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S.P.H. Alexander et al. The Concise Guide to PHARMACOLOGY 2015/16: Catalytic receptors. British Journal of Pharmacology (2015) 172, 5979–6023

THE CONCISE GUIDE TO PHARMACOLOGY 2015/16:Catalytic receptors

Stephen PH Alexander1, Doriano Fabbro2, Eamonn Kelly3, Neil Marrion3, John A Peters4, Helen E Benson5,Elena Faccenda5, Adam J Pawson5, Joanna L Sharman5, Christopher Southan5, Jamie A Davies5

and CGTP Collaborators

1School of Biomedical Sciences, University of Nottingham Medical School, Nottingham, NG7 2UH, UK 2 PIQUR Therapeutics, Basel 4057, Switzerland 3School of Physiology and Pharmacology, University of Bristol, Bristol, BS8 1TD, UK 4Neuroscience Division, Medical Education Institute, Ninewells Hospital and Medical School, University of Dundee, Dundee, DD1 9SY, UK 5Centre for Integrative Physiology, University of Edinburgh, Edinburgh, EH8 9XD, UK

Abstract

The Concise Guide to PHARMACOLOGY 2015/16 provides concise overviews of the key properties of over 1750 human drug targets with their pharmacology, plus links to an open access knowledgebaseof drug targets and their ligands (www.guidetopharmacology.org ), which provides more detailed views of target and ligand properties. The full contents can be found at http://onlinelibrary.wiley.com/doi/10.1111/bph.13353/full. G protein-coupled receptors are one of the eight major pharmacological targets into which the Guide is divided, with the others being: G protein-coupled receptors, ligand-gatedion channels, voltage-gated ion channels, other ion channels, nuclear hormone receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on thebest available pharmacological tools, alongside key references and suggestions for further reading. The Concise Guide is published in landscape format in order to facilitate comparison of related targets.It is a condensed version of material contemporary to late 2015, which is presented in greater detail and constantly updated on the website www.guidetopharmacology.org, superseding data presentedin the previous Guides to Receptors & Channels and the Concise Guide to PHARMACOLOGY 2013/14. It is produced in conjunction with NC-IUPHAR and provides the official IUPHAR classificationand nomenclature for human drug targets, where appropriate. It consolidates information previously curated and displayed separately in IUPHAR-DB and GRAC and provides a permanent, citable,point-in-time record that will survive database updates.

Conflict of interest

The authors state that there are no conflicts of interest to declare.

c 2015 The Authors. British Journal of Pharmacology published by John Wiley & Sons Ltd on behalf of The British Pharmacological Society.This is an open access article under the terms of the Creative Commons Attribution License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.

Overview: Catalytic receptors are cell-surface proteins, usuallydimeric in nature, which encompass ligand binding and func-tional domains in one polypeptide chain. The ligand bindingdomain is placed on theextracellular surface of the plasma mem-brane and separated from the functional domain by a singletransmembrane-spanning domain of 20-25 hydrophobic aminoacids. The functional domain on the intracellular face of theplasma membrane has catalytic activity, or interacts with partic-ular enzymes, giving the superfamily of receptors its name. En-

dogenous agonists of the catalytic receptor superfamily are pep-tides or proteins, the binding of which may induce dimerizationof the receptor, which is the functional version of the receptor.Amongst the catalytic receptors, particular subfamilies may bereadily identified dependent on the function of the enzymaticportion of the receptor. The smallest group is the particulateguanylyl cyclases of the natriuretic peptide receptor family. Themost widely recognized group is probably the receptor tyrosinekinase (RTK) family, epitomized by the neurotrophin receptor

family, where a crucial initial step is the activation of a signallingcascade by autophosphorylation of the receptor on intracellulartyrosine residue(s) catalyzed by enzyme activity intrinsic to thereceptor. A third group is the extrinsic protein tyrosine kinasereceptors, where the catalytic activity resides in a separate pro-tein from the binding site. Examples of this group include theGDNF and ErbB receptor families, where one, catalytically silent,member of the heterodimer is activated upon binding the ligand,causing the second member of the heterodimer, lacking ligand

Searchable database: http://www.guidetopharmacology.org/index.jsp Catalytic receptors 5979

Full Contents of ConciseGuide: http://onlinelibrary.wiley.com/doi/10.1111/bph.13353/full

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=862http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=862http://www.guidetopharmacology.org/http://onlinelibrary.wiley.com/doi/10.1111/bph.13353/fullhttp://onlinelibrary.wiley.com/doi/10.1111/bph.13353/fullhttp://onlinelibrary.wiley.com/doi/10.1111/bph.13353/fullhttp://www.guidetopharmacology.org/http://www.guidetopharmacology.org/http://www.guidetopharmacology.org/index.jsphttp://onlinelibrary.wiley.com/doi/10.1111/bph.13353/fullhttp://onlinelibrary.wiley.com/doi/10.1111/bph.13353/fullhttp://www.guidetopharmacology.org/index.jsphttp://www.guidetopharmacology.org/http://onlinelibrary.wiley.com/doi/10.1111/bph.13353/fullhttp://onlinelibrary.wiley.com/doi/10.1111/bph.13353/fullhttp://www.guidetopharmacology.org/http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=862


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binding capacity, to initiate signaling through tyrosine phos-phorylation. A fourth group, the receptor threonine/serine ki-nase (RTSK) family, exemplified by TGF-β and BMP receptors,has intrinsic serine/threonine protein kinase activity in the het-

erodimeric functional unit. A fifth group is the receptor ty-rosine phosphatases (RTP), which appear to lack cognate lig-ands, but may be triggered by events such as cell:cell contactand have identified roles in the skeletal, hematopoietic and

immune systems.A sixth group of catalytic receptors in the Guide is the integrins,which have roles in cell:cell communication, often associatedwith signaling in the blood.

