Top ▲

Interleukin-1 receptor, type I

Click here for help

Target id: 1905

Nomenclature: Interleukin-1 receptor, type I

Family: Immunoglobulin-like family of IL-1 receptors

Contents:

Quaternary Structure: Subunits
Interleukin 1 receptor, type I (Ligand-binding subunit)
IL-1 receptor accessory protein (Other subunit)
Database Links Click here for help
SynPHARM 77163 (in complex with IL-1 receptor antagonist)
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}

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols Click column headers to sort
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
Key to terms and symbols Click column headers to sort
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

Show »

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 12/10/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1905.