Target intelligence / Profile preview

Glycine N-methyltransferase (GNMT)

Target
GNMT
Molecular classification
Enzyme, Methyltransferase, Metabolic enzyme
01

Overview

Glycine N-methyltransferase is a tetrameric enzyme found primarily in the liver that catalyzes the transfer of a methyl group from S-adenosylmethionine to glycine, producing sarcosine and S-adenosylhomocysteine. It helps regulate the SAM/SAH ratio—critical for cellular methylation reactions, including those affecting DNA, proteins, and lipids. GNMT is involved in detoxifying certain carcinogens and is linked to several metabolic and epigenetic pathways. Genetic deficiencies can result in metabolic disorders and increased cancer risk, while differential expression and activity have been associated with liver cancer, prostate cancer, and non-alcoholic fatty liver disease. GNMT also interacts with endogenous ligands (e.g., folate metabolites), and its product sarcosine is being studied as a biomarker for prostate cancer progression.

Other names
Glycine methyltransferaseGlycine sarcosine methyltransferaseGlycine sarcosine N-methyltransferaseGNMT_HUMANHEL-S-182mPEpididymis secretory sperm binding protein Li 182mP
02

Mechanism of action

Induction or inhibition of GNMT activity affects cellular methylation status, detoxification capacity, and metabolism; GNMT modulators can affect oncogenic potential through changes in SAM/SAH ratio

03

Biological functions

Methylation of glycine (sarcosine biosynthesis)Regulation of SAM/SAH ratio (affects global methylation, including DNA methylation)Detoxification of xenobiotics (e.g., polyaromatic hydrocarbons, aflatoxin)Regulation of gene expression via epigenetic effectsInvolvement in one-carbon metabolism, transmethylation, and energy metabolism
04

Disease associations

Liver cancer (hepatocarcinoma)Prostate cancerNon-alcoholic fatty liver disease (NAFLD)Hypermethioninemia (inborn error)Metabolic dysfunction/chronic diseases
05

Safety considerations

Altered GNMT activity can lead to abnormal methylation and metabolite accumulation (e.g., excessive methionine, impaired detoxification)Therapeutic targeting may affect global methylation—potential for epigenetic disturbances
06

Interacting drugs

1,2,3,4,6-penta-O-galloyl-β-d-glucopyranoside (PGG) (GNMT inducer)

1 more in the full profile.

07

Biomarkers

Sarcosine (proposed prostate cancer biomarker)GNMT protein level or activity (biomarker for liver disease/NAFLD)

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