 2400- | HCAs, | The Mixture of Ferulic Acid and P-Coumaric Acid Suppresses Colorectal Cancer through lncRNA 495810/PKM2 Mediated Aerobic Glycolysis |
| - | in-vitro, | CRC, | NA | - | in-vivo, | CRC, | NA |
| 2407- | HCAs, | 2'-hydroxycinnamaldehyde inhibits cancer cell proliferation and tumor growth by targeting the pyruvate kinase M2 |
| - | in-vitro, | Pca, | DU145 | - | in-vitro, | Pca, | LNCaP |
| 2178- | itraC, | Itraconazole inhibits tumor growth via CEBPB-mediated glycolysis in colorectal cancer |
| - | in-vivo, | CRC, | HCT116 |
| 2390- | KaempF, | Kaempferol Can Reverse the 5-Fu Resistance of Colorectal Cancer Cells by Inhibiting PKM2-Mediated Glycolysis |
| - | in-vitro, | CRC, | HCT8 |
| 2351- | lamb, | Anti-Warburg effect via generation of ROS and inhibition of PKM2/β-catenin mediates apoptosis of lambertianic acid in prostate cancer cells |
| - | in-vitro, | Pca, | DU145 | - | in-vitro, | Pca, | PC3 |
| 2346- | LT, | Luteolin suppressed PKM2 and promoted autophagy for inducing the apoptosis of hepatocellular carcinoma cells |
| - | in-vitro, | HCC, | HepG2 |
| 2376- | MET, | Metformin Inhibits Epithelial-to-Mesenchymal Transition of Keloid Fibroblasts via the HIF-1α/PKM2 Signaling Pathway |
| - | in-vitro, | Nor, | NA |
| 2375- | MET, | Metformin inhibits gastric cancer via the inhibition of HIF1α/PKM2 signaling |
| - | in-vitro, | GC, | SGC-7901 |
| 2371- | MET, | The role of pyruvate kinase M2 in anticancer therapeutic treatments |
| - | Review, | Var, | NA |
| 2377- | MET, | Metformin Inhibits TGF-β1-Induced Epithelial-to-Mesenchymal Transition via PKM2 Relative-mTOR/p70s6k Signaling Pathway in Cervical Carcinoma Cells |
| - | in-vitro, | Cerv, | HeLa | - | in-vitro, | Cerv, | SiHa |
| 2378- | MET, | Metformin inhibits epithelial-mesenchymal transition of oral squamous cell carcinoma via the mTOR/HIF-1α/PKM2/STAT3 pathway |
| - | in-vitro, | SCC, | CAL27 | - | in-vivo, | NA, | NA |
| 2379- | MET, | Down‐regulation of PKM2 enhances anticancer efficiency of THP on bladder cancer |
| - | in-vitro, | Bladder, | T24/HTB-9 | - | in-vitro, | BC, | UMUC3 |
| 2374- | MET, | Metformin Induces Apoptosis and Downregulates Pyruvate Kinase M2 in Breast Cancer Cells Only When Grown in Nutrient-Poor Conditions |
| - | in-vitro, | BC, | MCF-7 | - | in-vitro, | BC, | SkBr3 | - | in-vitro, | BC, | MDA-MB-231 |
| 2384- | MET, | Integration of metabolomics and transcriptomics reveals metformin suppresses thyroid cancer progression via inhibiting glycolysis and restraining DNA replication |
| - | in-vitro, | Thyroid, | BCPAP | - | in-vivo, | NA, | NA | - | in-vitro, | Thyroid, | TPC-1 |
| 2385- | MET, | Metformin activates chaperone-mediated autophagy and improves disease pathologies in an Alzheimer disease mouse model |
| - | in-vitro, | AD, | H4 | - | in-vitro, | NA, | HEK293 | - | in-vivo, | NA, | NA | - | in-vitro, | NA, | SH-SY5Y |
| 2386- | MET, | Mechanisms of metformin inhibiting cancer invasion and migration |
| - | Review, | Var, | NA |
| 2387- | MET, | GEM, | Metformin Increases the Response of Cholangiocarcinoma Cells to Gemcitabine by Suppressing Pyruvate Kinase M2 to Activate Mitochondrial Apoptosis |
| - | in-vitro, | CCA, | HCC9810 |