Family structure

5981 Cytokine receptor family

5981 IL-2 receptor family




5985 Prolactin receptor family

5986 Interferon receptor family


5988 Immunoglobulin-like family of IL-1 receptors


5990 GDNF receptor family

5991 Integrins

5994 Natriuretic peptide receptor family

5996 Pattern recognition receptors5996 Toll-like receptor family

5997 NOD-like receptor family– Receptor kinases– Other protein kinases– TK: Tyrosine kinase

5999 Receptor serine/threonine kinase (RSTK) family

6000 Type I receptor serine/threonine kinases

6001 Type II receptor serine/threonine kinases

6001 Type III receptor serine/threonine kinases

6002 RSTK functional heteromers

6003 Receptor tyrosine kinases6004 Type I RTKs: ErbB (epidermal growth factor)

receptor family

6005 Type II RTKs: Insulin receptor family

6005 Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family6007 Type IV RTKs: VEGF (vascular endothelial growth factor)

receptor family

6008 Type V RTKs: FGF (fibroblast growth factor)receptor family

6008 Type VI RTKs: PTK7/CCK4

6009 Type VII RTKs: Neurotrophin receptor/Trk family

6010 Type VIII RTKs: ROR family

6010 Type IX RTKs: MuSK

6010 Type X RTKs: HGF (hepatocyte growth factor)receptor family

6011 Type XI RTKs: TAM (TYRO3-, AXL- and MER-TK)receptor family

6012 Type XII RTKs: TIE family of angiopoietin receptors

6012 Type XIII RTKs: Ephrin receptor family

6013 Type XIV RTKs: RET

6014 Type XV RTKs: RYK

6014 Type XVI RTKs: DDR (collagen receptor) family

6015 Type XVII RTKs: ROS receptors

6015 Type XVIII RTKs: LMR family6016 Type XIX RTKs: Leukocyte tyrosine kinase (LTK)

receptor family

6016 Type XX RTKs: STYK1– TKL: Tyrosine kinase-like

6017 Receptor tyrosine phosphatases (RTP)

6018 Tumour necrosis factor (TNF) receptor family

Searchable database: http://www.guidetopharmacology.org/index.jsp Catalytic receptors 5980

Full Contents of ConciseGuide: http://onlinelibrary.wiley.com/doi/10.1111/bph.13353/full

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Cytokine receptor familyCatalytic receptors Cytokine receptor family

Overview: Cytokines are not a clearly defined group of agents,otherthan having an impact on immune signalling pathways, al-

though many cytokines have effects on other systems, such as indevelopment. A feature of some cytokines, which allows themto be distinguished from hormones, is that they may be pro-duced by “non-secretory” cells, for example, endothelial cells.Within the cytokine receptor family, some subfamilies may beidentified, which are described elsewhere in the Guide to PHAR-MACOLOGY, receptors for the TNF family, the TGF-β family andthe chemokines. Within this group of records are described TypeI cytokine receptors, typifiedby interleukin receptors, and TypeIIcytokine receptors, exemplified by interferon receptors. These re-ceptors possess a conserved extracellularregion, knownas thecy-tokine receptor homology domain (CHD), along with a range of other structural modules, including extracellular immunoglobu-lin(Ig)-like andfibronectintype III (FBNIII)-likedomains,a trans-

membranedomain, and intracellular homologydomains. An un-usual feature of this group of agents is the existence of soluble

and decoy receptors. These bind cytokines without allowing sig-nalling to occur. A further attribute is the production of endoge-nous antagonist molecules, which bind to the receptors selec-tively and prevent signalling. A commonality of these families of receptors is the ligand-induced homo- or hetero-oligomerisation,which results in the recruitment of intracellular protein part-ners to evoke cellular responses, particularly in inflammatory orhaematopoietic signalling. Although not a n exclusive signallingpathway, a common feature of the majority of cytokine recep-tors is activation of the JAK/STAT pathway. This cascade is basedaround the protein tyrosine kinase activity of the Janus kinases(JAK), which phosphorylate the receptor and thereby facilitatethe recruitment of signal transducers and activators of transcrip-tion (STATs). The activated homo- or heterodimeric STATs func-

tion principally as transcription factors in the nucleus.

Type I cytokine receptors are characterized by two pairs of conserved cysteines linked via disulfide bonds and a C-terminalWSXWS motif within their CHD. Type I receptors are commonlyclassified into five groups, based on sequence and structual ho-mology of the receptor and its cytokine ligand, which is poten-tially morereflectiveof evolutionaryrelationships thanan earlierscheme based on the use of common signal transducing chainswithin a receptor complex. These are the IL-2, IL-3, IL-6, IL-12and prolactin families.

Type II cytokine receptors also have two pairs of conservedcysteines but with a different arrangementto Type I and also lackthe WSXWS motif. The type II cytokine receptors include the in-terferon, IL-10, IL-1 and IL-17 receptors.

IL-2 receptor familyCatalytic receptors Cytokine receptor family IL-2 receptor family

Overview: The IL-2 receptor family consists of one or more ligand-selective subunits, and a common γ chain (γ c): IL2RG, P31785), though IL-4 and IL-7 receptors can form complexes with other receptorchains. Receptors of this family associate with Jak1 and J ak3, primarily activating Stat5, although certain family members can also activate Stat1, Stat3, or Stat6. Ro264550 has been described as a selectiveIL-2 receptor antagonist, which binds to IL-2 [177].

Nomenclature Interleukin-2 receptor Interleukin-4 receptor type I Interleukin-4 receptor type II Interleukin-7 receptor Interleukin-9 receptor

Subunits Interleukin-2 receptor subunit β(Ligand-binding subunit),Interleukin-2 receptor subunit γ

(Other subunit),Interleukin-2 receptor subunit α(Ligand-binding subunit)

Interleukin-4 receptor subunit α(Ligand-binding subunit),Interleukin-2 receptor subunit γ

(Other subunit)

Interleukin-13 receptor subunit α1(Other subunit),Interleukin-4 receptor subunit α

(Ligand-binding subunit)

Interleukin-2 receptor subunit γ (Other subunit),Interleukin-7 receptor subunit α


Interleukin-2 receptor subunit γ (Other subunit),Interleukin 9 receptor


Endogenous agonists IL-2 (IL2, P60568) IL-4 (IL4, P05112) IL-13 (IL13, P35225), IL-4 (IL4,P05112)

IL-7 (IL7 , P13232) IL-9 (IL9, P15248)

