CD36

gene
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Also known as SCARB3GPIVFATGP4GP3BGPIIIB

Summary

CD36 (CD36 molecule (CD36 blood group), HGNC:1663) is a protein-coding gene on chromosome 7q21.11, encoding Platelet glycoprotein 4 (P16671). Multifunctional glycoprotein that acts as a receptor for a broad range of ligands.

The protein encoded by this gene is the fourth major glycoprotein of the platelet surface and serves as a receptor for thrombospondin in platelets and various cell lines. Since thrombospondins are widely distributed proteins involved in a variety of adhesive processes, this protein may have important functions as a cell adhesion molecule. It binds to collagen, thrombospondin, anionic phospholipids and oxidized LDL. It directly mediates cytoadherence of Plasmodium falciparum parasitized erythrocytes and it binds long chain fatty acids and may function in the transport and/or as a regulator of fatty acid transport. Mutations in this gene cause platelet glycoprotein deficiency. Multiple alternatively spliced transcript variants have been found for this gene.

Source: NCBI Gene 948 — RefSeq curated summary.

At a glance

  • Gene–disease (curated): platelet-type bleeding disorder 10 (Strong, GenCC)
  • GWAS associations: 45
  • Clinical variants (ClinVar): 341 total — 29 pathogenic, 32 likely-pathogenic
  • Phenotypes (HPO): 5
  • Druggable target: yes
  • Dosage sensitivity (ClinGen): haploinsufficiency autosomal recessive, triplosensitivity unscored
  • MANE Select transcript: NM_001001548

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:1663
Approved symbolCD36
NameCD36 molecule (CD36 blood group)
Location7q21.11
Locus typegene with protein product
StatusApproved
AliasesSCARB3, GPIV, FAT, GP4, GP3B, GPIIIB
Ensembl geneENSG00000135218
Ensembl biotypeprotein_coding
OMIM173510
Entrez948

Gene structure

Transcript identifiers

Ensembl transcripts: 120 — 113 protein_coding, 4 protein_coding_CDS_not_defined, 2 retained_intron, 1 nonsense_mediated_decay

ENST00000309881, ENST00000394788, ENST00000413265, ENST00000419819, ENST00000426978, ENST00000428497, ENST00000432207, ENST00000433696, ENST00000435819, ENST00000436384, ENST00000438020, ENST00000441034, ENST00000441109, ENST00000447544, ENST00000464213, ENST00000478292, ENST00000480599, ENST00000482059, ENST00000488048, ENST00000526804, ENST00000534394, ENST00000538969, ENST00000544133, ENST00000648416, ENST00000855923, ENST00000855924, ENST00000855925, ENST00000855926, ENST00000855927, ENST00000855928, ENST00000855929, ENST00000855930, ENST00000855931, ENST00000855932, ENST00000855933, ENST00000855934, ENST00000855935, ENST00000855936, ENST00000855937, ENST00000855938, ENST00000855939, ENST00000855940, ENST00000855941, ENST00000855942, ENST00000855943, ENST00000855944, ENST00000855945, ENST00000855946, ENST00000855947, ENST00000855948, ENST00000855949, ENST00000855950, ENST00000855951, ENST00000855952, ENST00000855953, ENST00000855954, ENST00000855955, ENST00000855956, ENST00000855957, ENST00000855958, ENST00000855959, ENST00000855960, ENST00000855961, ENST00000855962, ENST00000855963, ENST00000855964, ENST00000855965, ENST00000855966, ENST00000956914, ENST00000956915, ENST00000956916, ENST00000956917, ENST00000956918, ENST00000956919, ENST00000956920, ENST00000956921, ENST00000956922, ENST00000956923, ENST00000956924, ENST00000956925, ENST00000956926, ENST00000956927, ENST00000956928, ENST00000956929, ENST00000956930, ENST00000956931, ENST00000956932, ENST00000956933, ENST00000956934, ENST00000956935, ENST00000956936, ENST00000956937, ENST00000956938, ENST00000956939, ENST00000956940, ENST00000956941, ENST00000956942, ENST00000956943, ENST00000956944, ENST00000956945, ENST00000956946, ENST00000956947, ENST00000956948, ENST00000956949, ENST00000956950, ENST00000956951, ENST00000956952, ENST00000956953, ENST00000956954, ENST00000956955, ENST00000956956, ENST00000956957, ENST00000956958, ENST00000956959, ENST00000956960, ENST00000956961, ENST00000956962, ENST00000956963, ENST00000956964, ENST00000956965

RefSeq mRNA: 15 — MANE Select: NM_001001548 NM_000072, NM_001001547, NM_001001548, NM_001127443, NM_001127444, NM_001289908, NM_001289909, NM_001289911, NM_001371074, NM_001371075, NM_001371077, NM_001371078, NM_001371079, NM_001371080, NM_001371081

CCDS: CCDS34673, CCDS78249, CCDS78250, CCDS78251

Canonical transcript exons

ENST00000447544 — 15 exons

ExonStartEnd
ENSE000006986268066644380666489
ENSE000008770678066995380670022
ENSE000008770688067097780671164
ENSE000014201988064608880646181
ENSE000015195788067398380674147
ENSE000019340208067638480679274
ENSE000034631668067277080672843
ENSE000035499228067192280672040
ENSE000036103298067335580673409
ENSE000036593558066440680664497
ENSE000036859038064665280646860
ENSE000037856048066106380661210
ENSE000037859038065654080656700
ENSE000037891318066299080663169
ENSE000038447688063864280638746

Expression profiles

Bgee: expression breadth ubiquitous, 252 present calls, max score 99.61.

FANTOM5 (CAGE): breadth broad, TPM avg 105.2832 / max 8849.2525, expressed in 913 samples.