| 2260- | MF, | Alternative magnetic field exposure suppresses tumor growth via metabolic reprogramming |
| - | in-vitro, | GBM, | U87MG | - | in-vitro, | GBM, | LN229 | - | in-vivo, | NA, | NA |
| 991- | OA, | Blockade of glycolysis-dependent contraction by oroxylin a via inhibition of lactate dehydrogenase-a in hepatic stellate cells |
| - | in-vivo, | NA, | NA | - | in-vivo, | Nor, | NA |
| 2396- | PACs, | PKM2 is the target of proanthocyanidin B2 during the inhibition of hepatocellular carcinoma |
| - | in-vitro, | HCC, | HCCLM3 | - | in-vitro, | HCC, | SMMC-7721 cell | - | in-vitro, | HCC, | Bel-7402 | - | in-vitro, | HCC, | HUH7 | - | in-vitro, | HCC, | HepG2 | - | in-vitro, | Nor, | L02 |
| 2429- | PB, | Impact of butyrate on PKM2 and HSP90β expression in human colon tissues of different transformation stages: a comparison of gene and protein data |
| - | in-vitro, | Colon, | NA |
| 1672- | PBG, | The Potential Use of Propolis as an Adjunctive Therapy in Breast Cancers |
| - | Review, | BC, | NA |
| 1661- | PBG, | Propolis: a natural compound with potential as an adjuvant in cancer therapy - a review of signaling pathways |
| - | Review, | Var, | NA |
| 1664- | PBG, | Anticancer Activity of Propolis and Its Compounds |
| - | Review, | Var, | NA |
| 1231- | PBG, | Caffeic acid phenethyl ester inhibits MDA-MB-231 cell proliferation in inflammatory microenvironment by suppressing glycolysis and lipid metabolism |
| - | in-vitro, | BC, | MDA-MB-231 |
| - | in-vitro, | HCC, | HepG2 |
| 2381- | PBG, | Chinese Poplar Propolis Inhibits MDA-MB-231 Cell Proliferation in an Inflammatory Microenvironment by Targeting Enzymes of the Glycolytic Pathway |
| - | in-vitro, | BC, | MDA-MB-231 |
| 2380- | PBG, | Potential Strategies for Overcoming Drug Resistance Pathways Using Propolis and Its Polyphenolic/Flavonoid Compounds in Combination with Chemotherapy and Radiotherapy |
| - | Review, | Var, | NA |
| 2409- | PTS, | Pterostilbene Induces Pyroptosis in Breast Cancer Cells through Pyruvate Kinase 2/Caspase-8/Gasdermin C Signaling Pathway |
| - | in-vitro, | BC, | EMT6 | - | in-vitro, | BC, | 4T1 | - | in-vitro, | Nor, | HC11 |
| 2408- | PTS, | Pterostilbene suppresses the growth of esophageal squamous cell carcinoma by inhibiting glycolysis and PKM2/STAT3/c-MYC signaling pathway |
| - | in-vitro, | ESCC, | NA |
| 910- | QC, | The Anti-Cancer Effect of Quercetin: Molecular Implications in Cancer Metabolism |
| 2343- | QC, | Pharmacological Activity of Quercetin: An Updated Review |
| - | Review, | Nor, | NA |
| 2338- | QC, | Quercetin: A Flavonoid with Potential for Treating Acute Lung Injury |
| - | Review, | Nor, | NA |
| 2339- | QC, | Quercetin protects against LPS-induced lung injury in mice via SIRT1-mediated suppression of PKM2 nuclear accumulation |
| - | in-vivo, | Nor, | NA |
| 2340- | QC, | Oral Squamous Cell Carcinoma Cells with Acquired Resistance to Erlotinib Are Sensitive to Anti-Cancer Effect of Quercetin via Pyruvate Kinase M2 (PKM2) |
| - | in-vitro, | OS, | NA |
| 2341- | QC, | Quercetin suppresses the mobility of breast cancer by suppressing glycolysis through Akt-mTOR pathway mediated autophagy induction |
