Target intelligence / Profile preview

Gamma-glutamyltransferase (GGT)

Target
GGT
Molecular classification
Enzyme, Transferase, Transmembrane protein
01

Overview

Gamma-glutamyltransferase is a membrane-bound enzyme that catalyzes the transfer of gamma-glutamyl groups from molecules like glutathione to amino acids, peptides, or water. It plays a central role in the gamma-glutamyl cycle responsible for glutathione synthesis and degradation—critical processes in cellular antioxidant defense and detoxification. The enzyme is highly expressed on the luminal surface of cells in tissues such as the liver, kidney, pancreas, bile ducts, heart, brain and others. Clinically significant as a sensitive biomarker for hepatobiliary dysfunction—including cholestasis—and alcohol consumption monitoring. Elevated serum/plasma concentrations are associated with various pathologies including chronic liver diseases/cancer but can also be influenced by medications or metabolic conditions unrelated to primary hepatic injury. Gamma-glutamyltransferase is considered an emerging therapeutic target due to its involvement in redox regulation and tumor biology.[1][3][4]

Other names
γ-glutamyltransferasegamma-GTgamma-glutamyl transpeptidaseGGTP
02

Mechanism of action

*For drugs targeting this molecule directly*: Inhibition of enzymatic activity to modulate glutathione metabolism or reduce pro-tumorigenic effects in cancer. *For interacting drugs listed above*: Induction or inhibition of enzyme expression/activity as a side effect rather than direct therapeutic targeting.[3]

03

Biological functions

Glutathione metabolismAmino acid transport across cell membranesDrug and xenobiotic detoxificationRegulation of oxidative stress and redox homeostasis
04

Disease associations

Cancer (notably liver cancer)Liver disease (including hepatitis, cirrhosis)Bile duct disorders (cholestasis)Cardiovascular disease (heart failure)Diabetes/metabolic syndromePancreatic disease
05

Safety considerations

High sensitivity but low specificity for liver damage—elevated by many non-liver conditions or medications/alcohol use; not diagnostic alone for specific diseases; potential confounding by sex/age differences in normal range; risk of overinterpretation leading to unnecessary further testing
06

Interacting drugs

Acetaminophen (increases GGT levels)

4 more in the full profile.

07

Biomarkers

Serum/plasma GGT level for diagnosis and monitoring of liver and bile duct diseases, alcohol use disorder, drug-induced liver injury; used alongside other liver function tests such as ALT, AST, ALP

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