Target intelligence / Profile preview

Interleukin-1 receptor antagonist protein (IL-1RA)

Target
IL-1RA
Molecular classification
Cytokine antagonist, Receptor ligand antagonist, Soluble protein, Member of interleukin-1 cytokine family
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Overview

The interleukin-1 receptor antagonist protein (IL-1RA) is a 17–20 kDa cytokine (gene: IL1RN, chromosome 2q14.1) that binds to the interleukin-1 receptor type I on cell surfaces without triggering activation, competitively inhibiting pro-inflammatory signaling of IL-1α and IL-1β. It is secreted by immune, epithelial, and adipose cells, constituting a key endogenous regulator of inflammation and a clinical target for the treatment of inflammatory diseases. IL-1RA's crystal structure demonstrates architectural similarity to IL-1α/β, but with critical differences in receptor-binding loops that confer its antagonist function.

Other names
IL-1raIL1RNICIL-1RAIL1 inhibitorIL1F3IRAP
02

Mechanism of action

Competitive antagonism at interleukin-1 receptor type I (IL-1RI), blocking signal transduction by preventing IL-1α/IL-1β binding; Downregulation of inflammatory cytokine cascade (e.g., inhibition of MyD88 signaling)

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Biological functions

Anti-inflammatory antagonismModulation of immune responseInhibition of IL-1-mediated signalingBlocking cell activation by IL-1
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Disease associations

Inflammation (especially systemic and local inflammatory diseases)Rheumatoid arthritisSeptic shockGraft-versus-host diseaseCertain leukemiasOther autoimmune and autoinflammatory syndromes
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Safety considerations

Increased risk of infection due to immune suppressionHypersensitivity reactionsInjection site reactions (for recombinant drug)Unintended effects on host defense (e.g., susceptibility to opportunistic infection)
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Interacting drugs

Anakinra (recombinant IL-1RA)

3 more in the full profile.

07

Biomarkers

Serum IL-1RA (measured for disease activity or drug response)Circulating IL-1β or IL-1α (indirect, for pathway activation)Expression levels of IL1RN gene (genetic risk, for selection)

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