Endogenous antagonists IL-1 receptor antagonist (IL1RN ,P18510)

– – – –

Antagonists Ro26-4550 [177] – – – –

Selective antagonists AF12198 [3] – – – –

Searchable database: http://www.guidetopharmacology.org/index.jsp IL-2 receptor family 5981Full Contents of ConciseGuide: http://onlinelibrary.wiley.com/doi/10.1111/bph.13353/full

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Nomenclature Interleukin 13 receptor, α2 Interleukin-15 receptor Interleukin-21 receptor Thymic stromal lymphopoietin receptor

HGNC, UniProt IL13RA2, Q14627 – – –

Subunits – Interleukin-2 receptor subunit β(Ligand-binding subunit),

Interleukin-15 receptor subunit α(Ligand-binding subunit),Interleukin-2 receptor subunit γ (Other subunit)

Interleukin-2 receptor subunit γ (Other subunit), Interleukin 21 receptor


Cytokine receptor-like factor 2 (Other subunit), Interleukin-7 receptor subunit α


E ndogenous a gonists – IL-15 (IL15, P40933) IL-21 (IL21, Q9HBE4) thymic stromal lymphopoietin (TSLP ,Q969D9)

Commen ts Decoy receptor t hat bin ds IL-13 (IL13,P35225) as a monomer.

– – –

Subunits

Nomenclature Interleukin-2 receptor subunit α Interleukin-2 receptor subunit β Interleukin-2 receptor subunit γ Interleukin-4 receptor subunit α Interleukin-7 receptor subunit α

HGNC, UniProt IL2RA, P01589 IL2RB , P14784 IL2RG, P31785 IL4R, P24394 IL7R, P16871

Antibodies daclizumab (Binding) (p K d 8)[154], basiliximab (Binding)

– – dupilumab (Binding) (pIC50 11.1)[121]

–

Nomenclature Interleukin 9 receptor Interleukin-13 receptor subunit α1 Interleukin-15 receptor subunit α Interleukin 21 receptor Cytokine receptor-like factor 2

HGNC, UniProt IL9R, Q01113 IL13RA1, P78552 IL15RA, Q13261 IL21R, Q9HBE5 CRLF2, Q9HC73


http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1701http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1701http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1701http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2302http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2304http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2305http://www.genenames.org/data/hgnc_data.php?hgnc_id=5975http://www.genenames.org/data/hgnc_data.php?hgnc_id=5975http://www.uniprot.org/uniprot/Q14627http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1696http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1696http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1702http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1702http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2303http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2303http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2303http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2303http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1703http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1704http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1698http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1698http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4981http://www.genenames.org/data/hgnc_data.php?hgnc_id=5977http://www.genenames.org/data/hgnc_data.php?hgnc_id=5977http://www.genenames.org/data/hgnc_data.php?hgnc_id=5977http://www.uniprot.org/uniprot/P40933http://www.uniprot.org/uniprot/P40933http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4987http://www.genenames.org/data/hgnc_data.php?hgnc_id=6005http://www.genenames.org/data/hgnc_data.php?hgnc_id=6005http://www.genenames.org/data/hgnc_data.php?hgnc_id=6005http://www.uniprot.org/uniprot/Q9HBE4http://www.uniprot.org/uniprot/Q9HBE4http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5083http://www.genenames.org/data/hgnc_data.php?hgnc_id=30743http://www.genenames.org/data/hgnc_data.php?hgnc_id=30743http://www.genenames.org/data/hgnc_data.php?hgnc_id=30743http://www.uniprot.org/uniprot/Q969D9http://www.uniprot.org/uniprot/Q969D9http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4980http://www.genenames.org/data/hgnc_data.php?hgnc_id=5973http://www.genenames.org/data/hgnc_data.php?hgnc_id=5973http://www.genenames.org/data/hgnc_data.php?hgnc_id=5973http://www.uniprot.org/uniprot/P35225http://www.uniprot.org/uniprot/P35225http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1695http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1695http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1696http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1696http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2303http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2303http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1697http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1697http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1698http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1698http://www.genenames.org/data/hgnc_data.php?hgnc_id=6008http://www.genenames.org/data/hgnc_data.php?hgnc_id=6008http://www.uniprot.org/uniprot/P01589http://www.genenames.org/data/hgnc_data.php?hgnc_id=6009http://www.genenames.org/data/hgnc_data.php?hgnc_id=6009http://www.uniprot.org/uniprot/P14784http://www.genenames.org/data/hgnc_data.php?hgnc_id=6010http://www.genenames.org/data/hgnc_data.php?hgnc_id=6010http://www.uniprot.org/uniprot/P31785http://www.genenames.org/data/hgnc_data.php?hgnc_id=6015http://www.uniprot.org/uniprot/P24394http://www.genenames.org/data/hgnc_data.php?hgnc_id=6024http://www.genenames.org/data/hgnc_data.php?hgnc_id=6024http://www.uniprot.org/uniprot/P16871http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6880http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6879http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7574http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1699http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1700http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1700http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1700http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1702http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1702http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1703http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1704http://www.genenames.org/data/hgnc_data.php?hgnc_id=6030http://www.genenames.org/data/hgnc_data.php?hgnc_id=6030http://www.uniprot.org/uniprot/Q01113http://www.genenames.org/data/hgnc_data.php?hgnc_id=5974http://www.genenames.org/data/hgnc_data.php?hgnc_id=5974http://www.uniprot.org/uniprot/P78552http://www.genenames.org/data/hgnc_data.php?hgnc_id=5978http://www.genenames.org/data/hgnc_data.php?hgnc_id=5978http://www.uniprot.org/uniprot/Q13261http://www.genenames.org/data/hgnc_data.php?hgnc_id=6006http://www.genenames.org/data/hgnc_data.php?hgnc_id=6006http://www.uniprot.org/uniprot/Q9HBE5http://www.genenames.org/data/hgnc_data.php?hgnc_id=14281http://www.genenames.org/data/hgnc_data.php?hgnc_id=14281http://www.uniprot.org/uniprot/Q9HC73http://www.guidetopharmacology.org/index.jsphttp://onlinelibrary.wiley.com/doi/10.1111/bph.13353/fullhttp://onlinelibrary.wiley.com/doi/10.1111/bph.13353/fullhttp://www.guidetopharmacology.org/index.jsphttp://www.uniprot.org/uniprot/Q9HC73http://www.genenames.org/data/hgnc_data.php?hgnc_id=14281http://www.uniprot.org/uniprot/Q9HBE5http://www.genenames.org/data/hgnc_data.php?hgnc_id=6006http://www.uniprot.org/uniprot/Q13261http://www.genenames.org/data/hgnc_data.php?hgnc_id=5978http://www.uniprot.org/uniprot/P78552http://www.genenames.org/data/hgnc_data.php?hgnc_id=5974http://www.uniprot.org/uniprot/Q01113http://www.genenames.org/data/hgnc_data.php?hgnc_id=6030http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1704http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1703http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1702http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1700http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1699http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7574http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6879http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6880http://www.uniprot.org/uniprot/P16871http://www.genenames.org/data/hgnc_data.php?hgnc_id=6024http://www.uniprot.org/uniprot/P24394http://www.genenames.org/data/hgnc_data.php?hgnc_id=6015http://www.uniprot.org/uniprot/P31785http://www.genenames.org/data/hgnc_data.php?hgnc_id=6010http://www.uniprot.org/uniprot/P14784http://www.genenames.org/data/hgnc_data.php?hgnc_id=6009http://www.uniprot.org/uniprot/P01589http://www.genenames.org/data/hgnc_data.php?hgnc_id=6008http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1698http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1697http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2303http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1696http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1695http://www.uniprot.org/uniprot/P35225http://www.genenames.org/data/hgnc_data.php?hgnc_id=5973http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4980http://www.uniprot.org/uniprot/Q969D9http://www.genenames.org/data/hgnc_data.php?hgnc_id=30743http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5083http://www.uniprot.org/uniprot/Q9HBE4http://www.genenames.org/data/hgnc_data.php?hgnc_id=6005http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4987http://www.uniprot.org/uniprot/P40933http://www.genenames.org/data/hgnc_data.php?hgnc_id=5977http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4981http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1698http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1704http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1703http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2303http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2303http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1702http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1696http://www.uniprot.org/uniprot/Q14627http://www.genenames.org/data/hgnc_data.php?hgnc_id=5975http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2305http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2304http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2302http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1701


