Human lactate dehydrogenase (hLDH-A), a glycolytic enzyme responsible
for the conversion of pyruvate to lactate coupled with oxidation of NADH to NAD+,
plays a crucial role in the promotion of glycolysis in invasive tumor cells. hLDH-A has
been considered a vital therapeutic target for invasive cancers therefore, hLDH-A
inhibition reflects a valuable attempt in the development of innovative anticancer
strategies. Reagents that regulate or inhibit hLDH-A enzyme/ gene can play a role in
the prevention and treatment of various cancers and related diseases. In fact, selective
inhibition of hLDH-A using small molecules holds potential prospects for the treatment
of cancer. Consequently, significant progress has been made in the discovery of smallmolecules,
the selective inhibitors of hLDH-A displaying remarkable inhibitory
potency. The LDH-based approaches in the development of anticancer therapy and
treatment of related diseases are worthwhile because of the existence of LDH enzyme
at the end of glycolytic pathway. In this book chapter, 59 review and research articles,
and 15 patents filed on LDH and its application are discussed. Latest contributions in
regulation/inhibition of the LDH-A enzyme by various agents are summarized in this
book chapter.
Keywords: Aerobic glycolysis, anaerobic glycolysis, anti-inflammatory activity,
anti-proliferative activity, cancer cell metabolism, cancer cell proliferation,
epileptic treatment, FDG-PET, FRET, glycolytic pathway, gossypol, human
lactate dehydrogenase A, human lactate dehydrogenase B, isostere of pyruvate,
metabolic switch, mitochondrial dysfunction, NADH/NAD+, nanosensor, Nhydroxy-
indole, pyruvate dehydrogenase complex, selective hLDH5 inhibitors,
tumor glycolysis, warburg effect.
