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immunoglobulin heavy constant epsilon

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 2741

Nomenclature: immunoglobulin heavy constant epsilon

Family: Immunoglobulins

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 428 14q32.33 IGHE immunoglobulin heavy constant epsilon
Mouse - - 12 F1 Igh-7 immunoglobulin heavy chain 7 (heavy chain of IgE)
Previous and Unofficial Names Click here for help
Ighe
Database Links Click here for help
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
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Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  M1' peptide from IgE bound by humanized antibody 47H4 Fab
PDB Id:  3HR5
Ligand:  quilizumab
Resolution:  2.4Å
Species:  Mouse
References:  2

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

Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
ligelizumab Peptide Primary target of this compound Immunopharmacology Ligand Hs Binding 9.9 – 11.8 pKd 1,4
pKd 9.9 – 11.8 (Kd 1.39x10-10 – 1.47x10-12 M) [1,4]
Description: In vitro binding affinity
quilizumab Peptide Primary target of this compound Immunopharmacology Ligand Hs Binding 8.8 pKd 5
pKd 8.8 (Kd 1.5x10-9 M) [5]
omalizumab Peptide Approved drug Primary target of this compound Immunopharmacology Ligand Hs Binding 7.6 – 8.2 pKd 1,3
pKd 8.2 (Kd 6.98x10-9 M) [1]
Description: In vitro binding affinity
pKd 7.6 (Kd 2.6x10-8 M) [3]
Description: F(ab) apparent binding affinity of e25 measured by surface plasmon resonance
Immunopharmacology Comments
IgE is being investigated as a molecular target in allergic inflammatory conditions such as asthma, allergic rhinitis and chronic spontaneous urticaria. One anti-IgE monoclonal, omalizumab, has already been approved for use in patients with asthma or chronic spontaneous urticaria. Omalizumab binds to circulating free IgE. The hunt for additional IgE-targeting antibodies is ongoing. Quilizumab, is one such investigational agent that targets the membrane bound IgE (mIgE) which forms the allergen-binding component of the B cell receptor.
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 3 GO processes
GO:0006910 phagocytosis, recognition IBA
GO:0006911 phagocytosis, engulfment IBA
GO:0045087 innate immune response IBA
Immuno Process:  Antigen presentation
GO Annotations:  Associated to 2 GO processes
GO:0006910 phagocytosis, recognition IBA
GO:0006911 phagocytosis, engulfment IBA
Immuno Process:  T cell (activation)
GO Annotations:  Associated to 1 GO processes
GO:0006958 complement activation, classical pathway IBA
Immuno Process:  B cell (activation)
GO Annotations:  Associated to 2 GO processes
GO:0006958 complement activation, classical pathway IBA
GO:0050871 positive regulation of B cell activation IBA
Immuno Process:  Immune regulation
GO Annotations:  Associated to 4 GO processes
GO:0006958 complement activation, classical pathway IBA
GO:0038095 Fc-epsilon receptor signaling pathway TAS
GO:0050853 B cell receptor signaling pathway IBA
GO:0050871 positive regulation of B cell activation IBA
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 1 GO processes
GO:0019221 cytokine-mediated signaling pathway TAS
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 3 GO processes
GO:0038095 Fc-epsilon receptor signaling pathway TAS
GO:0050853 B cell receptor signaling pathway IBA
GO:0050871 positive regulation of B cell activation IBA

References

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1. Arm JP, Bottoli I, Skerjanec A, Floch D, Groenewegen A, Maahs S, Owen CE, Jones I, Lowe PJ. (2014) Pharmacokinetics, pharmacodynamics and safety of QGE031 (ligelizumab), a novel high-affinity anti-IgE antibody, in atopic subjects. Clin Exp Allergy, 44 (11): 1371-85. [PMID:25200415]

2. Brightbill HD, Jeet S, Lin Z, Yan D, Zhou M, Tan M, Nguyen A, Yeh S, Delarosa D, Leong SR et al.. (2010) Antibodies specific for a segment of human membrane IgE deplete IgE-producing B cells in humanized mice. J Clin Invest, 120 (6): 2218-29. [PMID:20458139]

3. Lowman HB, Presta LG, Jardieu PM, Lowe J. (1999) Anti-IgE antibodies and methods of improving polypeptides. Patent number: US5994511. Assignee: Genentech, Inc.. Priority date: 02/07/1997. Publication date: 30/11/1999.

4. Singh S, Foster C, Wu H. (2009) High affinity anti-human IgE antibodies. Patent number: US7531169 B2. Assignee: Tanox, Inc.. Priority date: 01/02/2003. Publication date: 12/05/2009.

5. Wu L, Balazs M, Brightbill H, Chan A, Chen Y, Chuntharapai A, Dennis M, Wong T. (2011) Apoptotic anti-IgE antibodies. Patent number: US8071097 B2. Assignee: Genentech, Inc.. Priority date: 22/03/2007. Publication date: 06/12/2011.

How to cite this page

Immunoglobulins: immunoglobulin heavy constant epsilon. Last modified on 08/05/2017. Accessed on 13/04/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2741.