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Overview: The IL-3 receptor family signal through a receptor complex comprising of a ligand-specific α subunit and a common β chain (CSF2RB, P32927), which is associated with Jak2 and signalsprimarily through Stat5.

Nomenclature Interleukin-3 receptor Interleukin-5 receptor Granulocyte macrophage colony-stimulating factor receptor

Subunits Interleukin 3 receptor, α subunit(Ligand-binding subunit),Cytokine receptor common β subunit(Other subunit)

Interleukin 5 receptor, α subunit(Ligand-binding subunit),Cytokine receptor common β subunit(Other subunit)

GM-CSF receptor, α subunit (Ligand-binding subunit),Cytokine receptor common β subunit (Other subunit)

Endogenousagonists

IL-3 (IL3, P08700) IL-5 (IL5, P05113) G-CSF (CSF3, P09919), GM-CSF (CSF2, P04141)

Selectiveantagonists

– YM90709 [133] –

Subunits

Nomenclature Interleukin 3 receptor, α subunit Interleukin 5 receptor, α subunit GM-CSF receptor, α subunit Cytokine receptor common β subunit

HGNC, UniProt IL3RA, P26951 IL5RA, Q01344 CSF2RA, P15509 CSF2RB , P32927

Endogenous agonists IL-3 (IL3, P08700) IL-5 (IL5, P05113) GM-CSF (CSF2, P04141) –

Antibodies – benralizumab (Binding) (p K d 8.7) [93] mavrilimumab (Binding) (pIC50 9.9) [29] –


Overview: The IL-6 receptor family signal through a ternary receptor complex consisting of the cognate receptor and either the IL-6 signal transducer gp130 ( IL6ST , P40189) or the oncostatin M-specificreceptor, β subunit (OSMR, Q99650), which then activates the JAK/STAT, Ras/Raf/MAPK and PI 3-kinase/PKB signalling modules. Unusually amongst the cytokine receptors, the CNTF receptor is aglycerophosphatidylinositol-linked protein.