FANTOM5 promoters (44 alternative TSS)

Promoter IDTPM avgSamples expressed
7930680.3204631
7930711.7376464
793122.654553
792952.1448258
793050.6555130
792930.640983
792910.608480
792890.580873
793030.502259
792900.467171

Top tissues by expression

291 total, by Bgee expression score (0-100, higher = more expressed):

TissueAnatomy IDExpression scoreQuality
adipose tissue of abdominal regionUBERON:000780899.61gold quality
omental fat padUBERON:001041499.60gold quality
monocyteCL:000057699.55gold quality
adipose tissueUBERON:000101399.53gold quality
jejunal mucosaUBERON:000039999.47gold quality
peritoneumUBERON:000235899.44gold quality
heart right ventricleUBERON:000208099.42gold quality
mononuclear cellCL:000084299.33gold quality
subcutaneous adipose tissueUBERON:000219099.28gold quality
left ventricle myocardiumUBERON:000656699.25gold quality
leukocyteCL:000073899.24gold quality
cardiac ventricleUBERON:000208299.20gold quality
heart left ventricleUBERON:000208499.20gold quality
apex of heartUBERON:000209899.09gold quality
skin of hipUBERON:000155499.02gold quality
connective tissueUBERON:000238498.89gold quality
right atrium auricular regionUBERON:000663198.79gold quality
myocardiumUBERON:000234998.77gold quality
cardiac atriumUBERON:000208198.72gold quality
trabecular bone tissueUBERON:000248398.42gold quality
vena cavaUBERON:000408798.42gold quality
hindlimb stylopod muscleUBERON:000425298.41gold quality
heartUBERON:000094898.30gold quality
skeletal muscle tissue of biceps brachiiUBERON:000450298.30gold quality
biceps brachiiUBERON:000150798.23gold quality
cardiac muscle of right atriumUBERON:000337998.23gold quality
skeletal muscle tissue of rectus abdominisUBERON:000451198.16gold quality
colonic epitheliumUBERON:000039798.08gold quality
buccal mucosa cellCL:000233698.07gold quality
duodenumUBERON:000211498.07gold quality

Single-cell (SCXA)

Detected in 23 experiment(s), a significant marker in 20.

ExperimentMarker?Max mean expression
E-GEOD-81383yes5237.96
E-ENAD-20yes2859.10
E-HCAD-24yes2021.64
E-CURD-11yes1889.19
E-MTAB-6701yes1697.95
E-MTAB-10553yes1548.28
E-GEOD-149689yes516.49
E-GEOD-83139yes178.53
E-HCAD-4yes140.82
E-CURD-122yes72.21
E-CURD-112yes65.82
E-HCAD-10yes53.10
E-MTAB-10042yes28.86
E-MTAB-6678yes26.03
E-HCAD-9yes20.59

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

3 targets.

TargetRegulation
CCL5Activation
CXCL1Activation
CXCL2Activation

Upstream regulators (CollecTRI, top): AEBP1, AHR, CEBPA, CEBPB, CEBPG, GLI2, HIF1A, IL13, IL4, KLF2, NFE2L2, NR1H2, NR1H3, NR1H4, NR1I2, NR2C2, POU2F2, PPARA, PPARD, PPARG, RUNX3, SREBF1, STAT1, STAT5A, TCF3, TCF4, TFAP2A, TFAP2B, TNF

miRNA regulators (miRDB)

42 targeting CD36, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-1277-5P100.0073.955056
HSA-MIR-5011-5P100.0083.465820
HSA-MIR-5692B100.0071.322622
HSA-MIR-5692C100.0071.322622
HSA-MIR-548C-3P99.9974.017587
HSA-MIR-150-5P99.9966.691976
HSA-MIR-570-3P99.9672.414910
HSA-MIR-96-5P99.9572.802140
HSA-MIR-6508-5P99.9270.672465
HSA-MIR-1213399.9271.822006
HSA-MIR-1271-5P99.9171.991972
HSA-MIR-106A-5P99.9073.942683
HSA-MIR-4753-3P99.9071.033786
HSA-MIR-17-5P99.8973.832665
HSA-MIR-106B-5P99.8874.722795
HSA-MIR-20A-5P99.8874.762769
HSA-MIR-20B-5P99.8874.012621
HSA-MIR-519D-3P99.8873.972607
HSA-MIR-526B-3P99.8874.062587
HSA-MIR-93-5P99.8873.982606
HSA-MIR-806799.8669.592260
HSA-MIR-629-3P99.8567.991875
HSA-MIR-520F-3P99.8271.321216
HSA-MIR-4713-5P99.7867.801794
HSA-MIR-2116-3P99.7464.32889
HSA-MIR-379-3P99.6969.601524
HSA-MIR-411-3P99.6969.631524
HSA-MIR-211399.5871.221521
HSA-MIR-360999.5269.892587
HSA-MIR-548AH-5P99.5269.732626

Functional genomics

ClinGen dosage: haploinsufficiency 30 (autosomal recessive), triplosensitivity Not yet evaluated (unscored). ClinGen Gene Dosage Map

Literature-anchored findings (GeneRIF, showing 40)

