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Translational and HIF-1α-Dependent Metabolic Reprogramming Underpin Metabolic Plasticity and Responses to Kinase Inhibitors and Biguanides

Hulea, L., Gravel, S., Morita, M., Cargnello, M., Uchenunu, O., Im, Y. K., Lehuédé, C., Ma, E. H., Leibovitch, M., McLaughlan, S., et al. (2018) · Cell Metabolism · doi:10.1016/j.cmet.2018.09.001 · Cited by 87 · see citing works

Pan-Cancer Metabolic Signature Predicts Co-Dependency on Glutaminase and De Novo Glutathione Synthesis Linked to a High-Mesenchymal Cell State

Daemen, A., Liu, B., Song, K., Kwong, M., Gao, M., Hong, R., Nannini, M., Peterson, D., Liederer, B. M., de la Cruz, C., et al. (2018) · Cell Metabolism · doi:10.1016/j.cmet.2018.06.003 · Cited by 89 · see citing works

Rationale for LDH-targeted cancer immunotherapy

Miholjcic, T. B. S., Halse, H. M., Bonvalet, M., Bigorgne, A., Rouanne, M., Dercle, L., Shankar, V., & Marabelle, A. (2022) · European Journal of Cancer · doi:10.1016/j.ejca.2022.11.032 · Cited by 89 · see citing works

Tyrosine Kinase Signaling in Cancer Metabolism: PKM2 Paradox in the Warburg Effect

Wiese, E. K., & Hitosugi, T. (2018) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2018.00079 · Cited by 82 · see citing works

Targeting L-Lactate Metabolism to Overcome Resistance to Immune Therapy of Melanoma and Other Tumor Entities

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Targeting lactate dehydrogenase a improves radiotherapy efficacy in non-small cell lung cancer: from bedside to bench

Yang, Y., Chong, Y., Chen, M., Dai, W., Zhou, X., Ji, Y., Qiu, G., & Du, X. (2021) · Journal of Translational Medicine · doi:10.1186/s12967-021-02825-2 · Cited by 81 · see citing works

Lactate production is a prioritized feature of adipocyte metabolism

Krycer, J. R., Quek, L., Francis, D., Fazakerley, D. J., Elkington, S. D., Díaz‐Vegas, A., Cooke, K. C., Weiss, F. C., Duan, X., Kurdyukov, S., et al. (2019) · Journal of Biological Chemistry · doi:10.1074/jbc.ra119.011178 · Cited by 71 · see citing works

Mitochondrial Protein UQCRC1 is Oncogenic and a Potential Therapeutic Target for Pancreatic Cancer

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Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties

Rai, G., Urban, D. J., Mott, B. T., Hu, X., Yang, S., Benavides, G. A., Johnson, M. S., Squadrito, G. L., Brimacombe, K. R., Lee, T. D., et al. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00916 · Cited by 64 · see citing works

The roles of intratumour heterogeneity in the biology and treatment of pancreatic ductal adenocarcinoma

Evan, T., Wang, V. M.-Y., & Behrens, A. (2022) · Oncogene · doi:10.1038/s41388-022-02448-x · Cited by 62 · see citing works

Myoferlin controls mitochondrial structure and activity in pancreatic ductal adenocarcinoma, and affects tumor aggressiveness

Rademaker, G., Hennequière, V., Brohée, L., Nokin, M., Lovinfosse, P., Durieux, F., Gofflot, S., Bellier, J., Costanza, B., Herfs, M. F., et al. (2018) · Oncogene · doi:10.1038/s41388-018-0287-z · Cited by 64 · see citing works

Targeting lactate dehydrogenase B-dependent mitochondrial metabolism affects tumor initiating cells and inhibits tumorigenesis of non-small cell lung cancer by inducing mtDNA damage

Deng, H., Gao, Y., Trappetti, V., Hertig, D., Karatkevich, D., Losmanová, T., Urzì, C., Ge, H., Geest, G. A., Bruggmann, R., et al. (2022) · Cellular and Molecular Life Sciences · doi:10.1007/s00018-022-04453-5 · Cited by 62 · see citing works

Targeting cancer metabolism to develop human lactate dehydrogenase (hLDH)5 inhibitors

