ArticleJournal of medicinal chemistry2020
Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties.
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Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.
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32citing papers in PubMed
2.3field-weighted citation impact, top 10% of its field
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Who cites it
32 citing papers in PubMed, 59 citations in OpenAlex.
- Lactate as a Signaling Molecule in the Tumor Microenvironment: Implications for Cancer Progression.Biochemical genetics · 2026Review
- CMA-DTI: a cross-modal fusion and attentive interaction network for interpretable drug-target interaction prediction.Frontiers in bioinformatics · 2026Article
- Metabolism, a Blossoming Target for Small-Molecule Anticancer Drugs.Molecules (Basel, Switzerland) · 2025Review
- Glucose metabolism and its direct action in cancer and immune regulation: opportunities and challenges for metabolic targeting.Journal of biomedical science · 2025Review
- Characterization of CHK-336, A First-in-Class, Liver-Targeted, Small-Molecule Lactate Dehydrogenase Inhibitor for Hyperoxaluria Treatment.Journal of the American Society of Nephrology : JASN · 2025Article
- Modification in Structures of Active Compounds in Anticancer Mitochondria-Targeted Therapy.International journal of molecular sciences · 2025Review
- Experimental, Theoretical, andACS omega · 2025Article
- OPPORTUNITIES AND CHALLENGES FOR TARGETING CANCER METABOLISM.Transactions of the American Clinical and Climatological Association · 2025Review
- Metabolic reprogramming of glucose: the metabolic basis for the occurrence and development of hepatocellular carcinoma.Frontiers in oncology · 2025Review
- Impact of lactate on immune cell function in the tumor microenvironment: mechanisms and therapeutic perspectives.Frontiers in immunology · 2025Review
- Exploring Sugar-Induced Cell Death (SICD) in Yeast: Implications for Diabetes and Cancer Research.Frontiers in cell death · 2025Article
- Dual role of lactate in human health and disease.Frontiers in physiology · 2025Review
- Synthesis of Ethyl Pyrimidine-Quinolincarboxylates Selected from Virtual Screening as Enhanced Lactate Dehydrogenase (LDH) Inhibitors.International journal of molecular sciences · 2024Article
- Synthesis and biological characterization of an orally bioavailable lactate dehydrogenase-A inhibitor against pancreatic cancer.European journal of medicinal chemistry · 2024Article
- Metabolic Rewiring in Cancer: Small Molecule Inhibitors in Colorectal Cancer Therapy.Molecules (Basel, Switzerland) · 2024Review
- Exploring the Key Amino Acid Residues Surrounding the Active Center of Lactate Dehydrogenase A for the Development of Ideal Inhibitors.Molecules (Basel, Switzerland) · 2024Article
- Forward Genetic Screens Identify Mechanisms of Resistance to Small-Molecule Lactate Dehydrogenase Inhibitors.ACS chemical biology · 2024Article
- Mitochondrial-Encoded Complex I Impairment Induces a Targetable Dependency on Aerobic Fermentation in Hürthle Cell Carcinoma of the Thyroid.Cancer discovery · 2023Article
- Synthesis andInternational journal of molecular sciences · 2023Article
- Discovery of the First Lactate Dehydrogenase Proteolysis Targeting Chimera Degrader for the Treatment of Pancreatic Cancer.Journal of medicinal chemistry · 2023Article
Corrections and comments
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Authors and funding
45 authors at 8 institutions in 1 country.
Ganesha RaiNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.ORCID 0000-0001-9763-9641
Daniel J UrbanNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Bryan T MottNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Xin HuNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Shyh-Ming YangNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.ORCID 0000-0003-1928-136X
Gloria A BenavidesMitochondrial Medicine Laboratory, Department of Pathology, University of Alabama at Birmingham, Birmingham, Alabama 35294, United States.
Michelle S JohnsonMitochondrial Medicine Laboratory, Department of Pathology, University of Alabama at Birmingham, Birmingham, Alabama 35294, United States.
Giuseppe L SquadritoMitochondrial Medicine Laboratory, Department of Pathology, University of Alabama at Birmingham, Birmingham, Alabama 35294, United States.
Kyle R BrimacombeNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Tobie D LeeNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Dorian M CheffNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Hu ZhuNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Mark J HendersonNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.ORCID 0000-0001-8590-7338
Katherine PohidaNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Gary A SulikowskiVanderbilt Institute of Chemical Biology, Vanderbilt University, Nashville, Tennessee 37232, United States.ORCID 0000-0002-1067-0767
David M DranowBeryllium Discovery Corp., 7869 Day Road West, Bainbridge Island, Washington 98110, United States.
Md KabirNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Pranav ShahNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Elias PadilhaNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Dingyin TaoNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.ORCID 0000-0001-6531-2740
Yuhong FangNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Plamen P ChristovVanderbilt Institute of Chemical Biology, Vanderbilt University, Nashville, Tennessee 37232, United States.
