Top ▲

CD36 molecule

Click here for help

Target id: 3104

Nomenclature: CD36 molecule

Family: CD molecules

Contents:

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
Alphafold P16671 (Hs), Q08857 (Mm)
ChEMBL Target CHEMBL1744526 (Hs), CHEMBL2176845 (Mm)
Ensembl Gene ENSG00000135218 (Hs), ENSMUSG00000002944 (Mm), ENSRNOG00000005906 (Rn)
Entrez Gene 948 (Hs), 12491 (Mm), 29184 (Rn)
Human Protein Atlas ENSG00000135218 (Hs)
KEGG Gene hsa:948 (Hs), mmu:12491 (Mm), rno:29184 (Rn)
OMIM 173510 (Hs)
Pharos P16671 (Hs)
RefSeq Nucleotide NM_000072 (Hs), NM_001159558 (Mm), NM_031561 (Rn)
RefSeq Protein NP_000063 (Hs), NP_001153030 (Mm), NP_113749 (Rn)
UniProtKB P16671 (Hs), Q08857 (Mm)
Wikipedia CD36 (Hs)

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:   null (null)
Immuno Process Associations
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 5 GO processes, IEA only
GO:0032731 positive regulation of interleukin-1 beta production ISS
click arrow to show/hide IEA associations
GO:0032735 positive regulation of interleukin-12 production IEA
GO:0032755 positive regulation of interleukin-6 production IEA
GO:0032760 positive regulation of tumor necrosis factor production IEA
GO:0060907 positive regulation of macrophage cytokine production IEA
Immuno Process:  Immune regulation
GO Annotations:  Associated to 3 GO processes, IEA only
GO:0034121 regulation of toll-like receptor signaling pathway IGI
click arrow to show/hide IEA associations
GO:0060907 positive regulation of macrophage cytokine production IEA
GO:0070892 lipoteichoic acid immune receptor activity IEA
Immuno Process:  Antigen presentation
GO Annotations:  Associated to 11 GO processes, IEA only
GO:0005041 low-density lipoprotein particle receptor activity IMP
GO:0005044 scavenger receptor activity IMP
GO:0006898 receptor-mediated endocytosis IMP
GO:0006911 phagocytosis, engulfment TAS
GO:0031623 receptor internalization ISS
GO:0034381 plasma lipoprotein particle clearance ISS
GO:0034383 low-density lipoprotein particle clearance IMP
GO:0150024 oxidised low-density lipoprotein particle clearance IMP
GO:0150025 oxidised low-density lipoprotein particle receptor activity IMP
click arrow to show/hide IEA associations
GO:0006910 phagocytosis, recognition IEA
GO:0060100 positive regulation of phagocytosis, engulfment IEA
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 2 GO processes, IEA only
GO:0034121 regulation of toll-like receptor signaling pathway IGI
click arrow to show/hide IEA associations
GO:0070892 lipoteichoic acid immune receptor activity IEA
Immuno Process:  Inflammation
GO Annotations:  Associated to 7 GO processes, IEA only
GO:0002532 production of molecular mediator involved in inflammatory response TAS
GO:0006911 phagocytosis, engulfment TAS
GO:0034121 regulation of toll-like receptor signaling pathway IGI
click arrow to show/hide IEA associations
GO:0006910 phagocytosis, recognition IEA
GO:0043277 apoptotic cell clearance IEA
GO:0060100 positive regulation of phagocytosis, engulfment IEA
GO:0070892 lipoteichoic acid immune receptor activity IEA
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

Show »

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 10/06/2023. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=3104.