The biochemical and clinical perspectives of lactate dehydrogenase: an enzyme of active metabolism

AA Khan, KS Allemailem… - … Metabolic & Immune …, 2020 - ingentaconnect.com
Background: Lactate dehydrogenase (LDH) is a group of oxidoreductase isoenzymes
catalyzing the reversible reaction between pyruvate and lactate. The five isoforms of this …

Recent Update on Human Lactate Dehydrogenase Enzyme 5 (hLDH5) Inhibitors: A Promising Approach for Cancer Chemotherapy: Miniperspective

R Rani, V Kumar - Journal of medicinal chemistry, 2016 - ACS Publications
Human lactate dehydrogenase (h LDH5), a glycolytic enzyme responsible for the conversion
of pyruvate to lactate coupled with oxidation of NADH to NAD+, plays a crucial role in the …

Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition

A Boudreau, HE Purkey, A Hitz, K Robarge… - Nature chemical …, 2016 - nature.com
Metabolic reprogramming in tumors represents a potential therapeutic target. Herein we
used shRNA depletion and a novel lactate dehydrogenase (LDHA) inhibitor, GNE-140, to …

Discovery and optimization of potent, cell-active pyrazole-based inhibitors of lactate dehydrogenase (LDH)

G Rai, KR Brimacombe, BT Mott, DJ Urban… - Journal of medicinal …, 2017 - ACS Publications
We report the discovery and medicinal chemistry optimization of a novel series of pyrazole-
based inhibitors of human lactate dehydrogenase (LDH). Utilization of a quantitative high …

[HTML][HTML] An update on therapeutic opportunities offered by cancer glycolytic metabolism

C Granchi, D Fancelli, F Minutolo - Bioorganic & medicinal chemistry letters, 2014 - Elsevier
Almost all invasive cancers, regardless of tissue origin, are characterized by specific
modifications of their cellular energy metabolism. In fact, a strong predominance of aerobic …

Targeting L‐lactate metabolism to overcome resistance to immune therapy of melanoma and other tumor entities

RG Feichtinger, R Lang - Journal of oncology, 2019 - Wiley Online Library
Although immunotherapy plays a significant role in tumor therapy, its efficacy is impaired by
an immunosuppressive tumor microenvironment. A molecule that contributes to the protumor …

Murburn precepts for lactic‐acidosis, Cori cycle, and Warburg effect: Interactive dynamics of dehydrogenases, protons, and oxygen

KM Manoj, V Nirusimhan, A Parashar… - Journal of Cellular …, 2022 - Wiley Online Library
It is unresolved why lactate is transported to the liver for further utilization within the
physiological purview of Cori cycle, when muscles have more lactate dehydrogenase (LDH) …

Pyrazole-based lactate dehydrogenase inhibitors with optimized cell activity and pharmacokinetic properties

G Rai, DJ Urban, BT Mott, X Hu, SM Yang… - Journal of medicinal …, 2020 - ACS Publications
Lactate dehydrogenase (LDH) catalyzes the conversion of pyruvate to lactate, with
concomitant oxidation of reduced nicotinamide adenine dinucleotide as the final step in the …

Protective effects of phloridzin against methotrexate-induced liver toxicity in rats

MMA Khalifa, AG Bakr, AT Osman - Biomedicine & Pharmacotherapy, 2017 - Elsevier
Background Liver is the largest internal organ concerning with metabolism, hormonal
balance and clarifying of the toxins. One of the main complications of methotrexate (MTX) …

Structural and functional regulation of lactate dehydrogenase-A in cancer

MR Woodford, VZ Chen, SJ Backe… - Future Medicinal …, 2020 - Taylor & Francis
Dysregulated metabolism is one of the hallmarks of cancer. Under normal physiological
conditions, ATP is primarily generated by oxidative phosphorylation. Cancers commonly …