| - | in-vitro, | BC, | MCF-7 | - | in-vitro, | BC, | MDA-MB-231 | - | in-vivo, | NA, | NA |
| 2344- | QC, | Quercetin: A natural solution with the potential to combat liver fibrosis |
| - | Review, | Nor, | NA |
| 2334- | RES, | Glut 1 in Cancer Cells and the Inhibitory Action of Resveratrol as A Potential Therapeutic Strategy |
| - | Review, | Var, | NA |
| 2332- | RES, | Resveratrol’s Anti-Cancer Effects through the Modulation of Tumor Glucose Metabolism |
| - | Review, | Var, | NA |
| 2330- | RES, | Resveratrol Induces Cancer Cell Apoptosis through MiR-326/PKM2-Mediated ER Stress and Mitochondrial Fission |
| - | in-vitro, | CRC, | DLD1 | - | in-vitro, | Cerv, | HeLa | - | in-vitro, | BC, | MCF-7 |
| 2329- | RES, | Resveratrol induces apoptosis in human melanoma cell through negatively regulating Erk/PKM2/Bcl-2 axis |
| - | in-vitro, | Melanoma, | A375 |
| 2328- | RES, | Resveratrol Inhibits Cancer Cell Metabolism by Down Regulating Pyruvate Kinase M2 via Inhibition of Mammalian Target of Rapamycin |
| - | in-vitro, | Cerv, | HeLa | - | in-vitro, | Liver, | HepG2 | - | in-vitro, | BC, | MCF-7 |
| 2439- | RES, | By reducing hexokinase 2, resveratrol induces apoptosis in HCC cells addicted to aerobic glycolysis and inhibits tumor growth in mice |
| - | in-vitro, | HCC, | HCCLM3 | - | in-vitro, | Nor, | L02 | - | in-vitro, | HCC, | SMMC-7721 cell | - | in-vitro, | HCC, | Bel-7402 | - | in-vitro, | HCC, | HUH7 |
| 2404- | SFN, | Prostate cancer chemoprevention by sulforaphane in a preclinical mouse model is associated with inhibition of fatty acid metabolism |
| - | in-vitro, | Pca, | LNCaP | - | in-vitro, | Pca, | 22Rv1 | - | in-vivo, | NA, | NA |
| 2405- | SFN, | Sulforaphane Targets the TBX15/KIF2C Pathway to Repress Glycolysis and Cell Proliferation in Gastric Carcinoma Cells |
| - | in-vitro, | GC, | SGC-7901 | - | in-vitro, | GC, | BGC-823 |
| 2403- | SFN, | Reversal of the Warburg phenomenon in chemoprevention of prostate cancer by sulforaphane |
| - | in-vitro, | Pca, | LNCaP | - | in-vitro, | Pca, | 22Rv1 | - | in-vitro, | Pca, | PC3 | - | in-vivo, | NA, | NA |
| 2406- | SFN, | Sulforaphane and Its Protective Role in Prostate Cancer: A Mechanistic Approach |
| - | Review, | Pca, | NA |
| 2445- | SFN, | Sulforaphane-Induced Cell Cycle Arrest and Senescence are accompanied by DNA Hypomethylation and Changes in microRNA Profile in Breast Cancer Cells |
| - | in-vitro, | BC, | MCF-7 | - | in-vitro, | BC, | MDA-MB-231 | - | in-vitro, | BC, | SkBr3 |
| 2306- | SIL, | CUR, | RES, | EA, | Identification of Natural Compounds as Inhibitors of Pyruvate Kinase M2 for Cancer Treatment |
| - | in-vitro, | BC, | MDA-MB-231 |
| 2410- | SIL, | Autophagy activated by silibinin contributes to glioma cell death via induction of oxidative stress-mediated BNIP3-dependent nuclear translocation of AIF |
| - | in-vitro, | GBM, | U87MG | - | in-vitro, | GBM, | U251 | - | in-vivo, | NA, | NA |
| 2359- | SK, | Regulating lactate-related immunometabolism and EMT reversal for colorectal cancer liver metastases using shikonin targeted delivery |
| - | in-vivo, | Liver, | NA |
| 2420- | SK, | Pyruvate kinase M2 regulates mitochondrial homeostasis in cisplatin-induced acute kidney injury |
