tumor necrosis factor

Target id: 2635

Nomenclature: tumor necrosis factor

Family: Cytokines and growth factors

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

This target is also described as a ligand entry: tumour necrosis factor membrane formtumour necrosis factor shed form

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 233 6p21.3 TNF tumor necrosis factor
Mouse - 235 17 B1 Tnf tumor necrosis factor
Rat - 235 20p12 Tnf tumor necrosis factor
Previous and Unofficial Names
DIF
TNF-alpha
TNFSF2
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GeneCards
GenitoUrinary Development Molecular Anatomy Project
InterPro
KEGG Gene
NeXtProt
OMIM
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene Hs.
UniProtKB
Wikipedia

Download all structure-activity data for this target as a CSV file

Antagonists
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Affinity Units Reference
etanercept Hs Inhibition - - 1-2
[1-2]
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Affinity Units Reference
infliximab Hs Inhibition 8.7 pKd 3
pKd 8.7 (Kd 1.8x10-9 M) [3]
Description: Binding affinity of antibody cA2 and recombinant human TNFα
adalimumab Hs Inhibition >8.0 pKd 5
pKd >8.0 (Kd <1x10-8 M) [5]
golimumab Hs Inhibition 10.7 pIC50 6
pIC50 10.7 (IC50 1.8x10-11 M) [6]
Description: Affinity for soluble THFα measured by surface plasmon resonance
certolizumab pegol Hs Inhibition - - 4
[4]
Description: Note IC90 value of 3ng/ml is provided
Antibody Comments
See Tracey et al. (2009) for a contemporary review of the mechanisms of action of anti-TNFα therapies (antagonists and antibodies) in immune-mediated inflammatory diseases [7].
Clinically-Relevant Mutations and Pathophysiology
Disease:  Asthma, susceptibility to
Disease Ontology: DOID:2841
OMIM: 600807
Disease:  Cerebral malaria
Synonyms: Malaria, susceptibility to [OMIM: 611162]
Disease Ontology: DOID:14069
OMIM: 611162

References

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1. Feldman M, Taylor P, Paleolog E, Brennan FM, Maini RN. (1998) Anti-TNF alpha therapy is useful in rheumatoid arthritis and Crohn's disease: analysis of the mechanism of action predicts utility in other diseases. Transplant. Proc.30 (8): 4126-7. [PMID:9865320]

2. Goldenberg MM. (1999) Etanercept, a novel drug for the treatment of patients with severe, active rheumatoid arthritis. Clin Ther21 (1): 75-87; discussion 1-2. [PMID:10090426]

3. Le J, Vilcek J, Dadonna P, Ghrayeb J, Knight D, Siegel SA. (1997) Methods of treating TNF-α-mediated Crohn's disease using chimeric anti-TNF antibodies. Patent number: US5656272. Assignee: New York University Medical Center, Centocor, Inc.. Priority date: 18/03/1991. Publication date: 12/08/1997.

4. Nesbitt A, Fossati G, Bergin M, Stephens P, Stephens S, Foulkes R, Brown D, Robinson M, Bourne T. (2007) Mechanism of action of certolizumab pegol (CDP870): in vitro comparison with other anti-tumor necrosis factor alpha agents. Inflamm. Bowel Dis.13 (11): 1323-32. [PMID:17636564]

5. Salfeld JG, Allen DJ, Hoogenboom HRJM, Kaymakcalan Z, Labkovsky B, Mankovich JA, McGuinness BT, Roberts AJ, Sakorafas P, Schoenhaut D. (2001) Human antibodies that bind human TNFα. Patent number: US6258562. Assignee: Basf Aktiengesellschaft. Priority date: 09/02/1996. Publication date: 10/07/2001.

6. Shealy DJ, Cai A, Staquet K, Baker A, Lacy ER, Johns L, Vafa O, Gunn 3rd G, Tam S, Sague S et al.. (2010) Characterization of golimumab, a human monoclonal antibody specific for human tumor necrosis factor α. MAbs2 (4): 428-39. [PMID:20519961]

7. Tracey D, Klareskog L, Sasso EH, Salfeld JG, Tak PP. (2008) Tumor necrosis factor antagonist mechanisms of action: a comprehensive review. Pharmacol. Ther.117 (2): 244-79. [PMID:18155297]

How to cite this page

Cytokines and growth factors: tumor necrosis factor. Last modified on 01/04/2015. Accessed on 01/09/2015. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2635.