  • novel variants in individuals from malaria-endemic Ghana (PMID:11668637)
  • The metabolic role of CD36 was tested by glucose loading in type I or II CD36 deficiency pts. Changes in triglyceride and glucose metabolism were seen in CD36 deficiency due to impaired fast FA clearance by muscle and increased liver FA uptake. (PMID:11686358)
  • A redox-dependent conformational fraction of CD36, localized in the CD36 C-terminal cysteine-rich region, mediates cytoadherence of Plasmodium falciparum-infected erythrocytes to CD36-expressing cells and is inducible by low toxicity reducing agents. (PMID:11714819)
  • CD36 Pro90Ser mutation is not necessarily related to the insulin resistance syndrome, but is associated with high free fatty acid concentrations in Japanese (PMID:11718687)
  • CD36 deficiency induced by antiretroviral therapy. (PMID:11834946)
  • promoter structure and trans activation by pparalpha and ppargamma ligands (PMID:11867619)
  • Advanced glycation endproducts generated in situ are recognized by CD36, which might contribute to the pathogenesis of diabetic macrovascular complications. (PMID:11872368)
  • identification of terminal six amino acids of carboxy cytoplasmic tail as a functional domain implicated in binding and capture of oxidized low-density lipoprotein (PMID:12023894)
  • Genomic heterogeneity of type II CD36 deficiency (PMID:12031598)
  • Results offer structural insights into the molecular patterns recognized by the scavenger receptor CD36 and provide a platform for the development of potential therapeutic inhibitory agents. (PMID:12105195)
  • Heterozygotes, CD36+/-, have a significant reduction of long-chain fatty acids uptake in the heart independent of heart disease, suggesting genotype dependency and that CD36 might be a fundamental determinant of myocardial LCFA uptake. (PMID:12224819)
  • Data show that expression of CD36 on platelet membranes was increased in myeloproliferative, but was not significantly different from normal controls in non-insulin-dependent diabetes mellitus. (PMID:12479587)
  • mediates nonopsonic phagocytosis of erythrocytes infected with stage I and IIA gametocytes of Plasmodium falciparum in monocytes and macrophages (PMID:12496189)
  • Adhesion of dendritic cells derived from CD34+ progenitors to resting human dermal microvascular endothelial cells is down-regulated upon maturation and partially depends on CD11a-CD18, CD11b-CD18 and CD36. (PMID:12516552)
  • polySia of milk CD36 is significant for neonatal development in terms of protection and nutrition (PMID:12576469)
  • Macrophage recognition and phagocytosis of apoptotic fibroblasts is critically dependent on this protein. (PMID:12598312)
  • mediates endocytic uptake of advanced glycation end products (PMID:12606036)
  • Expression of the monocyte-macrophage LDL scavenger receptor CD36 is increased in people with diabetes mellitus, type 2. (PMID:12618277)
  • Expression in melanoma cells is regulated by NSAIDs. (PMID:12664607)
  • TSP-1-induced inhibition of megakaryocytopoiesis is probably mediated in part by the binding of TSP-1 to CD36 expressed on the megakaryocytic progenitors (PMID:12679131)
  • data suggest that platelet Cd36 has a key role in VLDL-induced collagen-mediated platelet aggregation, possibly contributing to atherothrombosis associated with increased VLDL levels (PMID:12716760)
  • Lipoprotein abnormalities in human genetic CD36 deficiency is associated with insulin resistance and abnormal fatty acid metabolism. (PMID:12716848)
  • Expression of CD36 mRNA was up-regulated by mildly- and moderately-oxLDL, but not highly-oxLDL. (PMID:12801610)
  • CD36 is localized in lipid rafts but not in caveolae, and binding of OxLDL to CD36 leads to endocytosis through a lipid raft pathway (PMID:12947091)
  • CD36 and SR-BI are receptors for hypochlorite-modified low density lipoprotein (PMID:12968020)
  • Higher levels of fatty acid translocase/CD36 in human female liver may aid sexually dimorphic development of diseases resulting from or characterized by disturbances in lipid metabolism, such as arteriosclerosis, hyperlipidemia, and insulin resistance. (PMID:14684613)
  • there is a CD36-dependent signaling cascade initiated by fibrillar amyloid species that may promote atherogenesis (PMID:14699114)
  • CD36 ribozyme specifically suppresses CD36 gene expression and growth in osteosarcoma csell lines. (PMID:14719070)
  • CD36 colocalizes with caveolin-3, suggesting that caveolae may regulate cellular fatty acid uptake by CD36. CD36 expression is higher in type 1 compared with type 2 fibers, whereas caveolin-3 expression is significantly higher in type 2 than in type 1 (PMID:14729862)
  • CD36 was reactive with microvascular endothelium and adipocytes.Its expression on these high endothelial cells suggest that it participate in trafficking of leukocytes,especially lymphocytes to the omentum. (PMID:15048167)
  • CD36 is regulated by estrogen receptors in breast cancer cells (PMID:15050739)
  • CD36 has a role in beta-amyloid deposition but not with Alzheimer’s disease (PMID:15059642)
  • Promoter polymorphism in CD36 is associated with atherogenesis is french population. (PMID:15064117)
  • Redistribution of FAT/CD36 to the sarcolemma may contribute to the etiology of insulin resistance in human muscle. (PMID:15132977)
  • A rare CD36 nonsense mutation found in a Caucasian pedigree with autosomal dominant type II diabetes. (PMID:15221799)
  • Single Nucleotide Polymorphisms in CD36 Antigens is associated with cardiovascular diseases (PMID:15282206)
  • In patients with type I CD36 deficiency, immunization with CD36 antigen by transfusion, can produce anti-CD36 antibody, and potentially lead to platelet transfusion refractoriness or post-tansfusion purpur (PMID:15339698)
  • host membrane proteins such as AE1 contribute to the adhesion of malaria-infected erythrocytes to CD36 (PMID:15478802)
  • Single nucleotide polymorphism promoter mutation in the CD36 gene represents a putative genetic marker for insulin-resistance in the French population. (PMID:15671915)
  • CD36 activity appears important for uptake of fatty acids into beta-cells as well as for mediating their modulatory effects on insulin secretion. (PMID:15677505)

