Target intelligence / Profile preview

Alpha-1-acid glycoprotein (AGP)

Target
AGP
Molecular classification
Acute-phase protein, Transport protein, Lipocalin family (PF00061 domain)
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Overview

Alpha-1-acid glycoprotein (AGP; orosomucoid) is a highly glycosylated acute-phase plasma protein, primarily produced by the liver but also expressed in other tissues. It comprises two isoforms in humans (AGP1 and AGP2, encoded by ORM1 and ORM2 genes) and features a lipocalin beta-barrel structure that affords broad ligand-binding capacity. AGP rises substantially during inflammation, infection, tissue injury, pregnancy, or estrogen therapy, with glycosylation pattern and proteoform diversity influencing its biological activities. Its main physiological functions are regulation of immune responses—especially dampening excessive inflammation—transport of basic and neutral lipophilic drugs and hormones, and possible roles in metabolic regulation. AGP's drug-binding profoundly affects pharmacokinetics and pharmacodynamics, and serum AGP levels are often monitored clinically as markers of inflammation and for dose adjustment of AGP-bound drugs.

Other names
OrosomucoidOrosomucoid-1AGP 1AGP1OMD 1
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Mechanism of action

Drug sequestration via high-affinity binding Modulation of free and bioactive drug concentrations

03

Biological functions

Drug transportHormone carrierImmune system modulation (including regulation of cytokine secretion)Acute-phase reaction in response to inflammation, injury, or infectionMetabolic regulation (proposed)
04

Disease associations

InflammationInfectionCancer (impacts pharmacodynamics of some chemotherapeutics)Liver injuryChronic and acute inflammatory conditionsPregnancy-related changes
05

Safety considerations

Therapeutic challenge: High-affinity binding to drugs can reduce their efficacy and complicate dosing, especially for chemotherapeutics and psychoactive drugsInterindividual variability: Glycosylation pattern and genetic variation (AGP1 and AGP2, allelic variants) can alter binding and serum levels, complicating prediction of drug response
06

Interacting drugs

Warfarin

9 more in the full profile.

07

Biomarkers

AGP plasma concentration (used in monitoring inflammatory conditions and as a marker for pharmacokinetics)

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