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TLR2

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 1752

Nomenclature: TLR2

Family: Toll-like receptor family

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 784 4q31.3 TLR2 toll like receptor 2
Mouse 1 784 3 E3 Tlr2 toll-like receptor 2
Rat - - 2q34 Tlr2 toll-like receptor 2
Previous and Unofficial Names Click here for help
CD282 | TIL4 | toll-like receptor 2 | Ly105
Database Links Click here for help
Alphafold
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
UniProtKB
Wikipedia

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

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 13 [PMID: 23098072] Small molecule or natural product Hs Agonist 7.6 pKi 4
pKi 7.6 (Ki 2.5x10-8 M) [4]
diprovocim-1 Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Agonist 10.0 pEC50 5
pEC50 10.0 (EC50 1.1x10-10 M) [5]
Description: Measuring ligand-induced TNF-α release from treated human THP-1 myeloid cells.
defoslimod Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Mm Agonist - - 3
[3]
View species-specific agonist tables
Agonist Comments
The unlabelled parent molecule of compound 13 in the table above (compound 10 in [4]) has a Ki of 11nM.
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
tomaralimab Peptide Immunopharmacology Ligand Mm Binding 7.9 pKd 1
pKd 7.9 (Kd 1.19x10-8 M) [1]
Description: In a BIACORE surface plasmon resonance (SPR) assay.
tomaralimab Peptide Primary target of this compound Immunopharmacology Ligand Hs Binding 7.5 pKd 1
pKd 7.5 (Kd 2.89x10-8 M) [1]
Description: In a BIACORE surface plasmon resonance (SPR) assay.
Immunopharmacology Comments
TLR1/2 and 2/6 heterodimers detect and initiate an immune response to triacylated and diacylated [6] lipopeptides respectively [2]. The synthetic lipopeptides Pam3CSK4 and Pam2CSK4 activate TLR1/2 and 2/6 heterodimers respectively.
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 11 GO processes
GO:0001875 lipopolysaccharide immune receptor activity TAS
GO:0002687 positive regulation of leukocyte migration IMP
GO:0002752 cell surface pattern recognition receptor signaling pathway IMP
GO:0006954 inflammatory response IBA
GO:0038187 pattern recognition receptor activity IDA
GO:0043312 neutrophil degranulation TAS
GO:0045087 innate immune response TAS
GO:0050729 positive regulation of inflammatory response IC
GO:0050765 negative regulation of phagocytosis ISS
GO:0071346 cellular response to interferon-gamma IDA
click arrow to show/hide IEA associations
GO:0001774 microglial cell activation IEA
Immuno Process:  Immune system development
GO Annotations:  Associated to 1 GO processes
GO:0014005 microglia development ISS
Immuno Process:  Immune regulation
GO Annotations:  Associated to 6 GO processes
GO:0001875 lipopolysaccharide immune receptor activity TAS
GO:0002687 positive regulation of leukocyte migration IMP
GO:0002730 regulation of dendritic cell cytokine production IDA
GO:0002752 cell surface pattern recognition receptor signaling pathway IMP
GO:0050729 positive regulation of inflammatory response IC
GO:0060907 positive regulation of macrophage cytokine production IMP
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 16 GO processes
GO:0002730 regulation of dendritic cell cytokine production IDA
GO:0032613 interleukin-10 production IDA
GO:0032640 tumor necrosis factor production ISS
GO:0032695 negative regulation of interleukin-12 production IMP
GO:0032700 negative regulation of interleukin-17 production IMP
GO:0032722 positive regulation of chemokine production IDA
GO:0032728 positive regulation of interferon-beta production ISS
GO:0032735 positive regulation of interleukin-12 production ISS
GO:0032741 positive regulation of interleukin-18 production ISS
GO:0032755 positive regulation of interleukin-6 production IDA
GO:0032757 positive regulation of interleukin-8 production IDA
GO:0032760 positive regulation of tumor necrosis factor production ISS
GO:0060907 positive regulation of macrophage cytokine production IMP
GO:0071346 cellular response to interferon-gamma IDA
GO:1903974 positive regulation of cellular response to macrophage colony-stimulating factor stimulus IDA
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GO:0032733 positive regulation of interleukin-10 production IEA
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 2 GO processes
GO:0002687 positive regulation of leukocyte migration IMP
GO:0032722 positive regulation of chemokine production IDA
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 4 GO processes
GO:0001875 lipopolysaccharide immune receptor activity TAS
GO:0002752 cell surface pattern recognition receptor signaling pathway IMP
GO:0043312 neutrophil degranulation TAS
click arrow to show/hide IEA associations
GO:0001774 microglial cell activation IEA
Physiological Functions Comments
Involved in the pro-inflammatory response to bacterial lipopeptides.
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Breast cancer
Disease Ontology: DOID:1612
OMIM: 114480
Disease:  Colorectal cancer
Disease Ontology: DOID:9256
OMIM: 114500
Disease:  Coronary restenosis
Disease Ontology: DOID:4247
Disease:  Gastric cancer
Synonyms: Stomach cancer
Disease Ontology: DOID:10534
OMIM: 613659
Disease:  Hepatocellular carcinoma
Disease Ontology: DOID:684
OMIM: 114550
Disease:  Leprosy, susceptibility to, 3; LPRS3
Disease Ontology: DOID:1024
OMIM: 246300
Disease:  Lyme disease
Disease Ontology: DOID:11729
Disease:  Mycobacterium tuberculosis, susceptibility to
Disease Ontology: DOID:399
OMIM: 607948
Disease:  Preterm birth
Synonyms: Premature labor [Disease Ontology: DOID:10875]
Disease Ontology: DOID:10875
Disease:  Staphylococcal infection
Synonyms: Staphylococcal infectious disease [Disease Ontology: DOID:98]
Disease Ontology: DOID:98
Disease:  Urinary tract infection
Synonyms: Acute cystitis [Disease Ontology: DOID:13148]
Disease Ontology: DOID:13148