| - | in-vivo, | AKI, | NA |
| 2419- | SK, | Regulation of glycolysis and the Warburg effect in wound healing |
| - | in-vivo, | Nor, | NA |
| 2418- | SK, | Experimental Study of Hepatocellular Carcinoma Treatment by Shikonin Through Regulating PKM2 |
| - | in-vitro, | HCC, | SMMC-7721 cell | - | in-vitro, | HCC, | HUH7 | - | in-vitro, | HCC, | HepG2 |
| 2416- | SK, | Shikonin induces cell death by inhibiting glycolysis in human testicular cancer I-10 and seminoma TCAM-2 cells |
| - | in-vitro, | Testi, | TCAM-2 |
| 2415- | SK, | Shikonin induces programmed death of fibroblast synovial cells in rheumatoid arthritis by inhibiting energy pathways |
| - | in-vivo, | Arthritis, | NA |
| 2354- | SK, | PKM2-dependent glycolysis promotes NLRP3 and AIM2 inflammasome activation |
| - | in-vivo, | Sepsis, | NA |
| 2355- | SK, | Pharmacological properties and derivatives of shikonin-A review in recent years |
| - | Review, | Var, | NA |
| 2370- | SK, | The role of pyruvate kinase M2 in anticancer therapeutic treatments |
| - | Review, | Var, | NA |
| 2356- | SK, | ESM1 enhances fatty acid synthesis and vascular mimicry in ovarian cancer by utilizing the PKM2-dependent warburg effect within the hypoxic tumor microenvironment |
| - | in-vitro, | Ovarian, | CaOV3 | - | in-vitro, | Ovarian, | OV90 | - | in-vivo, | NA, | NA |
| 2357- | SK, | GTPBP4 promotes hepatocellular carcinoma progression and metastasis via the PKM2 dependent glucose metabolism |
| - | Study, | HCC, | NA | - | in-vivo, | NA, | NA |
| 2358- | SK, | SIRT1 improves lactate homeostasis in the brain to alleviate parkinsonism via deacetylation and inhibition of PKM2 |
| - | in-vivo, | Park, | NA |
| 2360- | SK, | Shikonin inhibits growth, invasion and glycolysis of nasopharyngeal carcinoma cells through inactivating the phosphatidylinositol 3 kinase/AKT signal pathway |
| - | in-vitro, | NPC, | HONE1 | - | in-vitro, | NPC, | SUNE-1 |
| 2361- | SK, | Natural shikonin and acetyl-shikonin improve intestinal microbial and protein composition to alleviate colitis-associated colorectal cancer |
| - | in-vivo, | CRC, | NA |
| 2362- | SK, | RIP1 and RIP3 contribute to shikonin-induced glycolysis suppression in glioma cells via increase of intracellular hydrogen peroxide |
| - | in-vitro, | GBM, | U87MG | - | in-vivo, | GBM, | NA | - | in-vitro, | GBM, | U251 |
| 2363- | SK, | Inhibition of PKM2 by shikonin impedes TGF-β1 expression by repressing histone lactylation to alleviate renal fibrosis |
| - | in-vivo, | CKD, | NA |
| 2364- | SK, | Pyruvate Kinase M2 Mediates Glycolysis Contributes to Psoriasis by Promoting Keratinocyte Proliferation |
| - | in-vivo, | PSA, | NA |
| 2191- | SK, | Shikonin Suppresses Skin Carcinogenesis via Inhibiting Cell Proliferation |
| - | in-vitro, | Melanoma, | NA |
| 2200- | SK, | Shikonin inhibits the growth of anaplastic thyroid carcinoma cells by promoting ferroptosis and inhibiting glycolysis |
| - | in-vitro, | Thyroid, | CAL-62 | - | in-vitro, | Thyroid, | 8505C |
| 2197- | SK, | Shikonin derivatives for cancer prevention and therapy |
| - | Review, | Var, | NA |
| 2196- | SK, | Research progress in mechanism of anticancer action of shikonin targeting reactive oxygen species |
