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Interleukin-1 receptor, type I

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 1905

Nomenclature: Interleukin-1 receptor, type I

Family: Immunoglobulin-like family of IL-1 receptors

Quaternary Structure: Subunits
Interleukin 1 receptor, type I (Ligand-binding subunit)
IL-1 receptor accessory protein (Other subunit)
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SynPHARM
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Complex of the interleukin-1 receptor with the interleukin-1 receptor antagonist (IL1RA)
PDB Id:  1IRA
Ligand:  IL-1 receptor antagonist
Resolution:  2.7Å
Species:  Human
References:  4
Natural/Endogenous Ligands Click here for help
IL-1α {Sp: Human}
IL-1β {Sp: Human}
IL-1 receptor antagonist {Sp: Human}

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Inhibitors
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Ligand Sp. Action Value Parameter Reference
isunakinra Peptide Primary target of this compound Immunopharmacology Ligand Hs Inhibition 10.5 pKd 3
pKd 10.5 (Kd 3x10-11 M) [3]
anakinra Peptide Approved drug Primary target of this compound Immunopharmacology Ligand Hs Inhibition 7.8 pKd 2
pKd 7.8 (Kd 1.5x10-8 M) [2]
Agonists
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Ligand Sp. Action Value Parameter Reference
IL-1α {Sp: Human} Peptide Ligand is endogenous in the given species Immunopharmacology Ligand Hs Agonist - -
IL-1β {Sp: Human} Peptide Ligand is endogenous in the given species Immunopharmacology Ligand Hs Agonist - -
Antagonists
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
AF12198 Peptide Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist - - 1
[1]
IL-1 receptor antagonist {Sp: Human} Peptide Click here for species-specific activity table Ligand is endogenous in the given species Immunopharmacology Ligand Hs Antagonist - -
Immunopharmacology Comments
Interleukin-1 receptor, type I (IL-1RI) is a heterodimer containing the ligand binding interleukin 1 receptor, type I (IL1R1) subunit and the IL-1 receptor accessory protein (IL1RAP) required for signal transduction. This receptor is primarily responsible for transmitting the inflammatory effects of interleukin-1 (IL-1). Endogenous ligands for this receptor include IL-1α, IL-1β and IL-1RA. IL-1RI signalling is involved in many biological functions; thymocyte proliferation, B cell development, IL-2 and IL-6 production, stress responses, inflammatory responses, sleep regulation, appetite and Th17 deifferentiation. This latter function links IL-1RI signalling with Th17-mediated autoimmune diseases.

References

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1. Akeson AL, Woods CW, Hsieh LC, Bohnke RA, Ackermann BL, Chan KY, Robinson JL, Yanofsky SD, Jacobs JW, Barrett RW et al.. (1996) AF12198, a novel low molecular weight antagonist, selectively binds the human type I interleukin (IL)-1 receptor and blocks in vivo responses to IL-1. J. Biol. Chem., 271 (48): 30517-23. [PMID:8940020]

2. Dripps DJ, Verderber E, Ng RK, Thompson RC, Eisenberg SP. (1991) Interleukin-1 receptor antagonist binds to the type II interleukin-1 receptor on B cells and neutrophils. J. Biol. Chem., 266 (30): 20311-5. [PMID:1834644]

3. Kovalchin J, King B, Masci A, Hopkins E, Fry J, Hou J, Li C, Tenneson K, Weber S, Wolfe G et al.. (2018) Preclinical Development of EBI-005: An IL-1 Receptor-1 Inhibitor for the Topical Ocular Treatment of Ocular Surface Inflammatory Diseases. Eye Contact Lens, 44 (3): 170-181. [PMID:28727604]

4. Schreuder H, Tardif C, Trump-Kallmeyer S, Soffientini A, Sarubbi E, Akeson A, Bowlin T, Yanofsky S, Barrett RW. (1997) A new cytokine-receptor binding mode revealed by the crystal structure of the IL-1 receptor with an antagonist. Nature, 386 (6621): 194-200. [PMID:9062194]

How to cite this page

Immunoglobulin-like family of IL-1 receptors: Interleukin-1 receptor, type I. Last modified on 16/11/2017. Accessed on 27/10/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1905.