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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

Contents:

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 O60603 (Hs), Q9QUN7 (Mm)
CATH/Gene3D 3.80.10.10, 3.40.50.10140
ChEMBL Target CHEMBL4163 (Hs), CHEMBL1075106 (Mm)
DrugBank Target O60603 (Hs)
Ensembl Gene ENSG00000137462 (Hs), ENSMUSG00000027995 (Mm), ENSRNOG00000009822 (Rn)
Entrez Gene 7097 (Hs), 24088 (Mm), 310553 (Rn)
Human Protein Atlas ENSG00000137462 (Hs)
KEGG Gene hsa:7097 (Hs), mmu:24088 (Mm), rno:310553 (Rn)
OMIM 603028 (Hs)
Pharos O60603 (Hs)
UniProtKB O60603 (Hs), Q9QUN7 (Mm)
Wikipedia TLR2 (Hs)

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:  Antigen presentation
GO Annotations:  Associated to 1 GO processes
GO:0050765 negative regulation of phagocytosis ISS
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 5 GO processes
GO:0001875 lipopolysaccharide immune receptor activity TAS
GO:0002224 toll-like receptor signaling pathway IDA
GO:0034134 toll-like receptor 2 signaling pathway IDA
GO:0038124 toll-like receptor TLR6:TLR2 signaling pathway IDA
click arrow to show/hide IEA associations
GO:0001774 microglial cell activation IEA
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 1 GO processes
GO:0032722 positive regulation of chemokine production IDA
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 10 GO processes
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:0071346 cellular response to type II interferon IDA
GO:1903974 positive regulation of cellular response to macrophage colony-stimulating factor stimulus IDA
click arrow to show/hide IEA associations
GO:0032733 positive regulation of interleukin-10 production IEA
Immuno Process:  Immune regulation
GO Annotations:  Associated to 5 GO processes
GO:0001875 lipopolysaccharide immune receptor activity TAS
GO:0002224 toll-like receptor signaling pathway IDA
GO:0034134 toll-like receptor 2 signaling pathway IDA
GO:0038124 toll-like receptor TLR6:TLR2 signaling pathway IDA
GO:0050729 positive regulation of inflammatory response IGI
Immuno Process:  Inflammation
GO Annotations:  Associated to 11 GO processes
GO:0001875 lipopolysaccharide immune receptor activity TAS
GO:0002224 toll-like receptor signaling pathway IDA
GO:0006954 inflammatory response IBA
GO:0034134 toll-like receptor 2 signaling pathway IDA
GO:0038124 toll-like receptor TLR6:TLR2 signaling pathway IDA
GO:0038187 pattern recognition receptor activity IDA
GO:0045087 innate immune response TAS
GO:0050729 positive regulation of inflammatory response IGI
GO:0050765 negative regulation of phagocytosis ISS
GO:0071346 cellular response to type II interferon IDA
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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