Cross-species orthologs

9 orthologs

OrganismSymbolGene ID
danio_reriocd36ENSDARG00000032639
mus_musculusCd36ENSMUSG00000002944
rattus_norvegicusCd36-ps1ENSRNOG00000005906
rattus_norvegicusENSRNOG00000073733
rattus_norvegicusENSRNOG00000078327
rattus_norvegicusENSRNOG00000090226
caenorhabditis_elegansWBGENE00013039
caenorhabditis_elegansWBGENE00013578
caenorhabditis_elegansWBGENE00015389

Paralogs (2): SCARB1 (ENSG00000073060), SCARB2 (ENSG00000138760)

Protein

Protein identifiers

Platelet glycoprotein 4P16671 (reviewed: P16671)

Alternative names: Fatty acid translocase, Glycoprotein IIIb, Leukocyte differentiation antigen CD36, PAS IV, PAS-4, Platelet collagen receptor, Platelet glycoprotein IV, Thrombospondin receptor

All UniProt accessions (11): A4D1B1, E7ERZ9, E7EU05, E7EVU1, E7EWI4, E7EX47, P16671, E9PC45, E9PJX8, E9PLT1, H0YEE7

UniProt curated annotations — full annotation on UniProt →

Function. Multifunctional glycoprotein that acts as a receptor for a broad range of ligands. Ligands can be of proteinaceous nature like thrombospondin, fibronectin, collagen or amyloid-beta as well as of lipidic nature such as oxidized low-density lipoprotein (oxLDL), anionic phospholipids, long-chain fatty acids and bacterial diacylated lipopeptides. They are generally multivalent and can therefore engage multiple receptors simultaneously, the resulting formation of CD36 clusters initiates signal transduction and internalization of receptor-ligand complexes. The dependency on coreceptor signaling is strongly ligand specific. Cellular responses to these ligands are involved in angiogenesis, inflammatory response, fatty acid metabolism, taste and dietary fat processing in the intestine. Binds long-chain fatty acids and facilitates their transport into cells, thus participating in muscle lipid utilization, adipose energy storage, and gut fat absorption. Mechanistically, palmitoylated CD36 captures fatty acids on the cell surface, the binding of fatty acids activates downstream kinase LYN, which phosphorylates the palmitoyltransferase ZDHHC5 and inactivates it, resulting in the subsequent depalmitoylation of CD36, a step needed to initiate the endocytic process and delivery of fatty acids into the cell. In the small intestine, plays a role in proximal absorption of dietary fatty acid and cholesterol for optimal chylomicron formation, possibly through the activation of MAPK1/3 (ERK1/2) signaling pathway. Involved in oral fat perception and preferences. Detection into the tongue of long-chain fatty acids leads to a rapid and sustained rise in flux and protein content of pancreatobiliary secretions. In taste receptor cells, mediates the induction of an increase in intracellular calcium levels by long-chain fatty acids, leading to the activation of the gustatory neurons in the nucleus of the solitary tract. Important factor in both ventromedial hypothalamus neuronal sensing of long-chain fatty acid and the regulation of energy and glucose homeostasis. Receptor for thrombospondins, THBS1 and THBS2, mediating their antiangiogenic effects. Involved in inducing apoptosis in podocytes in response to elevated free fatty acids, acting together with THBS1. As a coreceptor for TLR4:TLR6 heterodimer, promotes inflammation in monocytes/macrophages. Upon ligand binding, such as oxLDL or amyloid-beta 42, interacts with the heterodimer TLR4:TLR6, the complex is internalized and triggers inflammatory response, leading to NF-kappa-B-dependent production of CXCL1, CXCL2 and CCL9 cytokines, via MYD88 signaling pathway, and CCL5 cytokine, via TICAM1 signaling pathway, as well as IL1B secretion, through the priming and activation of the NLRP3 inflammasome. Selective and nonredundant sensor of microbial diacylated lipopeptide that signal via TLR2:TLR6 heterodimer, this cluster triggers signaling from the cell surface, leading to the NF-kappa-B-dependent production of TNF, via MYD88 signaling pathway and subsequently is targeted to the Golgi in a lipid-raft dependent pathway. (Microbial infection) Directly mediates cytoadherence of Plasmodium falciparum parasitized erythrocytes and the internalization of particles independently of TLR signaling.

Subunit / interactions. Interacts with THBS1 and THBS2; the interactions mediate the THBS antiangiogenic activity. Upon interaction with a ligand, such as oxidized low-density lipoprotein (oxLDL) or amyloid-beta 42, rapidly forms a complex with TLR4 and TLR6; the complex is internalized and triggers an inflammatory signal. Through its C-terminus, interacts with PTK2, PXN and LYN, but not with SRC. LYN kinase activity is required for facilitating TLR4:TLR6 heterodimerization and signal initiation. Upon interaction with ligands such as diacylated lipopeptides, interacts with the TLR2:TLR6 heterodimer. Interacts with CD9, CD81, FCER1G, ITGB2 and/or ITGB2; forming a membrane heteromeric complex required for the internalization of CD36 and its ligands. Interacts (when palmitoylated) with ARF6; this interaction mediates CD36 transport to the plasma membrane. (Microbial infection) Binds to Plasmodium falciparum EMP1.

Subcellular location. Cell membrane. Membrane raft. Golgi apparatus. Apical cell membrane.

Post-translational modifications. N-glycosylated and O-glycosylated with a ratio of 2:1. Palmitoylated by ZDHHC5. Palmitoylation is required for proper localization at the plasma membrane. Ubiquitinated at Lys-469 and Lys-472. Ubiquitination is induced by fatty acids such as oleic acid and leads to degradation by the proteasome. Ubiquitination and degradation are inhibited by insulin which blocks the effect of fatty acids.