References

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1. Dellacasagrande J. (2011) Humanised antibodies to toll-like receptor 2 and uses thereof. Patent number: WO2011003925. Assignee: Opsona Therapeutics Limited. Priority date: 06/07/2009. Publication date: 13/01/2011.

2. Farhat K, Riekenberg S, Heine H, Debarry J, Lang R, Mages J, Buwitt-Beckmann U, Röschmann K, Jung G, Wiesmüller KH et al.. (2008) Heterodimerization of TLR2 with TLR1 or TLR6 expands the ligand spectrum but does not lead to differential signaling. J Leukoc Biol, 83 (3): 692-701. [PMID:18056480]

3. Garay RP, Viens P, Bauer J, Normier G, Bardou M, Jeannin JF, Chiavaroli C. (2007) Cancer relapse under chemotherapy: why TLR2/4 receptor agonists can help. Eur J Pharmacol, 563 (1-3): 1-17. [PMID:17383632]

4. Huynh AS, Chung WJ, Cho HI, Moberg VE, Celis E, Morse DL, Vagner J. (2012) Novel toll-like receptor 2 ligands for targeted pancreatic cancer imaging and immunotherapy. J Med Chem, 55 (22): 9751-62. [PMID:23098072]

5. Morin MD, Wang Y, Jones BT, Mifune Y, Su L, Shi H, Moresco EMY, Zhang H, Beutler B, Boger DL. (2018) Diprovocims: A New and Exceptionally Potent Class of Toll-like Receptor Agonists. J Am Chem Soc, 140 (43): 14440-14454. [PMID:30272974]

6. Nakao Y, Funami K, Kikkawa S, Taniguchi M, Nishiguchi M, Fukumori Y, Seya T, Matsumoto M. (2005) Surface-expressed TLR6 participates in the recognition of diacylated lipopeptide and peptidoglycan in human cells. J Immunol, 174 (3): 1566-73. [PMID:15661917]

Contributors

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