Target intelligence / Profile preview

Glutamine–5-phosphoribosylpyrophosphate Amidotransferase (GPAT)

Target
GPAT
Molecular classification
Enzyme, Short-chain dehydrogenases/reductases
01

Overview

Glutamine–5-phosphoribosylpyrophosphate amidotransferase (GPAT) is a key enzyme in the de novo purine biosynthesis pathway. It catalyzes the first committed step: the conversion of 5-phosphoribosyl-1-pyrophosphate (PRPP) and glutamine into 5-phosphoribosyl-1-amine (PRA), pyrophosphate, and glutamate. GPAT is tightly regulated and a potential therapeutic target, particularly in cancer.

Other names
ATaseAmidophosphoribosyltransferase
02

Mechanism of action

Covalent modification of active site cysteine, inhibiting glutamine binding and glutaminolysis.

03

Biological functions

Purine biosynthesisNucleotide metabolismCell proliferationAmino acid metabolism
04

Disease associations

Mature B-cell lymphomaTransplant rejectionCancer
05

Safety considerations

Potential for off-target effects due to broad role in nucleotide synthesis.Inhibition can impact normal cell function alongside cancerous cells.
06

Interacting drugs

DON (6-diazo‑5‑oxo L-norleucine)

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