Disease relevance. Platelet glycoprotein IV deficiency (PG4D) [MIM:608404] A disorder characterized by macrothrombocytopenia without notable hemostatic problems and bleeding tendency. Platelet glycoprotein IV deficiency can be divided into 2 subgroups. The type I phenotype is characterized by platelets and monocytes/macrophages exhibiting complete CD36 deficiency. The type II phenotype lacks the surface expression of CD36 in platelets, but expression in monocytes/macrophages is near normal. The disease is caused by variants affecting the gene represented in this entry. Patients also have postprandial hypertriglyceridemia, insulin resistance and hypertension increasing atherosclerotic risk. Coronary heart disease 7 (CHDS7) [MIM:610938] A multifactorial disease characterized by an imbalance between myocardial functional requirements and the capacity of the coronary vessels to supply sufficient blood flow. Decreased capacity of the coronary vessels is often associated with thickening and loss of elasticity of the coronary arteries. Disease susceptibility is associated with variants affecting the gene represented in this entry.

Polymorphism. Genetic variations in CD36 are involved in susceptibility to malaria and influence the severity and outcome of malaria infection [MIM:611162].

Similarity. Belongs to the CD36 family.

Isoforms (4)

UniProt IDNamesCanonical?
P16671-11yes
P16671-22, ex8-del
P16671-33, ex6-7-del
P16671-44, ex4-del

RefSeq proteins (15): NP_000063, NP_001001547, NP_001001548, NP_001120915, NP_001120916, NP_001276837, NP_001276838, NP_001276840, NP_001358003, NP_001358004, NP_001358006, NP_001358007, NP_001358008, NP_001358009, NP_001358010 (=MANE)

Domains & families (InterPro)

IDNameType
IPR002159CD36_famFamily
IPR005428CD36/SCARB1/SNMP1Family

Pfam: PF01130

Catalyzed reactions (Rhea), 10 shown:

  • (9Z)-octadecenoate(out) = (9Z)-octadecenoate(in) (RHEA:33655)
  • a fatty acid(in) = a fatty acid(out) (RHEA:38879)
  • a long-chain fatty acid(out) = a long-chain fatty acid(in) (RHEA:39283)
  • octadecanoate(in) = octadecanoate(out) (RHEA:39807)
  • butanoate(out) = butanoate(in) (RHEA:45248)
  • tetradecanoate(out) = tetradecanoate(in) (RHEA:45252)
  • hexadecanoate(out) = hexadecanoate(in) (RHEA:45256)
  • tetracosanoate(out) = tetracosanoate(in) (RHEA:45260)
  • (9Z,12Z)-octadecadienoate(out) = (9Z,12Z)-octadecadienoate(in) (RHEA:45264)
  • (5Z,8Z,11Z,14Z)-eicosatetraenoate(out) = (5Z,8Z,11Z,14Z)-eicosatetraenoate(in) (RHEA:71395)

UniProt features (98 total): strand 23, helix 18, sequence variant 11, glycosylation site 10, turn 6, lipid moiety-binding region 4, splice variant 4, mutagenesis site 4, topological domain 3, disulfide bond 3, sequence conflict 3, cross-link 2, transmembrane region 2, region of interest 2, initiator methionine 1, chain 1, site 1

Structure

Experimental structures (PDB)

1 structures.

PDBMethodResolution (Å)
5LGDX-RAY DIFFRACTION2.07

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-P16671-F194.140.84

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Catalytic / active sites (1): 463 (critical for tlr4-tlr6 dimerization and signaling)

Post-translational modifications (6): 3, 7, 464, 466, 469, 472

Disulfide bonds (3): 243–311, 272–333, 313–322

Glycosylation sites (10): 79, 102, 134, 163, 205, 220, 235, 247, 321, 417

Mutagenesis-validated functional residues (4):

PositionPhenotype
462–472no effect on cell surface location. loss of oxldl-induced nf-kappa-b activation.
463no effect on cell surface location. loss of oxldl-induced nf-kappa-b activation. loss of complex formation with tlr4 and
464no effect on cell surface location, nor on oxldl-induced nf-kappa-b activation.
469–472abolishes ubiquitination induced by lipids. enhances fatty acid uptake.

Function

Pathways and Gene Ontology

Reactome pathways

47 pathways

IDPathway
R-HSA-114608Platelet degranulation
R-HSA-1236973Cross-presentation of particulate exogenous antigens (phagosomes)
R-HSA-1236974ER-Phagosome pathway
R-HSA-166058MyD88:MAL(TIRAP) cascade initiated on plasma membrane
R-HSA-168188Toll Like Receptor TLR6:TLR2 Cascade
R-HSA-1989781PPARA activates gene expression
R-HSA-3000471Scavenging by Class B Receptors
R-HSA-381340Transcriptional regulation of white adipocyte differentiation
R-HSA-434313Intracellular metabolism of fatty acids regulates insulin secretion
R-HSA-5602498MyD88 deficiency (TLR2/4)
R-HSA-5603041IRAK4 deficiency (TLR2/4)
R-HSA-5686938Regulation of TLR by endogenous ligand
R-HSA-6785807Interleukin-4 and Interleukin-13 signaling
R-HSA-6798695Neutrophil degranulation
R-HSA-9841922MLL4 and MLL3 complexes regulate expression of PPARG target genes in adipogenesis and hepatic steatosis
R-HSA-109582Hemostasis
R-HSA-1236975Antigen processing-Cross presentation
R-HSA-1266738Developmental Biology
R-HSA-1280215Cytokine Signaling in Immune system
R-HSA-1280218Adaptive Immune System
R-HSA-1430728Metabolism
R-HSA-163685Integration of energy metabolism
R-HSA-1643685Disease
R-HSA-166016Toll Like Receptor 4 (TLR4) Cascade
R-HSA-168179Toll Like Receptor TLR1:TLR2 Cascade
R-HSA-168249Innate Immune System
R-HSA-168256Immune System
R-HSA-168898Toll-like Receptor Cascades
R-HSA-181438Toll Like Receptor 2 (TLR2) Cascade
R-HSA-212165Epigenetic regulation of gene expression