Zhang, S., He, Y., & Tam, K. Y. (2018) · Drug Discovery Today · doi:10.1016/j.drudis.2018.05.014 · Cited by 62 · see citing works

Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice

Purkey, H. E., Robarge, K. D., Chen, J., Chen, Z., Corson, L., Ding, C. Z., DiPasquale, A. G., Dragovich, P. S., Eigenbrot, C. W., Evangelista, M., et al. (2016) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.6b00190 · Cited by 60 · see citing works

Structural and Functional Regulation of Lactate dehydrogenase-A in Cancer

Woodford, M. R., Chen, V. Z., Backe, S. J., Bratslavsky, G., & Mollapour, M. (2020) · Future Medicinal Chemistry · doi:10.4155/fmc-2019-0287 · Cited by 59 · see citing works

Tumor lactic acid: a potential target for cancer therapy

Byun, J. (2023) · Archives of Pharmacal Research · doi:10.1007/s12272-023-01431-8 · Cited by 58 · see citing works

Machilin A Inhibits Tumor Growth and Macrophage M2 Polarization Through the Reduction of Lactic Acid

Chung, T., Kim, E.-Y., Han, C. W., Park, S. Y., Jeong, M. S., Yoon, D., Choi, H., Jin, L., Park, M.-J., Kwon, Y. J., et al. (2019) · Cancers · doi:10.3390/cancers11070963 · Cited by 57 · see citing works

Transcriptional regulation and post-translational modifications in the glycolytic pathway for targeted cancer therapy

Ni, X., Lu, C., Xu, G.-Q., & Ma, J. (2024) · Acta Pharmacologica Sinica · doi:10.1038/s41401-024-01264-1 · Cited by 56 · see citing works

Palmitoylation alters LDHA activity and pancreatic cancer response to chemotherapy

Chen, L., Xing, X., Zhu, Y., Chen, Y., Pei, H., Song, Q., Li, J., & Zhang, P. (2024) · Cancer Letters · doi:10.1016/j.canlet.2024.216696 · Cited by 55 · see citing works

NAT10/ac4C/JunB facilitates TNBC malignant progression and immunosuppression by driving glycolysis addiction

Li, G., Ma, X., Sui, S., Chen, Y., Li, H., Liu, L., Zhang, X., Zhang, L., Hao, Y., Yang, Z., et al. (2024) · Journal of Experimental & Clinical Cancer Research · doi:10.1186/s13046-024-03200-x · Cited by 54 · see citing works

Lactate: a rising star in tumors and inflammation

Liu, H., Pan, M., Liu, M., Zeng, L., Li, Y., Huang, Z., Guo, C., & Wang, H. (2024) · Frontiers in Immunology · doi:10.3389/fimmu.2024.1496390 · Cited by 53 · see citing works

Inhibition of glycolysis by targeting lactate dehydrogenase A facilitates hyaluronan synthase 2 synthesis in synovial fibroblasts of temporomandibular joint osteoarthritis

Li, H. M., Guo, H. L., Xu, C., Liu, L., Hu, S. Y., Hu, Z. H., Jiang, H., He, Y., Li, Y. J., Ke, J., et al. (2020) · Bone · doi:10.1016/j.bone.2020.115584 · Cited by 52 · see citing works

Metabolic Reprogramming and Renal Fibrosis

Zhu, X., Jiang, L., Long, M., Wei, X. S., Hou, Y., & Du, Y. (2021) · Frontiers in Medicine · doi:10.3389/fmed.2021.746920 · Cited by 53 · see citing works

Opa1 and Drp1 reciprocally regulate cristae morphology, ETC function, and NAD+ regeneration in KRas-mutant lung adenocarcinoma

Sessions, D. T., Kim, K., Kashatus, J. A., Churchill, N., Park, K.-S., Mayo, M. W., Sesaki, H., & Kashatus, D. F. (2022) · Cell Reports · doi:10.1016/j.celrep.2022.111818 · Cited by 49 · see citing works

Dual Enzyme-Driven Cascade Reactions Modulate Immunosuppressive Tumor Microenvironment for Catalytic Therapy and Immune Activation