| - | Review, | Var, | NA |
| 2194- | SK, | Efficacy of Shikonin against Esophageal Cancer Cells and its possible mechanisms in vitro and in vivo |
| - | in-vitro, | ESCC, | Eca109 | - | in-vitro, | ESCC, | EC9706 | - | in-vivo, | NA, | NA |
| 2192- | SK, | Shikonin Inhibits Tumor Growth of ESCC by suppressing PKM2 mediated Aerobic Glycolysis and STAT3 Phosphorylation |
| - | in-vitro, | ESCC, | KYSE-510 | - | in-vitro, | ESCC, | Eca109 | - | in-vivo, | NA, | NA |
| 2190- | SK, | Shikonin exerts antitumor activity by causing mitochondrial dysfunction in hepatocellular carcinoma through PKM2-AMPK-PGC1α signaling pathway |
| - | in-vitro, | HCC, | HCCLM3 |
| 2189- | SK, | PKM2 inhibitor shikonin suppresses TPA-induced mitochondrial malfunction and proliferation of skin epidermal JB6 cells |
| - | in-vitro, | Melanoma, | NA |
| 2187- | SK, | VitK3, | Shikonin, vitamin K3 and vitamin K5 inhibit multiple glycolytic enzymes in MCF-7 cells |
| - | in-vitro, | BC, | MCF-7 |
| 2186- | SK, | Shikonin differentially regulates glucose metabolism via PKM2 and HIF1α to overcome apoptosis in a refractory HCC cell line |
| - | in-vitro, | HCC, | HepG2 | - | in-vitro, | HCC, | HCCLM3 |
| 2185- | SK, | Shikonin Inhibits Tumor Growth in Mice by Suppressing Pyruvate Kinase M2-mediated Aerobic Glycolysis |
| - | in-vitro, | Lung, | LLC1 | - | in-vitro, | Melanoma, | B16-BL6 | - | in-vivo, | NA, | NA |
| 2184- | SK, | Cisplatin, | PKM2 Inhibitor Shikonin Overcomes the Cisplatin Resistance in Bladder Cancer by Inducing Necroptosis |
| - | in-vitro, | CRC, | T24/HTB-9 |
| 2182- | SK, | Cisplatin, | Shikonin inhibited glycolysis and sensitized cisplatin treatment in non-small cell lung cancer cells via the exosomal pyruvate kinase M2 pathway |
| - | in-vitro, | Lung, | A549 | - | in-vitro, | Lung, | PC9 | - | in-vivo, | NA, | NA |
| 2181- | SK, | Shikonin and its analogs inhibit cancer cell glycolysis by targeting tumor pyruvate kinase-M2 |
| - | in-vitro, | BC, | MCF-7 | - | in-vitro, | Lung, | A549 | - | in-vitro, | Cerv, | HeLa |
| 2223- | SK, | Non-metabolic enzyme function of PKM2 in hepatocellular carcinoma: A review |
| - | in-vitro, | Var, | NA |
| 3045- | SK, | Cutting off the fuel supply to calcium pumps in pancreatic cancer cells: role of pyruvate kinase-M2 (PKM2) |
| - | in-vitro, | PC, | MIA PaCa-2 |
| 3041- | SK, | Promising Nanomedicines of Shikonin for Cancer Therapy |
| - | Review, | Var, | NA |
| 3040- | SK, | Pharmacological Properties of Shikonin – A Review of Literature since 2002 |
| - | Review, | Var, | NA | - | Review, | IBD, | NA | - | Review, | Stroke, | NA |
| 2470- | SK, | PKM2/PDK1 dual-targeted shikonin derivatives restore the sensitivity of EGFR-mutated NSCLC cells to gefitinib by remodeling glucose metabolism |
| - | in-vitro, | Lung, | H1299 |
| 1050- | SK, | Shikonin improves the effectiveness of PD-1 blockade in colorectal cancer by enhancing immunogenicity via Hsp70 upregulation |
| - | in-vitro, | Colon, | CT26 |
| 1049- | SK, | Shikonin inhibits immune checkpoint PD-L1 expression on macrophage in sepsis by modulating PKM2 |
| - | in-vivo, | NA, | NA |