http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=306http://www.uniprot.org/uniprot/P32927http://www.uniprot.org/uniprot/P32927http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2307http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2308http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2309http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1705http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1705http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1705http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2306http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2306http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2306http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1706http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1706http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1706http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2306http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2306http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2306http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1707http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1707http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1707http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2306http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2306http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2306http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4994http://www.genenames.org/data/hgnc_data.php?hgnc_id=6011http://www.genenames.org/data/hgnc_data.php?hgnc_id=6011http://www.uniprot.org/uniprot/P08700http://www.uniprot.org/uniprot/P08700http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4997http://www.genenames.org/data/hgnc_data.php?hgnc_id=6016http://www.genenames.org/data/hgnc_data.php?hgnc_id=6016http://www.genenames.org/data/hgnc_data.php?hgnc_id=6016http://www.uniprot.org/uniprot/P05113http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4934http://www.genenames.org/data/hgnc_data.php?hgnc_id=2438http://www.genenames.org/data/hgnc_data.php?hgnc_id=2438http://www.genenames.org/data/hgnc_data.php?hgnc_id=2438http://www.uniprot.org/uniprot/P09919http://www.uniprot.org/uniprot/P09919http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4942http://www.genenames.org/data/hgnc_data.php?hgnc_id=2434http://www.genenames.org/data/hgnc_data.php?hgnc_id=2434http://www.genenames.org/data/hgnc_data.php?hgnc_id=2434http://www.uniprot.org/uniprot/P04141http://www.uniprot.org/uniprot/P04141http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5090http://www.ncbi.nlm.nih.gov/pubmed/12469943?dopt=AbstractPlushttp://www.ncbi.nlm.nih.gov/pubmed/12469943?dopt=AbstractPlushttp://www.ncbi.nlm.nih.gov/pubmed/12469943?dopt=AbstractPlushttp://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1705http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1705http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1705http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1706http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1706http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1706http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1707http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1707http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1707http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2306http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2306http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2306http://www.genenames.org/data/hgnc_data.php?hgnc_id=6012http://www.genenames.org/data/hgnc_data.php?hgnc_id=6012http://www.uniprot.org/uniprot/P26951http://www.genenames.org/data/hgnc_data.php?hgnc_id=6017http://www.genenames.org/data/hgnc_data.php?hgnc_id=6017http://www.uniprot.org/uniprot/Q01344http://www.genenames.org/data/hgnc_data.php?hgnc_id=2435http://www.genenames.org/data/hgnc_data.php?hgnc_id=2435http://www.uniprot.org/uniprot/P15509http://www.genenames.org/data/hgnc_data.php?hgnc_id=2436http://www.genenames.org/data/hgnc_data.php?hgnc_id=2436http://www.uniprot.org/uniprot/P32927http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4994http://www.genenames.org/data/hgnc_data.php?hgnc_id=6011http://www.genenames.org/data/hgnc_data.php?hgnc_id=6011http://www.genenames.org/data/hgnc_data.php?hgnc_id=6011http://www.uniprot.org/uniprot/P08700http://www.uniprot.org/uniprot/P08700http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4997http://www.genenames.org/data/hgnc_data.php?hgnc_id=6016http://www.genenames.org/data/hgnc_data.php?hgnc_id=6016http://www.uniprot.org/uniprot/P05113http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4942http://www.genenames.org/data/hgnc_data.php?hgnc_id=2434http://www.genenames.org/data/hgnc_data.php?hgnc_id=2434http://www.genenames.org/data/hgnc_data.php?hgnc_id=2434http://www.uniprot.org/uniprot/P04141http://www.uniprot.org/uniprot/P04141http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7674http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7785http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=307http://www.uniprot.org/uniprot/P40189http://www.uniprot.org/uniprot/Q99650http://www.guidetopharmacology.org/index.jsphttp://onlinelibrary.wiley.com/doi/10.1111/bph.13353/fullhttp://onlinelibrary.wiley.com/doi/10.1111/bph.13353/fullhttp://www.guidetopharmacology.org/index.jsphttp://www.uniprot.org/uniprot/Q99650http://www.uniprot.org/uniprot/P40189http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=307http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7785http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7674http://www.uniprot.org/uniprot/P04141http://www.genenames.org/data/hgnc_data.php?hgnc_id=2434http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4942http://www.uniprot.org/uniprot/P05113http://www.genenames.org/data/hgnc_data.php?hgnc_id=6016http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4997http://www.uniprot.org/uniprot/P08700http://www.genenames.org/data/hgnc_data.php?hgnc_id=6011http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4994http://www.uniprot.org/uniprot/P32927http://www.genenames.org/data/hgnc_data.php?hgnc_id=2436http://www.uniprot.org/uniprot/P15509http://www.genenames.org/data/hgnc_data.php?hgnc_id=2435http://www.uniprot.org/uniprot/Q01344http://www.genenames.org/data/hgnc_data.php?hgnc_id=6017http://www.uniprot.org/uniprot/P26951http://www.genenames.org/data/hgnc_data.php?hgnc_id=6012http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2306http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1707http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1706http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1705http://www.ncbi.nlm.nih.gov/pubmed/12469943?dopt=AbstractPlushttp://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5090http://www.uniprot.org/uniprot/P04141http://www.genenames.org/data/hgnc_data.php?hgnc_id=2434http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4942http://www.uniprot.org/uniprot/P09919http://www.genenames.org/data/hgnc_data.php?hgnc_id=2438http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4934http://www.uniprot.org/uniprot/P05113http://www.genenames.org/data/hgnc_data.php?hgnc_id=6016http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4997http://www.uniprot.org/uniprot/P08700http://www.genenames.org/data/hgnc_data.php?hgnc_id=6011http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4994http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2306http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1707http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2306http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1706http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2306http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1705http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2309http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2308http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2307http://www.uniprot.org/uniprot/P32927http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=306


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Nomenclature Interleukin-6 receptor Interleukin-11 receptor Interleukin-31 receptor Ciliary neutrophic factor receptor

Subunits Interleukin-6 receptor, α subunit(Ligand-binding subunit),Interleukin-6 receptor, β subunit (Other subunit)

Interleukin-11 receptor, α subunit(Ligand-binding subunit),Interleukin-6 receptor, β subunit (Other subunit)

Interleukin-31 receptor, α subunit(Ligand-binding subunit),Oncostatin M-specific receptor, β subunit(Other subunit)

Leukemia inhibitory factor receptor (Other subunit), Interleukin-6 receptor, β subunit,Ciliary neurotrophic factor receptor α subunit(Ligand-binding subunit)

Endogenousagonists

IL-6 (IL6, P05231) IL-11 (IL11, P20809) IL-31 (IL31, Q6EBC2) CRCF1/CLCF1 heterodimer (CLCF1 CRLF1,O75462 Q9UBD9),ciliary neurotrophic factor (CNTF , P26441)

Agonists – oprelvekin – –

Antibodies tocilizumab (Binding) (p K d 8.6) – – –

Nomenclature Leptin receptor Leukemia inhibitory factor receptor Oncostatin-M receptor Interleukin-27 receptor

HGNC, UniProt LEPR, P48357 – – –

Subunits – Leukemia inhibitory factor receptor (Ligand-binding subunit),Interleukin-6 receptor, β subunit (Other subunit)

Interleukin-6 receptor, β subunit (Other subunit),Oncostatin M-specific receptor, β subunit(Ligand-binding subunit)

Interleukin-6 receptor, β subunit(Other subunit),Interleukin 27 receptor, alpha(Ligand-binding subunit)

Endogenous agonists leptin (LEP , P41159) LIF (LIF , P15018), cardiotrophin-1 (CTF1,Q16619), oncostatin M (OSM , P13725)

oncostatin M (OSM , P13725) IL-27 (EBI3 IL27 , Q14213Q8NEV9)

Subunits

Nomenclature Interleukin-6 receptor, α subunit Interleukin-6 receptor, β subunit Interleukin-11 receptor, α subunit Interleukin 27 receptor, alpha

