Target intelligence / Profile preview

Glycinamide Ribonucleotide Formyltransferase (GART)

Target
GART
Molecular classification
Enzyme, Purinosome complex
01

Overview

GART is a trifunctional enzyme essential for the de novo purine biosynthesis pathway. It catalyzes three distinct reactions: glycinamide ribonucleotide synthetase (GARS), aminoimidazole ribonucleotide synthetase (AIRS), and glycinamide ribonucleotide formyltransferase (GARTfase). Specifically, the GART domain catalyzes the formation of N2-formyl-N1-(5-phospho-D-ribosyl)glycinamide from glycinamide ribonucleotide using 10-formyltetrahydrofolate as a cofactor. The folate-binding region is targeted by antifolate chemotherapeutic agents, disrupting nucleotide synthesis required for cell proliferation.

Other names
Trifunctional purine biosynthetic protein adenosine-3GAR transformylaseGARS-AIRS-GARTPUR2 ProteinTrifunctional purine biosynthetic protein adenosine–3
02

Mechanism of action

Inhibition of folate-binding site, disrupting nucleotide synthesis

03

Biological functions

Purine biosynthesisNucleotide synthesisCell proliferation
04

Disease associations

CancerInflammation
05

Safety considerations

Inhibition can affect normal cell proliferation
06

Interacting drugs

Lometrexol

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