Liu, H., Jiang, S., Li, M., Shan, L., Wu, J., He, T., Wang, D., Lin, J., & Huang, P. (2024) · ACS Nano · doi:10.1021/acsnano.4c07374 · Cited by 46 · see citing works

Pathogenesis and therapeutic targeting of aberrant MYC expression in haematological cancers

Schick, M., Habringer, S., Nilsson, J. A., & Keller, U. B. (2017) · British Journal of Haematology · doi:10.1111/bjh.14917 · Cited by 46 · see citing works

Cryptotanshinone suppresses ovarian cancer via simultaneous inhibition of glycolysis and oxidative phosphorylation

Wang, T., Zhang, M., Khan, M. T., Li, J., Wu, X. J., Ma, T., & Li, Y. (2023) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2023.115956 · Cited by 45 · see citing works

Regulatory T Cell Metabolism: A Promising Therapeutic Target for Cancer Treatment?

Kim, J., Li, J., Wei, J., & Lim, S. A. (2025) · Immune Network · doi:10.4110/in.2025.25.e13 · Cited by 45 · see citing works

Metabolic Plasiticy in Cancers—Distinct Role of Glycolytic Enzymes GPI, LDHs or Membrane Transporters MCTs

Ždralević, M., Marchiq, I., de Padua, M. M. C., Parks, S. K., & Pouysségur, J. (2017) · Frontiers in Oncology · doi:10.3389/fonc.2017.00313 · Cited by 43 · see citing works

Lactate dehydrogenase and glycerol-3-phosphate dehydrogenase cooperatively regulate growth and carbohydrate metabolism during Drosophila melanogaster larval development

Li, H., Rai, M., Buddika, K., Sterrett, M. C., Luhur, A., Mahmoudzadeh, N. H., Julick, C. R., Pletcher, R. C., Chawla, G., Gosney, C. J., et al. (2019) · Development · doi:10.1242/dev.175315 · Cited by 41 · see citing works

ONC212 is a Novel Mitocan Acting Synergistically with Glycolysis Inhibition in Pancreatic Cancer

Ferrarini, I., Louie, A. D., Zhou, L., & El‐Deiry, W. S. (2021) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-20-0962 · Cited by 44 · see citing works

The impact of non-genetic heterogeneity on cancer cell death

Inde, Z., & Dixon, S. J. (2017) · Critical Reviews in Biochemistry and Molecular Biology · doi:10.1080/10409238.2017.1412395 · Cited by 40 · see citing works

Development of novel human lactate dehydrogenase A inhibitors: High-throughput screening, synthesis, and biological evaluations

Zhou, Y., Tao, P., Wang, M., Xu, P., Lü, W., Lei, P., & You, Q. (2019) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2019.05.033 · Cited by 43 · see citing works

Structural Evidence for Isoform-Selective Allosteric Inhibition of Lactate Dehydrogenase A

Friberg, A., Rehwinkel, H., Nguyen, D., Pütter, V., Quanz, M., Weiske, J., Eberspächer, U., Heisler, I., & Langer, G. (2020) · ACS Omega · doi:10.1021/acsomega.0c00715 · Cited by 43 · see citing works

Discovery of the First Lactate Dehydrogenase Proteolysis Targeting Chimera Degrader for the Treatment of Pancreatic Cancer

Sun, N., Kabir, M., Lee, Y., Xie, L., Hu, X., Velez, J., Chen, X., Kanıskan, H. Ü., & Jin, J. J. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c01505 · Cited by 43 · see citing works

Human lung fibroblast-to-myofibroblast transformation is not driven by an LDH5-dependent metabolic shift towards aerobic glycolysis

Schruf, E., Schroeder, V., Kuttruff, C. A., Weigle, S., Krell, M., Benz, M., Bretschneider, T., Holweg, A., Schuler, M. J., Frick, M., et al. (2019) · Respiratory Research · doi:10.1186/s12931-019-1058-2 · Cited by 41 · see citing works

Chiral Pyridine-3,5-bis- (L-phenylalaninyl-L-leucinyl) Schiff Base Peptides as Potential Anticancer Agents: Design, Synthesis, and Molecular Docking Studies Targeting Lactate Dehydrogenase-A