HGNC, UniProt IL6R

, P08887 IL6ST

, P40189 IL11RA

, Q14626 IL27RA

, Q6UWB1 Antibodies sarilumab (Binding) (p K d

10.6–11.1) [171]– – –

Nomenclature Interleukin-31 receptor, α subunit Ciliary neurotrophic factor receptor α subunit Leukemia inhibitory factor receptor Oncostatin M-specific receptor, β subunit

HGNC, UniProt IL31RA, Q8NI17 CNTFR, P26992 LIFR, P42702 OSMR, Q99650


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ctDisplayForward?objectId=2310


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Overview: IL-12 receptors are a subfamily of the IL-6 receptor family. IL12RB1 is shared between receptors for IL-12 and IL-23; the functional agonist at IL-12 receptors is a heterodimer of IL-12A/IL-12B,while that for IL-23 receptors is a heterodimer of IL-12B/IL-23A.

Nomenclature Interleukin-12 receptor Interleukin-23 receptor Interleukin-12 receptor, β1subunit

Interleukin-12 receptor, β2subunit

Interleukin 23 receptor

HGNC, UniProt – – IL12RB1, P42701 IL12RB2, Q99665 IL23R, Q5VWK5

Subunits Interleukin-12 receptor, β2 subunit(Other subunit),Interleukin-12 receptor, β1 subunit(Ligand-binding subunit)

Interleukin 23 receptor (Ligand-bindingsubunit),Interleukin-12 receptor, β1 subunit(Ligand-binding subunit)

– – –

Endogenous agonists IL-12 (IL12A IL12B , P29459 P29460) IL-23 (IL12B IL23A, P29460) – – –

Prolactin receptor familyCatalytic receptors

Cytokine receptor family

Prolactin receptor family

Overview: Prolactin family receptors form homodimers in the presence of their respective ligands, associate exclusively with Jak2 and signal via Stat5.

Nomenclature Eythropoietin receptor Granulocyte colony-stimulating factor receptor

Growth hormone receptor Prolactin receptor Thrombopoietin receptor

HGNC, UniProt EPOR, P19235 CSF3R, Q99062 GHR, P10912 PRLR, P16471 MPL, P40238

Endogenous agonists erythropoietin (EPO, P01588)

(Selective) (pIC50 11.1) [48]

G-CSF (CSF3, P09919) growth hormone 1 (GH1,

P01241), growth hormone 2(GH2, P01242)

choriomammotropin (CSH1 CSH2,

P01243),chorionic somatomammotropinhormone-like 1(CSHL1, Q14406), prolactin (PRL,P01236)

thrombopoietin (THPO, P40225)

Agonists peginesatide (pIC50 10.4) [48] pegfilgrastim – – romiplostim

Selective agonists – – – – eltrombopag (pEC50 7.4) [119]

Antagonists – – pegvisomant [180] – –

Searchable database: http://www.guidetopharmacology.org/index.jsp Prolactin receptor family 5985Full Contents of ConciseGuide: http://onlinelibrary.wiley.com/doi/10.1111/bph.13353/full