| 2373- | TMZ, | The role of pyruvate kinase M2 in anticancer therapeutic treatments |
| - | Review, | Var, | NA |
| 2353- | TQ, | The effects of thymoquinone on pancreatic cancer: Evidence from preclinical studies |
| - | Review, | PC, | NA |
| 3425- | TQ, | Advances in research on the relationship between thymoquinone and pancreatic cancer |
| 3431- | TQ, | PI3K-AKT Pathway Modulation by Thymoquinone Limits Tumor Growth and Glycolytic Metabolism in Colorectal Cancer |
| - | in-vitro, | CRC, | HCT116 | - | in-vitro, | CRC, | SW48 |
| 2413- | TTT, | Tumor treating fields (TTFields) impairs aberrant glycolysis in glioblastoma as evaluated by [18F]DASA-23, a non-invasive probe of pyruvate kinase M2 (PKM2) expression |
| - | in-vitro, | GBM, | U87MG |
| 2350- | UA, | Ursolic acid-mediated changes in glycolytic pathway promote cytotoxic autophagy and apoptosis in phenotypically different breast cancer cells |
| - | in-vitro, | BC, | MCF-7 | - | in-vitro, | BC, | MDA-MB-231 |
| 2411- | UA, | Ursolic acid in health and disease |
| - | Review, | Var, | NA |
| 3136- | VitC, | Vitamin C uncouples the Warburg metabolic switch in KRAS mutant colon cancer |
| - | in-vitro, | Colon, | SW48 | - | in-vitro, | Colon, | LoVo |
| 3141- | VitC, | High-dose Vitamin C inhibits PD-L1 expression by activating AMPK in colorectal cancer |
| - | in-vitro, | CRC, | HCT116 |
| 3145- | VitC, | Vitamin C inhibits the growth of colorectal cancer cell HCT116 and reverses the glucose‐induced oncogenic effect by downregulating the Warburg effect |
| - | in-vitro, | CRC, | HCT116 |
| 2369- | VitD3, | Long Non-coding RNA MEG3 Activated by Vitamin D Suppresses Glycolysis in Colorectal Cancer via Promoting c-Myc Degradation |
| - | in-vitro, | CRC, | DLD1 | - | in-vitro, | CRC, | RKO |
| 2365- | VitD3, | Vitamin D Affects the Warburg Effect and Stemness Maintenance of Non- Small-Cell Lung Cancer Cells by Regulating the PI3K/AKT/mTOR Signaling Pathway |
| - | in-vitro, | Lung, | A549 | - | in-vitro, | Lung, | H1975 | - | in-vivo, | NA, | NA |
| 2428- | VitK3, | Vitamin K3 and K5 are inhibitors of tumor pyruvate kinase M2 |
| - | Study, | Var, | NA |
| 2372- | VitK3, | The role of pyruvate kinase M2 in anticancer therapeutic treatments |
| - | Review, | Var, | NA |
| 2397- | Wor, | Phytochemicals targeting glycolysis in colorectal cancer therapy: effects and mechanisms of action |
| - | Review, | Var, | NA |
| 2414- | β‐Ele, | Beta‐elemene inhibits breast cancer metastasis through blocking pyruvate kinase M2 dimerization and nuclear translocation |
| - | in-vitro, | BC, | MDA-MB-231 | - | in-vitro, | BC, | MCF-7 | - | in-vivo, | NA, | NA |
| 2425- | γ-Toc, | Anticancer Effects of γ-Tocotrienol Are Associated with a Suppression in Aerobic Glycolysis |
| - | in-vitro, | NA, | MCF-7 | - | in-vivo, | NA, | NA |
Query results interpretion may depend on "conditions" listed in the research papers. Such Conditions may include : -low or high Dose -format for product, such as nano of lipid formations -different cell line effects -synergies with other products -if effect was for normal or cancerous cells
Filter Conditions: Pro/AntiFlg:% IllCat:% CanType:% Cells:% prod#:% Target#:772 State#:% Dir#:1
wNotes=0 sortOrder:rid,rpid