Amr, A. E. E., Mageid, R. E. A., El-Naggar, M. H., Naglah, A. M., Nossier, E. S., & Elsayed, E. A. (2020) · Molecules · doi:10.3390/molecules25051096 · Cited by 41 · see citing works

Discovery of human lactate dehydrogenase A (LDHA) inhibitors as anticancer agents to inhibit the proliferation of MG-63 osteosarcoma cells

Fang, A., Zhang, Q., Fan, H., Zhou, Y., Yao, Y., Zhang, Y., & Huang, X. (2017) · MedChemComm · doi:10.1039/c7md00222j · Cited by 40 · see citing works

Cytosolic ME1 integrated with mitochondrial IDH2 supports tumor growth and metastasis

Shao, C., Lu, W., Du, Y., Yan, W., Bao, Q., Tian, Y., Wang, G., Ye, H., & Hao, H. (2020) · Redox Biology · doi:10.1016/j.redox.2020.101685 · Cited by 40 · see citing works

Development of a novel lactate dehydrogenase A inhibitor with potent antitumor activity and immune activation

Du, M., Yu, T., Zhan, Q., Li, H., Zou, Y., Geng, M., Meng, T., & Xie, Z. (2022) · Cancer Science · doi:10.1111/cas.15468 · Cited by 38 · see citing works

Metabolic reprogramming driven by METTL1-mediated tRNA m7G modification promotes acquired anlotinib resistance in oral squamous cell carcinoma

Chen, J., Zhou, Q., Li, S., Ling, R., Zhao, Y., Chen, D., Wang, A., & Cao, Y. (2024) · Translational research · doi:10.1016/j.trsl.2024.01.009 · Cited by 39 · see citing works

The biological role of metabolic reprogramming in pancreatic cancer

Suzuki, T., Otsuka, M., Seimiya, T., Iwata, T., Kishikawa, T., & Koike, K. (2020) · MedComm · doi:10.1002/mco2.37 · Cited by 37 · see citing works

Targeting glucose metabolism to develop anticancer treatments and therapeutic patents

Zhou, Y., Guo, Y., & Tam, K. Y. (2022) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2022.2027912 · Cited by 38 · see citing works

Lactate-dependent transcriptional regulation controls mammalian eye morphogenesis

Takata, N., Miska, J. M., Morgan, M. A., Patel, P. A., Billingham, L. K., Joshi, N., Schipma, M. J., Dumar, Z. J., Joshi, N., Misharin, A. V., et al. (2023) · Nature Communications · doi:10.1038/s41467-023-39672-2 · Cited by 38 · see citing works

Glucometabolic Reprogramming in the Hepatocellular Carcinoma Microenvironment: Cause and Effect

Tian, H., Zhu, X., Lv, Y., Jiao, Y., & Wang, G. (2020) · Cancer Management and Research · doi:10.2147/cmar.s258196 · Cited by 36 · see citing works

Identification of novel mRNA isoforms associated with meat tenderness using RNA sequencing data in beef cattle

Muniz, M. M. M., Fonseca, L. F. S., Silva, D. B. D. S., de Oliveira, H. R., Baldi, F. S., Chardulo, A. L., Ferro, J. A., Cánovas, Á., & de Albuquerque, L. G. (2020) · Meat Science · doi:10.1016/j.meatsci.2020.108378 · Cited by 35 · see citing works

Identification and Characterization of IMD-0354 as a Glutamine Carrier Protein Inhibitor in Melanoma

Feng, Y., Pathria, G., Heynen‐Genel, S., Jackson, M., James, B. P., Yin, J., Scott, D. A., & Ronai, Z. A. (2021) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-20-0354 · Cited by 35 · see citing works

Oncogenic KRAS triggers metabolic reprogramming in pancreatic ductal adenocarcinoma

Shen, X., Niu, N., & Xue, J. (2022) · Journal of Translational Internal Medicine · doi:10.2478/jtim-2022-0022 · Cited by 34 · see citing works

Mechanical Force Modulates Alveolar Bone Marrow Mesenchymal Cells Characteristics for Bone Remodeling during Orthodontic Tooth Movement through Lactate Production