MSigDB gene sets: 688 (showing top): GOBP_CELLULAR_RESPONSE_TO_LIPOPROTEIN_PARTICLE_STIMULUS, REACTOME_TRANSCRIPTIONAL_REGULATION_OF_WHITE_ADIPOCYTE_DIFFERENTIATION, GOBP_DIGESTION, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_REGULATION_OF_LIPID_STORAGE, REACTOME_INNATE_IMMUNE_SYSTEM, CHIBA_RESPONSE_TO_TSA_UP, GOBP_POSITIVE_REGULATION_OF_ENDOCYTOSIS, KEGG_ADIPOCYTOKINE_SIGNALING_PATHWAY, GOBP_REGULATION_OF_WOUND_HEALING, GOBP_CIRCULATORY_SYSTEM_PROCESS, REACTOME_ADAPTIVE_IMMUNE_SYSTEM, GOBP_INTRACELLULAR_PROTEIN_TRANSPORT, REACTOME_CYTOKINE_SIGNALING_IN_IMMUNE_SYSTEM, GOBP_INFLAMMATORY_RESPONSE

GO Biological Process (85): negative regulation of transcription by RNA polymerase II (GO:0000122), MAPK cascade (GO:0000165), positive regulation of cell-matrix adhesion (GO:0001954), production of molecular mediator involved in inflammatory response (GO:0002532), lipid metabolic process (GO:0006629), fatty acid metabolic process (GO:0006631), receptor-mediated endocytosis (GO:0006898), phagocytosis, recognition (GO:0006910), phagocytosis, engulfment (GO:0006911), inflammatory response (GO:0006954), cell adhesion (GO:0007155), cell surface receptor signaling pathway (GO:0007166), positive regulation of cytosolic calcium ion concentration (GO:0007204), blood coagulation (GO:0007596), positive regulation of gene expression (GO:0010628), negative regulation of gene expression (GO:0010629), positive regulation of macrophage derived foam cell differentiation (GO:0010744), positive regulation of cholesterol storage (GO:0010886), fatty acid transport (GO:0015908), long-chain fatty acid transport (GO:0015909), long-chain fatty acid import across plasma membrane (GO:0015911), short-chain fatty acid transport (GO:0015912), negative regulation of angiogenesis (GO:0016525), lipid storage (GO:0019915), obsolete cGMP-mediated signaling (GO:0019934), positive regulation of blood coagulation (GO:0030194), intestinal cholesterol absorption (GO:0030299), cholesterol transport (GO:0030301), receptor internalization (GO:0031623), regulation of lipopolysaccharide-mediated signaling pathway (GO:0031664), positive regulation of interleukin-1 beta production (GO:0032731), positive regulation of interleukin-12 production (GO:0032735), positive regulation of interleukin-6 production (GO:0032755), positive regulation of tumor necrosis factor production (GO:0032760), response to lipid (GO:0033993), regulation of toll-like receptor signaling pathway (GO:0034121), positive regulation of toll-like receptor 4 signaling pathway (GO:0034145), triglyceride transport (GO:0034197), plasma lipoprotein particle clearance (GO:0034381), low-density lipoprotein particle clearance (GO:0034383)

GO Molecular Function (18): amyloid-beta binding (GO:0001540), low-density lipoprotein particle receptor activity (GO:0005041), scavenger receptor activity (GO:0005044), long-chain fatty acid transmembrane transporter activity (GO:0005324), high-density lipoprotein particle binding (GO:0008035), lipid binding (GO:0008289), short-chain fatty acid transmembrane transporter activity (GO:0015636), low-density lipoprotein particle binding (GO:0030169), Toll-like receptor binding (GO:0035325), cargo receptor activity (GO:0038024), protein-containing complex binding (GO:0044877), transforming growth factor beta binding (GO:0050431), thrombospondin receptor activity (GO:0070053), lipoteichoic acid immune receptor activity (GO:0070892), lipoprotein particle binding (GO:0071813), oxidised low-density lipoprotein particle receptor activity (GO:0150025), oleate transmembrane transporter activity (GO:1901480), protein binding (GO:0005515)

GO Cellular Component (18): obsolete extracellular space (GO:0005615), Golgi apparatus (GO:0005794), plasma membrane (GO:0005886), caveola (GO:0005901), external side of plasma membrane (GO:0009897), cell surface (GO:0009986), membrane (GO:0016020), endocytic vesicle membrane (GO:0030666), platelet alpha granule membrane (GO:0031092), brush border membrane (GO:0031526), specific granule membrane (GO:0035579), signaling receptor complex (GO:0043235), membrane raft (GO:0045121), phagocytic vesicle (GO:0045335), cell periphery (GO:0071944), collagen trimer (GO:0005581), apical plasma membrane (GO:0016324), apical part of cell (GO:0045177)

Reactome top-level categories

Rollup of top-17 pathways:

