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CD36 molecule

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 3104

Nomenclature: CD36 molecule

Family: CD molecules

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 2 472 7q21.11 CD36 CD36 molecule
Mouse 2 472 5 8.11 cM Cd36 CD36 molecule
Rat 2 472 4q11 Cd36 CD36 molecule
Previous and Unofficial Names Click here for help
collagen type I receptor, thrombospondin receptor | platelet glycoprotein 4 | SCARB3 | fatty acid translocase (FAT)
Database Links Click here for help
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia

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

Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
peptide 1 [PMID: 31774287] Small molecule or natural product Immunopharmacology Ligand Rn Antagonist 7.1 pKd 1
pKd 7.1 (Kd 8x10-8 M) [1]
Description: Binding affinity to rat CD36 in isolated membranes purified from rat heart. Measured in a competition assay vs. the photoactivated agonist [125I]-Tyr-Bpa-Ala-hexarelin.
compound 3c [PMID: 30360354] Peptide Immunopharmacology Ligand Rn Antagonist 5.6 pIC50 3
pIC50 5.6 (IC50 2.53x10-6 M) [3]
Description: Measuring displacement of [125I]-Tyr-Bpa-Ala-hexarelin tracer from CD36 on purified membranes from rat heart in a radioligand binding assay.
peptide 5A Peptide Hs Antagonist - - 4
[4]
View species-specific antagonist tables
Immunopharmacology Comments
CD36 expressed by macrophages plays a key role in the recognition and phagocytosis (scavenging) of multiple ligands that are recognised either as damage-associated molecular patterns (DAMPs) released by apoptotic cells, or as potentially dangerous pathogen-associated ligands. CD36 associates with specific Toll-like receptor (TLR) DAMP-detecting heterodimers when bound by certain ligands, and following internalisation of the ligand/CD36/TLR clusters, inflammatory responses (e.g. NF-κB-dependent production of CXCL1, CXCL2, CCL9 and CCL5, NLRP3 inflammasome-mediated IL-1B production, and NF-κB-dependent production of TNF in reponse to microbial diacylated lipopeptide) are triggered. Pharmacological modulation of CD36/TLR signalling is being explored as a strategy to suppress macrophage-driven inflammation [1,5-6]. To date research has focussed on the development of azapeptide and azasulfurylpeptide ligand mimetics, which are designed with minimal liability with regards to neovascularization and with optimised and selective activity towards the CD36-mediated TLR2/6-triggered innate inflammatory response (i.e. pro-inflammatory cytokine and chemokine production in macrophages).
Cell Type Associations
Immuno Cell Type:  Macrophages & monocytes
Cell Ontology Term:   macrophage (CL:0000235)
Physiological Functions Click here for help
CD36 is involved in lipid accumulation, foam cell formation and atherosclerotic lesion development.
Species:  Mouse
Tissue: 
References:  2
Physiological Consequences of Altering Gene Expression Click here for help
CD36 deficient mice are protected against atherosclerosis.
Species:  Mouse
Tissue: 
Technique: 
References:  2

References

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1. Danelius E, Ohm RG, Ahsanullah, Mulumba M, Ong H, Chemtob S, Erdelyi M, Lubell WD. (2019) Dynamic Chirality in the Mechanism of Action of Allosteric CD36 Modulators of Macrophage-Driven Inflammation. J Med Chem, 62 (24): 11071-11079. [PMID:31774287]

2. Febbraio M, Podrez EA, Smith JD, Hajjar DP, Hazen SL, Hoff HF, Sharma K, Silverstein RL. (2000) Targeted disruption of the class B scavenger receptor CD36 protects against atherosclerotic lesion development in mice. J Clin Invest, 105 (8): 1049-56. [PMID:10772649]

3. Proulx C, Picard É, Boeglin D, Pohankova P, Chemtob S, Ong H, Lubell WD. (2012) Azapeptide analogues of the growth hormone releasing peptide 6 as cluster of differentiation 36 receptor ligands with reduced affinity for the growth hormone secretagogue receptor 1a. J Med Chem, 55 (14): 6502-11. [PMID:22712585]

4. Souza AC, Bocharov AV, Baranova IN, Vishnyakova TG, Huang YG, Wilkins KJ, Hu X, Street JM, Alvarez-Prats A, Mullick AE et al.. (2016) Antagonism of scavenger receptor CD36 by 5A peptide prevents chronic kidney disease progression in mice independent of blood pressure regulation. Kidney Int, 89 (4): 809-22. [PMID:26994575]

5. Turcotte S, Mellal K, Chingle R, Mulumba M, Omri S, Dif-Yaiche L, Chemtob S, Ong H, Lubell WD. (2018) Azasulfurylpeptide Modulation of CD36-Mediated Inflammation Without Effect on Neovascularization. Biomedicines, 6 (4). [PMID:30360354]

6. Zhang J, Mulumba M, Ong H, Lubell WD. (2017) Diversity-Oriented Synthesis of Cyclic Azapeptides by A3 -Macrocyclization Provides High-Affinity CD36-Modulating Peptidomimetics. Angew Chem Int Ed Engl, 56 (22): 6284-6288. [PMID:28090719]

How to cite this page

CD molecules: CD36 molecule. Last modified on 10/01/2020. Accessed on 16/04/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=3104.