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=308http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2292http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2293http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1715http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1715http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1715http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1715http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1716http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1716http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1716http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1716http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1717http://www.genenames.org/data/hgnc_data.php?hgnc_id=5971http://www.genenames.org/data/hgnc_data.php?hgnc_id=5971http://www.uniprot.org/uniprot/P42701http://www.genenames.org/data/hgnc_data.php?hgnc_id=5972http://www.genenames.org/data/hgnc_data.php?hgnc_id=5972http://www.uniprot.org/uniprot/Q99665http://www.genenames.org/data/hgnc_data.php?hgnc_id=19100http://www.genenames.org/data/hgnc_data.php?hgnc_id=19100http://www.uniprot.org/uniprot/Q5VWK5http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1716http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1716http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1716http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1715http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1715http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1715http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1717http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1715http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1715http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1715http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4977http://www.genenames.org/data/hgnc_data.php?hgnc_id=5969http://www.genenames.org/data/hgnc_data.php?hgnc_id=5969http://www.genenames.org/data/hgnc_data.php?hgnc_id=5970http://www.genenames.org/data/hgnc_data.php?hgnc_id=5970http://www.uniprot.org/uniprot/P29459http://www.uniprot.org/uniprot/P29460http://www.uniprot.org/uniprot/P29460http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4978http://www.genenames.org/data/hgnc_data.php?hgnc_id=5970http://www.genenames.org/data/hgnc_data.php?hgnc_id=15488http://www.genenames.org/data/hgnc_data.php?hgnc_id=15488http://www.uniprot.org/uniprot/P29460http://www.uniprot.org/uniprot/P29460http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=309http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1718http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1719http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1719http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1720http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1721http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1722http://www.genenames.org/data/hgnc_data.php?hgnc_id=3416http://www.genenames.org/data/hgnc_data.php?hgnc_id=3416http://www.uniprot.org/uniprot/P19235http://www.genenames.org/data/hgnc_data.php?hgnc_id=2439http://www.genenames.org/data/hgnc_data.php?hgnc_id=2439http://www.uniprot.org/uniprot/Q99062http://www.genenames.org/data/hgnc_data.php?hgnc_id=4263http://www.genenames.org/data/hgnc_data.php?hgnc_id=4263http://www.uniprot.org/uniprot/P10912http://www.genenames.org/data/hgnc_data.php?hgnc_id=9446http://www.genenames.org/data/hgnc_data.php?hgnc_id=9446http://www.uniprot.org/uniprot/P16471http://www.genenames.org/data/hgnc_data.php?hgnc_id=7217http://www.genenames.org/data/hgnc_data.php?hgnc_id=7217http://www.uniprot.org/uniprot/P40238http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4921http://www.genenames.org/data/hgnc_data.php?hgnc_id=3415http://www.genenames.org/data/hgnc_data.php?hgnc_id=3415http://www.genenames.org/data/hgnc_data.php?hgnc_id=3415http://www.uniprot.org/uniprot/P01588http://www.uniprot.org/uniprot/P01588http://www.ncbi.nlm.nih.gov/pubmed/16982323?dopt=AbstractPlushttp://www.ncbi.nlm.nih.gov/pubmed/16982323?dopt=AbstractPlushttp://www.ncbi.nlm.nih.gov/pubmed/16982323?dopt=AbstractPlushttp://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4934http://www.genenames.org/data/hgnc_data.php?hgnc_id=2438http://www.genenames.org/data/hgnc_data.php?hgnc_id=2438http://www.genenames.org/data/hgnc_data.php?hgnc_id=2438http://www.uniprot.org/uniprot/P09919http://www.uniprot.org/uniprot/P09919http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4943http://www.genenames.org/data/hgnc_data.php?hgnc_id=4261http://www.genenames.org/data/hgnc_data.php?hgnc_id=4261http://www.genenames.org/data/hgnc_data.php?hgnc_id=4261http://www.uniprot.org/uniprot/P01241http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4944http://www.genenames.org/data/hgnc_data.php?hgnc_id=4262http://www.genenames.org/data/hgnc_data.php?hgnc_id=4262http://www.uniprot.org/uniprot/P01242http://www.uniprot.org/uniprot/P01242http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4893http://www.genenames.org/data/hgnc_data.php?hgnc_id=2440http://www.genenames.org/data/hgnc_data.php?hgnc_id=2440http://www.genenames.org/data/hgnc_data.php?hgnc_id=2441http://www.genenames.org/data/hgnc_data.php?hgnc_id=2441http://www.uniprot.org/uniprot/P01243http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4894http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4894http://www.genenames.org/data/hgnc_data.php?hgnc_id=2442http://www.genenames.org/data/hgnc_data.php?hgnc_id=2442http://www.genenames.org/data/hgnc_data.php?hgnc_id=2442http://www.uniprot.org/uniprot/Q14406http://www.uniprot.org/uniprot/Q14406http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5049http://www.genenames.org/data/hgnc_data.php?hgnc_id=9445http://www.genenames.org/data/hgnc_data.php?hgnc_id=9445http://www.genenames.org/data/hgnc_data.php?hgnc_id=9445http://www.uniprot.org/uniprot/P01236http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5063http://www.genenames.org/data/hgnc_data.php?hgnc_id=11795http://www.genenames.org/data/hgnc_data.php?hgnc_id=11795http://www.genenames.org/data/hgnc_data.php?hgnc_id=11795http://www.uniprot.org/uniprot/P40225http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7447http://www.ncbi.nlm.nih.gov/pubmed/16982323?dopt=AbstractPlushttp://www.ncbi.nlm.nih.gov/pubmed/16982323?dopt=AbstractPlushttp://www.ncbi.nlm.nih.gov/pubmed/16982323?dopt=AbstractPlushttp://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6969http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6974http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6961http://www.ncbi.nlm.nih.gov/pubmed/18783949?dopt=AbstractPlushttp://www.ncbi.nlm.nih.gov/pubmed/18783949?dopt=AbstractPlushttp://www.ncbi.nlm.nih.gov/pubmed/18783949?dopt=AbstractPlushttp://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7485http://www.ncbi.nlm.nih.gov/pubmed/10770982?dopt=AbstractPlushttp://www.ncbi.nlm.nih.gov/pubmed/10770982?dopt=AbstractPlushttp://www.ncbi.nlm.nih.gov/pubmed/10770982?dopt=AbstractPlushttp://www.guidetopharmacology.org/index.jsphttp://onlinelibrary.wiley.com/doi/10.1111/bph.13353/fullhttp://onlinelibrary.wiley.com/doi/10.1111/bph.13353/fullhttp://www.guidetopharmacology.org/index.jsphttp://www.ncbi.nlm.nih.gov/pubmed/10770982?dopt=AbstractPlushttp://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7485http://www.ncbi.nlm.nih.gov/pubmed/18783949?dopt=AbstractPlushttp://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6961http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6974http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6969http://www.ncbi.nlm.nih.gov/pubmed/16982323?dopt=AbstractPlushttp://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7447http://www.uniprot.org/uniprot/P40225http://www.genenames.org/data/hgnc_data.php?hgnc_id=11795http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5063http://www.uniprot.org/uniprot/P01236http://www.genenames.org/data/hgnc_data.php?hgnc_id=9445http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5049http://www.uniprot.org/uniprot/Q14406http://www.genenames.org/data/hgnc_data.php?hgnc_id=2442http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4894http://www.uniprot.org/uniprot/P01243http://www.genenames.org/data/hgnc_data.php?hgnc_id=2441http://www.genenames.org/data/hgnc_data.php?hgnc_id=2440http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4893http://www.uniprot.org/uniprot/P01242http://www.genenames.org/data/hgnc_data.php?hgnc_id=4262http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4944http://www.uniprot.org/uniprot/P01241http://www.genenames.org/data/hgnc_data.php?hgnc_id=4261http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4943http://www.uniprot.org/uniprot/P09919http://www.genenames.org/data/hgnc_data.php?hgnc_id=2438http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4934http://www.ncbi.nlm.nih.gov/pubmed/16982323?dopt=AbstractPlushttp://www.uniprot.org/uniprot/P01588http://www.genenames.org/data/hgnc_data.php?hgnc_id=3415http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4921http://www.uniprot.org/uniprot/P40238http://www.genenames.org/data/hgnc_data.php?hgnc_id=7217http://www.uniprot.org/uniprot/P16471http://www.genenames.org/data/hgnc_data.php?hgnc_id=9446http://www.uniprot.org/uniprot/P10912http://www.genenames.org/data/hgnc_data.php?hgnc_id=4263http://www.uniprot.org/uniprot/Q99062http://www.genenames.org/data/hgnc_data.php?hgnc_id=2439http://www.uniprot.org/uniprot/P19235http://www.genenames.org/data/hgnc_data.php?hgnc_id=3416http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1722http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1721http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1720http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1719http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1718http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=309http://www.uniprot.org/uniprot/P29460http://www.genenames.org/data/hgnc_data.php?hgnc_id=15488http://www.genenames.org/data/hgnc_data.php?hgnc_id=5970http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4978http://www.uniprot.org/uniprot/P29460http://www.uniprot.org/uniprot/P29459http://www.genenames.org/data/hgnc_data.php?hgnc_id=5970http://www.genenames.org/data/hgnc_data.php?hgnc_id=5969http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4977http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1715http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1717http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1715http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1716http://www.uniprot.org/uniprot/Q5VWK5http://www.genenames.org/data/hgnc_data.php?hgnc_id=19100http://www.uniprot.org/uniprot/Q99665http://www.genenames.org/data/hgnc_data.php?hgnc_id=5972http://www.uniprot.org/uniprot/P42701http://www.genenames.org/data/hgnc_data.php?hgnc_id=5971http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1717http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1716http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1715http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2293http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2292http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=308