CategoryPathways
Antigen processing-Cross presentation2
Diseases associated with the TLR signaling cascade2
Immune System2
Response to elevated platelet cytosolic Ca2+1
Toll Like Receptor 4 (TLR4) Cascade1
Toll Like Receptor TLR1:TLR2 Cascade1
Toll Like Receptor TLR6:TLR2 Cascade1
Toll Like Receptor 2 (TLR2) Cascade1
Regulation of lipid metabolism by PPARalpha1
Binding and Uptake of Ligands by Scavenger Receptors1
Adipogenesis1
Free fatty acids regulate insulin secretion1
Toll-like Receptor Cascades1
Signaling by Interleukins1
Innate Immune System1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
cellular anatomical structure4
binding3
phagocytosis2
cargo receptor activity2
gene expression2
regulation of gene expression2
lipoprotein particle receptor activity2
fatty acid transmembrane transporter activity2
lipoprotein particle binding2
endocytic vesicle2
secretory granule membrane2
protein-containing complex2
regulation of transcription by RNA polymerase II1
transcription by RNA polymerase II1
negative regulation of DNA-templated transcription1
intracellular signaling cassette1
regulation of cell-matrix adhesion1
cell-matrix adhesion1
positive regulation of cell-substrate adhesion1
inflammatory response1
multicellular organismal process1
primary metabolic process1
lipid metabolic process1
monocarboxylic acid metabolic process1
endocytosis1
cell recognition1
plasma membrane invagination1
defense response1
cellular process1
signal transduction1
regulation of biological quality1
hemostasis1
wound healing1
coagulation1
positive regulation of macromolecule biosynthetic process1
negative regulation of macromolecule biosynthetic process1
macrophage derived foam cell differentiation1
regulation of macrophage derived foam cell differentiation1
positive regulation of cell differentiation1
cholesterol storage1

Protein interactions and networks

STRING

5204 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
CD36TLR2O60603996
CD36THBS1P07996996
CD36TLR4O00206996
CD36CD47Q08722994
CD36GP2P55259994
CD36TLR6Q9Y2C9993
CD36GP5P40197991
CD36CD163Q86VB7976
CD36LYNP07948973
CD36FYNP06241958
CD36CAV1Q03135956
CD36THBS2P35442954
CD36TLR1Q15399930
CD36APOBP04114917
CD36FCGR3AP08637916
CD36FCGR3BO75015916

IntAct

26 interactions, top by confidence:

ABTypeScore
THBS1CD36psi-mi:“MI:0407”(direct interaction)0.560
CD36UNGpsi-mi:“MI:0915”(physical association)0.560
APPCD36psi-mi:“MI:0915”(physical association)0.560
CD36LYNpsi-mi:“MI:0915”(physical association)0.500
LYNCD36psi-mi:“MI:0915”(physical association)0.500
CD36LYNpsi-mi:“MI:0914”(association)0.500
CD36PXNpsi-mi:“MI:0914”(association)0.460
Scarb2CD36psi-mi:“MI:0915”(physical association)0.400
CHRDCD36psi-mi:“MI:0915”(physical association)0.370
CD36TLR4psi-mi:“MI:0914”(association)0.350
CAND1GTPBP10psi-mi:“MI:0914”(association)0.350
CD36TTMPpsi-mi:“MI:0914”(association)0.350
VPS37Cpsi-mi:“MI:0914”(association)0.350
SMPD2A2ML1psi-mi:“MI:0914”(association)0.350
CD36dacDpsi-mi:“MI:0915”(physical association)0.000
CD36iccpsi-mi:“MI:0915”(physical association)0.000
yapECD36psi-mi:“MI:0915”(physical association)0.000
mpaACD36psi-mi:“MI:0915”(physical association)0.000
CD36cutApsi-mi:“MI:0915”(physical association)0.000

BioGRID (38): CROT (Affinity Capture-MS), C3orf52 (Affinity Capture-MS), MBOAT7 (Affinity Capture-MS), CD36 (Affinity Capture-Western), IRS1 (Affinity Capture-Western), FYN (Affinity Capture-Western), APOB (Reconstituted Complex), GPC4 (Co-localization), GPC4 (Affinity Capture-Western), CD36 (Affinity Capture-Western), HSD11B1 (Reconstituted Complex), LDLR (Reconstituted Complex), VLDLR (Reconstituted Complex), FYN (Affinity Capture-Western), LYN (Affinity Capture-Western)

ESM2 similar proteins: B0X4H5, B2LT48, B2RFN2, B3MTS2, B3P048, B4GMC9, B4IKJ4, B4JG39, B4KB36, B4LYC5, B4NK88, B4PQC2, B4R136, B7Z031, C3U0S3, D2A0H5, E0W3E3, E1JI63, E2IHA6, E5EZW6, E5EZW7, E5EZW9, E5EZX0, O02351, O35114, P16671, P26201, P27615, P70110, P86905, Q07969, Q08857, Q09606, Q11124, Q14108, Q17A88, Q24046, Q27367, Q295A8, Q7Q6R1

Diamond homologs: B2RFN2, C3U0S3, E1JI63, P16671, P26201, P70110, Q07969, Q08857, Q7Q6R1, O18824, O35114, P27615, P97943, Q14108, Q27367, Q60417, Q61009, Q8SQC1, Q8WTV0, Q11124, Q55FQ9, Q9BKJ9, Q9XYS8, P86905

SIGNOR signaling

4 interactions.

