Target intelligence / Profile preview

Glycinamide Ribonucleotide Transformylase (GARFTase)

Target
GARFTase
Molecular classification
Enzyme, Formyltransferase
01

Overview

Glycinamide ribonucleotide transformylase (GARFTase) is a key folate-dependent enzyme in the de novo purine biosynthesis pathway. It catalyzes the transfer of a formyl group from 10-formyltetrahydrofolate to glycinamide ribonucleotide (GAR), producing formylglycinamide ribonucleotide (FGAR). This reaction is essential for the synthesis of purine nucleotides. As an essential enzyme for cell proliferation, GARFTase is an important target for antitumor drug design. Inhibition disrupts de novo purine synthesis leading to cytotoxicity especially in rapidly dividing cells such as cancer cells.

Other names
Phosphoribosylglycinamide formyltransferaseGART
02

Mechanism of action

Inhibition of de novo purine synthesis

03

Biological functions

Purine biosynthesisNucleotide synthesisCell proliferation
04

Disease associations

CancerInflammation
05

Safety considerations

Cytotoxicity due to disruption of nucleotide synthesisPotential for off-target effects on normal cells
06

Interacting drugs

Antifolate drugs
07

Biomarkers

GART expression level in tumor tissue

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