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 of this pathway: the conversion of 5-phosphoribosyl-1-pyrophosphate (PRPP) and glutamine into 5-phosphoribosyl-1-amine (PRA). GPAT is allosterically regulated by AMP and GMP, ensuring balanced purine nucleotide synthesis. It is considered an attractive target for anticancer drug development.

Other names
AmidophosphoribosyltransferaseATase
02

Mechanism of action

Inhibition of glutaminase activity, leading to disruption of purine biosynthesis

03

Biological functions

Purine biosynthesisAmino acid metabolism
04

Disease associations

CancerTransplant rejection
05

Safety considerations

Potential for broad effects on rapidly dividing cells due to disruption of purine biosynthesis.
06

Interacting drugs

DON (6-diazo-5 oxo-L-norleucine)

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