Kwangho KimVanderbilt Institute of Chemical Biology, Vanderbilt University, Nashville, Tennessee 37232, United States.
Somnath JanaVanderbilt Institute of Chemical Biology, Vanderbilt University, Nashville, Tennessee 37232, United States.
Pavan MuttilCollege of Pharmacy, University of New Mexico Health Sciences Center, Albuquerque, New Mexico 87131, United States.ORCID 0000-0001-7636-8141
Tamara AndersonCollege of Pharmacy, University of New Mexico Health Sciences Center, Albuquerque, New Mexico 87131, United States.
Nitesh K KundaCollege of Pharmacy, University of New Mexico Health Sciences Center, Albuquerque, New Mexico 87131, United States.ORCID 0000-0002-3063-0375
Helen J HathawayCollege of Pharmacy, University of New Mexico Health Sciences Center, Albuquerque, New Mexico 87131, United States.
Donna F KusewittDept of Pathology, University of New Mexico Cancer Center, Albuquerque, New Mexico 87131, United States.
Nobu OshimaUrologic Oncology Branch, Center for Cancer Research, National Cancer Institute, 9000 Rockville Pike, Bethesda, Maryland 20892, United States.
Murali CherukuriUrologic Oncology Branch, Center for Cancer Research, National Cancer Institute, 9000 Rockville Pike, Bethesda, Maryland 20892, United States.
Douglas R DaviesBeryllium Discovery Corp., 7869 Day Road West, Bainbridge Island, Washington 98110, United States.
Jeffrey P NorenbergCollege of Pharmacy, University of New Mexico Health Sciences Center, Albuquerque, New Mexico 87131, United States.
Larry A SklarDept of Pathology, University of New Mexico Cancer Center, Albuquerque, New Mexico 87131, United States.
William J MooreNExT Program Support, Applied/Developmental Research Directorate, Leidos Biomedical Research, Inc., Frederick National Laboratory for Cancer Research, Frederick, Maryland 21702, United States.
Chi V DangAbramson Cancer Center, Abramson Family Cancer Research Institute, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104, United States.
Gordon M StottNExT Program Support, Applied/Developmental Research Directorate, Leidos Biomedical Research, Inc., Frederick National Laboratory for Cancer Research, Frederick, Maryland 21702, United States.
Leonard NeckersUrologic Oncology Branch, Center for Cancer Research, National Cancer Institute, 9000 Rockville Pike, Bethesda, Maryland 20892, United States.
Andrew J FlintNExT Program Support, Applied/Developmental Research Directorate, Leidos Biomedical Research, Inc., Frederick National Laboratory for Cancer Research, Frederick, Maryland 21702, United States.
Victor M Darley-UsmarMitochondrial Medicine Laboratory, Department of Pathology, University of Alabama at Birmingham, Birmingham, Alabama 35294, United States.
Anton SimeonovNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Alex G WatersonVanderbilt Institute of Chemical Biology, Vanderbilt University, Nashville, Tennessee 37232, United States.
Ajit JadhavNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.
Matthew D HallNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.ORCID 0000-0002-5073-442X
David J MaloneyNational Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States.ORCID 0000-0002-5607-4178
National Institutes of Health · USUniversity of New Mexico · USVanderbilt University · USUniversity of Alabama at Birmingham · USLeidos (United States) · USNational Cancer Institute · USBeryllium (United States) · USCancer Research Institute · US
Funding
Tumor Microenvironment and MetastasisP30CA010815 · NCI · WISTAR INSTITUTE · PI Maureen E. Murphy · 1985 to 2026
$75.9MTRAINING PROGRAM IN CANCER THERAPYT32CA078207 · NCI · MOUNT SINAI SCHOOL OF MEDICINE OF NYU · PI James J Manfredi · 1999 to 2026
$11.6MMYC--TRANSCRIPTION AND INTERACTION WITH P107R01CA051497 · NCI · WISTAR INSTITUTE · PI DANG, CHI V. · 1995 to 2025
$5.3MCCR NIH HHS HHSN261200800001CIntramural NIH HHS Z99 TR999999NCI NIH HHS HHSN261200800001ENCI NIH HHS P30 CA010815NCI NIH HHS R01 CA051497NCI NIH HHS T32 CA078207
Abstract
Lactate dehydrogenase (LDH) catalyzes the conversion of pyruvate to lactate, with concomitant oxidation of reduced nicotinamide adenine dinucleotide as the final step in the glycolytic pathway. Glycolysis plays an important role in the metabolic plasticity of cancer cells and has long been recognized as a potential therapeutic target. Thus, potent, selective inhibitors of LDH represent an attractive therapeutic approach. However, to date, pharmacological agents have failed to achieve significant target engagement
Indexed as
AnimalsEnzyme InhibitorsHalf-LifeHumansL-Lactate DehydrogenaseMicePyrazolesStructure-Activity RelationshipXenograft Model Antitumor AssaysEnzyme InhibitorsL-Lactate DehydrogenasePyrazoles
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.