LDH-A INHIBITION

The Warburg Effect refers to the observation that cancer cells preferentially utilize glycolysis to generate energy, even when alternative means are available. Therefore, inhibition of glycolysis has potential as a selective anticancer strategy for highly glycolytic tumors. In 2011 we identified small molecule inhibitors of lactate dehydrogenase A (LDH-A), an enzyme involved in the final steps of glycolysis, and showed that these compounds can induce death of cancer cells in culture. LDH-A inhibition and other tactics that exploit the Warburg Effect have considerable potential as selective anticancer strategies.

 

Related Publications:

128. 

Characterization of the Saffron Derivative Crocetin as an Inhibitor of Human Lactate Dehydrogenase 5 in the Antiglycolytic Approach against Cancer

Granchi, C.; Fortunato, S.; Meni, S.; Rizzolio, F.; Caligiuri, I.; Tuccinardi, T.; Lee, H.-Y.; Hergenrother, P. J.; Minutolo, F.

J. Agric. Food Chem. 2017, DOI: 10.1021/acs.jafc.7b01668.

 

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125. 

Reactive Oxygen Species Synergize to Potently and Selectively Induce Cancer Cell Death

Lee, H.-Y.; Parkinson, E. I.; Granchi, C.; Paterni, I.; Panigrahy, D.; Seth, P.; Minutolo, F.; Hergenrother, P. J.

ACS Chem. Biol. 2017, 12, 1416-1424.

 

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114.

Salicylketoximes that Target Glucose Transporter 1 Restrict Energy Supply to Lung Cancer Cells

Granchi, C.; Qian, Y.; Lee, H. Y.; Paterni, I.; Pasero, C.; Iegre, J.; Carlson, K. E.; Tuccinardi, T.; Chen, X.; Katzenellenbogen, J. A.; Hergenrother, P. J.; Minutolo, F.

ChemMedChem 2015, 10, 1892-1900.

 

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111.

Synthesis and Biological Evaluation of Non-Glucose Glycoconjugated N-Hydroyxindole Class LDH Inhibitors as Anticancer Agents

DiBussolo, V.; Calvaresi, E. C.; Granchi, C.; DelBino, L.; Frau, I.; Lang, M.; Tuccinardi, T.; Macchia, M.; Matinelli, A.; Hergenrother, P. J.; Minutolo, F.  

RSC Adv. 20155, 19944-19954.

 

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101.

Dual Targeting of the Warburg Effect with a Glucose-Conjugated Lactate Dehydrogenase Inhibitor

Calvaresi, E. C.; Granchi, C.; Tuccinardi, T.; DiBussolo, V.; Huigens, R. W.; Lee, H.-Y.; Palchaudhuri, R.; Macchia, M.; Martinelli, A.; Minutolo, F.; Hergenrother, P. J.

ChemBioChem 2013, 14, 2263-2267.

 

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96.

Assessing the Differential Action on Cancer Cells of LDH-A Inhibitors based on the N-Hydroxyindole-2-Carboxylate (NHI) and Malonic (Mal) Scaffolds

Granchi, C.; Calvaresi, E. C.; Tuccinardi, T.; Paterni, I.; Macchia, M.; Martinelli, A.; Hergenrother, P. J.; Minutolo, F.

Org. Biomol. Chem. 2013, 11, 6588-6596.

 

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95.

Glucose conjugation for the specific targeting and treatment of cancer

Calvaresi, E. C.; Hergenrother, P. J.

Chem. Sci. 2013, 4, 2319-2333.

 

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RSC Highlight

Chemical Biology Interface Highlight

80.

Discovery of N-Hydroxyindole-Based Inhibitors of Human Lactate Dehydrogenase Isoform A (LDH-A) as Starvation Agents Against Cancer Cells

Granchi, C.; Roy, S.; Giacomelli, C.; Macchia, M.; Tuccinardi, T.; Martinelli, A.; Lanza, M.; Betti, L.; Giannaccini, G.; Lucacchini, A.; Funel, N.; Leon, L. G.; Giovannetti, E.; Peters, G. J.; Palchaudhuri, R.; Calvaresi, E. C.; Hergenrother, P. J.; Minutolo, F.

J. Med. Chem. 2011, 54, 1599-1612.

 

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Professor Paul J. Hergenrother

hergenro@illinois.edu

261 Roger Adams Lab

600 S. Mathews Avenue

Urbana, IL 61802

The Chemistry Department at the University of Illinois

Copyright © 2014 The Hergenrother Group

Kate Neef

Administrative Assistant

kneef1@illinois.edu

245 Roger Adams Lab

#PJHteam