TLR2 | Toll-like receptor family | IUPHAR/BPS Guide to PHARMACOLOGY

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TLR2

target has curated data in GtoImmuPdb

Target id: 1752

Nomenclature: TLR2

Family: Toll-like receptor family

Contents:

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 766 4q31.3 TLR2 toll like receptor 2
Mouse - 760 3 37.40 cM Tlr2 toll-like receptor 2
Rat - - 2q34 Tlr2 toll-like receptor 2
Previous and Unofficial Names
CD282 | TIL4 | toll-like receptor 2 | Ly105
Database Links
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

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] Hs Agonist 7.6 pKi 4
⤷ pKi 7.6 (Ki 2.5x10-8 M) [4]
diprovocim-1 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 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 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 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 10 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: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 20 GO processes
GO:0002374 cytokine secretion involved in immune response IMP
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:0042535 positive regulation of tumor necrosis factor biosynthetic process IMP
GO:0050715 positive regulation of cytokine secretion IGI
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
GO:1904469 positive regulation of tumor necrosis factor secretion IGI
click arrow to show/hide IEA associations
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
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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