Target intelligence / Profile preview

Lactate dehydrogenase A (LDHA)

Target
LDHA
Molecular classification
Enzyme, Oxidoreductase, Tetrameric protein (forms part of the lactate dehydrogenase tetramer)
01

Overview

Lactate dehydrogenase A is an enzyme encoded by the *LDHA* gene in humans. It catalyzes the interconversion between pyruvate and L-lactate with concomitant interconversion between NADH and NAD+, playing a critical role in anaerobic glycolysis. LDHA is predominantly expressed in muscle tissue but is also found at high levels in various tumors. Its activity supports rapid ATP production under low oxygen conditions by regenerating NAD+, which sustains glycolytic flux. Overexpression or increased activity of LDHA has been linked to cancer progression, invasion, metastasis, and poor clinical outcomes. As such, it is considered a promising therapeutic target for anticancer drug development[3][6][8].

Other names
LDH-AL-lactate dehydrogenase A chainMuscle subunit of lactate dehydrogenaseM subunit
02

Mechanism of action

Inhibition leads to reduced conversion of pyruvate to lactate, disrupting tumor cell metabolism and proliferation[6]

03

Biological functions

Glycolysis (conversion of pyruvate to lactate and vice versa)Regeneration of NAD+ for continued glycolytic fluxCellular energy metabolism under hypoxic conditions
04

Disease associations

Cancer (notably upregulated in many tumors and associated with aggressive/metastatic phenotypes)[3][6]Exertional myoglobinuria[3]
05

Safety considerations

Potential toxicity due to inhibition in normal tissues that rely on anaerobic glycolysis (e.g., muscle)[6]
06

Interacting drugs

FX11 (experimental inhibitor)

1 more in the full profile.

07

Biomarkers

Elevated LDHA expression as a biomarker for cancer aggressiveness and poor prognosis[3][6]

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