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Interferon receptor familyCatalytic receptors Cytokine receptor family Interferon receptor family

Overview: The interferon receptor family includes receptors fortype I (α, β and ) and type II (γ ) interferons. There are at least13 differentgenesencoding IFN-α subunits in a clusteron human

chromosome 9p22: α1 ( IFNA1, P01562), α2 ( IFNA2, P01563), α4( IFNA4, P05014), α5 ( IFNA5, P01569), α6 ( IFNA6, P05013), α7( IFNA7 , P01567), α8 ( IFNA8, P32881), α10 ( IFNA10, P01566), α13

( IFNA13, P01562), α14 ( IFNA14, P01570), α16 ( IFNA16, P05015),α17 ( IFNA17 , P01571) and α21 ( IFNA21, P01568).

Nomenclature Interferon-α/β receptor Interferon-γ receptor

Subunits Interferon α/β receptor 2 (Other subunit), interferon α/β receptor 1 (Ligand-bindingsubunit)

Interferon γ receptor 2 (Other subunit), Interferon γ receptor 1 (Ligand-bindingsubunit)

Endogenousagonists

IFN-α1/13 (IFNA1 IFNA13, P01562), IFN-α10 (IFNA10, P01566), IFN-α14 (IFNA14,P01570), IFN-α16 (IFNA16, P05015), IFN-α17 (IFNA17 , P01571), IFN-α2 (IFNA2,P01563), IFN-α21 (IFNA21, P01568), IFN-α4 (IFNA4, P05014), IFN-α5 (IFNA5,P01569), IFN-α6 (IFNA6, P05013), IFN-α7 (IFNA7 , P01567), IFN-α8 (IFNA8, P32881),IFN-β (IFNB1, P01574), IFN-

(IFNK , Q9P0W0), IFN-

(IFNW1, P05000)

IFN-γ (IFNG, P01579)

Selective agonists peginterferon alfa-2b [191] –

Subunits

Nomenclature interferon α/β receptor 1 Interferon α/β receptor 2 Interferon γ receptor 1 Interferon γ receptor 2

HGNC, UniProt IFNAR1, P17181 IFNAR2, P48551 IFNGR1, P15260 IFNGR2, P38484

Selective agonists peginterferon alfa-2b [191] – – –

Antibodies anifrolumab (Binding) (p K d 10) [21] – – –

Searchable database: http://www.guidetopharmacology.org/index.jsp Interferon receptor family 5986Full Contents of ConciseGuide: http://onlinelibrary.wiley.com/doi/10.1111/bph.13353/full

http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=310http://www.uniprot.org/uniprot/P01562http://www.uniprot.org/uniprot/P01563http://www.uniprot.org/uniprot/P01563http://www.uniprot.org/uniprot/P05014http://www.uniprot.org/uniprot/P05014http://www.uniprot.org/uniprot/P01569http://www.uniprot.org/uniprot/P01569http://www.uniprot.org/uniprot/P05013http://www.uniprot.org/uniprot/P05013http://www.uniprot.org/uniprot/P01567http://www.uniprot.org/uniprot/P32881http://www.uniprot.org/uniprot/P01566http://www.uniprot.org/uniprot/P01566http://www.uniprot.org/uniprot/P01562http://www.uniprot.org/uniprot/P01570http://www.uniprot.org/uniprot/P01570http://www.uniprot.org/uniprot/P05015http://www.uniprot.org/uniprot/P01571http://www.uniprot.org/uniprot/P01571http://www.uniprot.org/uniprot/P01568http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1898http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1898http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1898http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1898http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1898http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1899http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1899http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1899http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1724http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1724http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1724http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1724http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1724http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1723http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1723http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1723http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1723http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1723http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1726http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1726http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1726http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1725http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1725http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1725http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4955http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4955http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4955http://www.genenames.org/data/hgnc_data.php?hgnc_id=5417http://www.genenames.org/data/hgnc_data.php?hgnc_id=5417http://www.genenames.org/data/hgnc_data.php?hgnc_id=5419http://www.genenames.org/data/hgnc_data.php?hgnc_id=5419http://www.uniprot.org/uniprot/P01562http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4956http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4956http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4956http://www.genenames.org/data/hgnc_data.php?hgnc_id=5418http://www.genenames.org/data/hgnc_data.php?hgnc_id=5418http://www.genenames.org/data/hgnc_data.php?hgnc_id=5418http://www.uniprot.org/uniprot/P01566http://www.uniprot.org/uniprot/P01566http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4957http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4957http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4957http://www.genenames.org/data/hgnc_data.php?hgnc_id=5420http://www.genenames.org/data/hgnc_data.php?hgnc_id=5420http://www.genenames.org/data/hgnc_data.php?hgnc_id=5420http://www.uniprot.org/uniprot/P01570http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4958http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4958http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4958http://www.genenames.org/data/hgnc_data.php?hgnc_id=5421http://www.genenames.org/data/hgnc_data.php?hgnc_id=5421http://www.genenames.org/data/hgnc_data.php?hgnc_id=5421http://www.uniprot.org/uniprot/P05015http://www.uniprot.org/uniprot/P05015http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4959http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4959http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4959http://www.genenames.org/data/hgnc_data.php?hgnc_id=5422http://www.genenames.org/data/hgnc_data.php?hgnc_id=5422http://www.genenames.org/data/hgnc_data.php?hgnc_id=5422http://www.uniprot.org/uniprot/P01571http://www.uniprot.org/uniprot/P01571http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4960http://www.guidetopharmacology.org/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