Zhai, M., Cui, S., Li, L., Chen, C., Zhang, Z., Liu, J., & Wei, F. (2022) · Cells · doi:10.3390/cells11233724 · Cited by 34 · see citing works

Lactate dehydrogenase A inhibition prevents RANKL-induced osteoclastogenesis by reducing enhanced glycolysis

Nishioku, T., Anzai, R., Hiramatsu, S., Terazono, A., Nakao, M., & Moriyama, M. (2023) · Journal of Pharmacological Sciences · doi:10.1016/j.jphs.2023.09.005 · Cited by 34 · see citing works

Lactic acid in macrophage polarization: A factor in carcinogenesis and a promising target for cancer therapy

Ajam-Hosseini, M., Heydari, R., Rasouli, M., Akhoondi, F., Hanjani, N. A., Bekeschus, S., & Doroudian, M. (2024) · Biochemical Pharmacology · doi:10.1016/j.bcp.2024.116098 · Cited by 34 · see citing works

G6PD-NF-κB-HGF Signal in Gastric Cancer-Associated Mesenchymal Stem Cells Promotes the Proliferation and Metastasis of Gastric Cancer Cells by Upregulating the Expression of HK2

Chen, B., Cai, T., Huang, C., Zang, X., Sun, L., Guo, S., Wang, Q., Chen, Z., Zhao, Y., Han, Z., et al. (2021) · Frontiers in Oncology · doi:10.3389/fonc.2021.648706 · Cited by 34 · see citing works

Myoferlin Contributes to the Metastatic Phenotype of Pancreatic Cancer Cells by Enhancing Their Migratory Capacity through the Control of Oxidative Phosphorylation

Rademaker, G., Costanza, B., Anania, S., Agirman, F., Maloujahmoum, N., Valentin, E. D., Goval, J.-J., Bellahcène, A., Castronovo, V., & Peulen, O. (2019) · Cancers · doi:10.3390/cancers11060853 · Cited by 33 · see citing works

Mitochondria and the permeability transition pore in cancer metabolic reprogramming

Guo, L. (2021) · Biochemical Pharmacology · doi:10.1016/j.bcp.2021.114537 · Cited by 33 · see citing works

Abstract 1423: Resistance to LDHA inhibitors requires signaling through the AMPK/mTOR/S6K pathway leading to increased oxidative phosphorylation

Boudreau, A., Peterson, D., Moffat, J. G., Liu, B., Kwong, M., Gao, M., Purkey, H. E., O’Brien, T., Hatzivassiliou, G., Daemen, A., et al. (2014) · Cancer Research · doi:10.1158/1538-7445.am2014-1423

Abstract 964: Inhibiting glycolysis with an LDHA inhibitor: A new solution to an old problem

O’Brien, T., Purkey, H. E., Hitz, A., Peterson, D., Boudreau, A., Delnagro, C., Kwong, M., Hong, R., Gao, M., Pang, J., et al. (2014) · Cancer Research · doi:10.1158/1538-7445.am2014-964 · Cited by 3 · see citing works

Transcriptional, chromatin, and metabolic landscapes of LDHA inhibitor–resistant pancreatic ductal adenocarcinoma

Malvi, P., Rawat, V., Gupta, R., & Wajapeyee, N. (2022) · Frontiers in Oncology · doi:10.3389/fonc.2022.926437 · Cited by 10 · see citing works

Targeting the Warburg effect via LDHA inhibition engages ATF4 signaling for cancer cell survival

Pathria, G., Scott, D. A., Feng, Y., Lee, J. S., Fujita, Y., Zhang, G., Sahu, A. D., Ruppin, E., Herlyn, M., Osterman, A. L., et al. (2018) · The EMBO Journal · doi:10.15252/embj.201899735 · Cited by 157 · see citing works

Additional file 5: of Cancer cell metabolic plasticity allows resistance to NAMPT inhibition but invariably induces dependence on LDHA

Thongon, N., Zucal, C., D’Agostino, V., Tebaldi, T., Ravera, S., Zamporlini, F., Piacente, F., Moschoi, R., Raffaelli, N., Quattrone, A., et al. (2018) · Figshare · doi:10.6084/m9.figshare.5965825