Lactate dehydrogenase (LDH) inhibition is considered a worthwhile attempt in the development of innovative anticancer strategies. Unfortunately, in spite of the involvement of several research institutions and pharma-companies, the discovery of LDH inhibitors with drug-like properties seems a hardly resolvable challenge. While awaiting new advancements, in the present review we will examine other pathologic conditions characterized by increased glycolysis and LDH activity, which could potentially benefit from LDH inhibition. The rationale for targeting LDH activity in these contexts is the same justifying the LDH-based approach in anticancer therapy: because of the enzyme position at the end of glycolytic pathway, LDH inhibitors are not expected to hinder glucose metabolism of normal cells. Moreover, we will summarize the latest contributions in the discovery of enzyme inhibitors and try to glance over the reasons underlying the complexity of this research.

Di Stefano, G., Manerba, M., Di Ianni, L., Fiume, L. (2016). Lactate dehydrogenase inhibition: Exploring possible applications beyond cancer treatment. FUTURE MEDICINAL CHEMISTRY, 8(6), 713-725 [10.4155/fmc.16.10].

Lactate dehydrogenase inhibition: Exploring possible applications beyond cancer treatment

DI STEFANO, GIUSEPPINA;MANERBA, MARCELLA;DI IANNI, LORENZA;FIUME, LUIGI
2016

Abstract

Lactate dehydrogenase (LDH) inhibition is considered a worthwhile attempt in the development of innovative anticancer strategies. Unfortunately, in spite of the involvement of several research institutions and pharma-companies, the discovery of LDH inhibitors with drug-like properties seems a hardly resolvable challenge. While awaiting new advancements, in the present review we will examine other pathologic conditions characterized by increased glycolysis and LDH activity, which could potentially benefit from LDH inhibition. The rationale for targeting LDH activity in these contexts is the same justifying the LDH-based approach in anticancer therapy: because of the enzyme position at the end of glycolytic pathway, LDH inhibitors are not expected to hinder glucose metabolism of normal cells. Moreover, we will summarize the latest contributions in the discovery of enzyme inhibitors and try to glance over the reasons underlying the complexity of this research.
2016
Di Stefano, G., Manerba, M., Di Ianni, L., Fiume, L. (2016). Lactate dehydrogenase inhibition: Exploring possible applications beyond cancer treatment. FUTURE MEDICINAL CHEMISTRY, 8(6), 713-725 [10.4155/fmc.16.10].
Di Stefano, Giuseppina; Manerba, Marcella; Di Ianni, Lorenza; Fiume, Luigi
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11585/572790
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