Target intelligence / Profile preview

Glutathione S-transferase alpha 1 (GSTA1)

Target
GSTA1
Molecular classification
Enzyme (specifically, transferase), Phase II detoxification enzyme, Glutathione S-transferase superfamily, alpha class
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Overview

Glutathione S-transferase alpha 1 is a cytosolic enzyme belonging to the alpha class of the glutathione S-transferases. It catalyzes the conjugation of reduced glutathione with various electrophilic compounds—both exogenous toxins/drugs and endogenous metabolic products—facilitating their detoxification. The protein also exhibits peroxidase activity toward lipid hydroperoxides and participates in steroid hormone biosynthesis. Overexpression has been linked with cancer development, particularly regarding chemoresistance mechanisms. The gene encoding this protein is located on chromosome 6p12.2.

Other names
GST class-alpha member 1GST HA subunit 1GSTA1-1GTH1Androst-5-ene-3,17-dione isomerase13-hydroperoxyoctadecadienoate peroxidase
02

Mechanism of action

Drugs targeting or affected by Glutathione S-transferases typically act through: - Inhibition or modulation of enzymatic activity to alter drug resistance profiles. - Enhancement or reduction of detoxification capacity for chemotherapeutic agents. - Conjugation with glutathione to increase solubility/excretion.

03

Biological functions

Detoxification of xenobiotics and endogenous compounds via glutathione conjugationProtection against oxidative stress through glutathione peroxidase activityMetabolism of prostaglandins and fatty acid hydroperoxidesSteroid hormone biosynthesis via isomerization reactions
04

Disease associations

Cancer (implicated in chemoresistance and tumor biology)Inflammation (involved in inflammatory mediator metabolism)
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Safety considerations

Potential for increased drug toxicity if inhibited, due to reduced detoxification capacityContribution to multidrug resistance when overexpressed in tumors
06

Interacting drugs

Busulfan (detoxified by conjugation)

2 more in the full profile.

07

Biomarkers

Chemotherapy resistance prediction in certain cancersHepatocellular injury monitoring due to its high liver expression

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