AEffectBMechanism
CD36“up-regulates quantity”“Fatty acid”relocalization
GRK2“down-regulates quantity by destabilization”CD36phosphorylation
CD36down-regulatesAngiogenesis
TFEB“up-regulates quantity by expression”CD36“transcriptional regulation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

341 variants total. Per-class counts are floors (≥ shown; pagination cap):

ClassificationCount (floor)
Pathogenic29
Likely pathogenic32
Uncertain significance184
Likely benign17
Benign26

Top pathogenic / likely-pathogenic (30)

Variant IDHGVSClassification
1301547NM_001001548.3(CD36):c.667_671dup (p.Ala225fs)Pathogenic
1322041NM_001001548.3(CD36):c.638_639del (p.Lys213fs)Pathogenic
1322043NM_001001548.3(CD36):c.729C>A (p.Cys243Ter)Pathogenic
13540NM_001001548.3(CD36):c.760T>C (p.Phe254Leu)Pathogenic
13541NM_001001548.3(CD36):c.1237A>C (p.Ile413Leu)Pathogenic
1356762NM_001001548.3(CD36):c.1086_1109dup (p.Tyr370Ter)Pathogenic
155322GRCh38/hg38 7q21.11(chr7:80627421-80651297)x1Pathogenic
1708387NM_001001548.3(CD36):c.120+1G>APathogenic
285207NM_001001548.3(CD36):c.1155del (p.Lys385fs)Pathogenic
3036442NM_001001548.3(CD36):c.1047_1051dup (p.Pro351fs)Pathogenic
3062947GRCh37/hg19 7q21.11(chr7:80107707-80303798)x1Pathogenic
3374841NM_001001548.3(CD36):c.1062_1098dup (p.His367delinsArgThrTyrTer)Pathogenic
3779488NM_001001548.3(CD36):c.430-1G>CPathogenic
3902427NM_001001548.3(CD36):c.15del (p.Asn6fs)Pathogenic
4076050GRCh37/hg19 7q21.11(chr7:80256738-80280613)x1Pathogenic
4279118GRCh37/hg19 7q21.11(chr7:80256738-80276756)x1Pathogenic
4279163GRCh37/hg19 7q21.11(chr7:80257096-80280613)x1Pathogenic
442306GRCh37/hg19 7q21.11(chr7:80256737-80277776)x0Pathogenic
685689GRCh37/hg19 7q21.11(chr7:80256254-80276756)x1Pathogenic
686205GRCh37/hg19 7q21.11(chr7:80242420-80303812)x1Pathogenic
686312GRCh37/hg19 7q21.11(chr7:80262999-80276756)x1Pathogenic
686525GRCh37/hg19 7q21.11(chr7:80256737-80276756)x1Pathogenic
686719GRCh37/hg19 7q21.11(chr7:80262999-80276756)x1Pathogenic
686754GRCh37/hg19 7q21.11(chr7:80254791-80276756)x1Pathogenic
688139GRCh37/hg19 7q21.11(chr7:80262999-80276756)x1Pathogenic
688327GRCh37/hg19 7q21.11(chr7:80254409-80276756)x1Pathogenic
688623GRCh37/hg19 7q21.11(chr7:80256737-80276756)x1Pathogenic
689019GRCh37/hg19 7q21.11(chr7:80256888-80276756)x1Pathogenic
987919NM_001001547.2:c.(?-183)(120_?)delPathogenic
1302074NM_001001548.3(CD36):c.430-1G>ALikely pathogenic

SpliceAI

6221 predictions. Top by Δscore:

VariantEffectΔscore
7:80414611:A:Gdonor_gain1.0000
7:80458861:CCT:Cacceptor_gain1.0000
7:80458863:T:Cacceptor_gain1.0000
7:80462324:C:CTacceptor_gain1.0000
7:80462325:A:Tacceptor_gain1.0000
7:80478839:A:ACdonor_gain1.0000
7:80478840:C:CCdonor_gain1.0000
7:80478840:CTAAG:Cdonor_gain1.0000
7:80488533:A:ACdonor_gain1.0000
7:80488534:C:CTdonor_gain1.0000
7:80488534:CTG:Cdonor_gain1.0000
7:80488534:CTGCA:Cdonor_gain1.0000
7:80494603:A:ACdonor_gain1.0000
7:80494604:C:CCdonor_gain1.0000
7:80541148:G:Tdonor_gain1.0000
7:80656539:GCAA:Gacceptor_gain1.0000
7:80661049:T:Aacceptor_gain1.0000
7:80661062:GA:Gacceptor_gain1.0000
7:80661206:TGGCA:Tdonor_gain1.0000
7:80661207:GGCA:Gdonor_gain1.0000
7:80661207:GGCAG:Gdonor_gain1.0000
7:80661208:GCA:Gdonor_gain1.0000
7:80661208:GCAG:Gdonor_gain1.0000
7:80661209:CAG:Cdonor_loss1.0000
7:80661210:AGT:Adonor_loss1.0000
7:80661211:G:Adonor_loss1.0000
7:80661211:G:GGdonor_gain1.0000
7:80661212:TGA:Tdonor_loss1.0000
7:80661213:G:GCdonor_loss1.0000
7:80661214:AG:Adonor_loss1.0000

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000027409 (7:80663604 G>A), RS1000032231 (7:80679458 T>C), RS1000107107 (7:80659528 C>T), RS1000114141 (7:80637436 C>A), RS1000129194 (7:80628340 C>G,T), RS1000191047 (7:80617349 CA>C,CAA), RS1000270618 (7:80674365 T>C), RS1000297566 (7:80608616 T>G), RS1000338107 (7:80679492 T>A), RS1000347504 (7:80641672 A>G), RS1000432594 (7:80660685 G>A), RS1000440867 (7:80620297 C>T), RS1000465011 (7:80661051 C>A,T), RS1000465877 (7:80629617 A>C,G), RS1000484969 (7:80641376 T>A)

Disease associations

OMIM: gene MIM:173510 | disease phenotypes: MIM:608404, MIM:610938, MIM:611162, MIM:231200, MIM:125853

GenCC curated gene-disease

DiseaseClassificationInheritance
platelet-type bleeding disorder 10StrongAutosomal recessive

Mondo (6): platelet-type bleeding disorder 10 (MONDO:0012031), coronary heart disease, susceptibility to, 7 (MONDO:0012585), malaria, susceptibility to (MONDO:0021024), osteopetrosis (MONDO:0017198), inherited bleeding disorder, platelet-type (MONDO:0000009), type 2 diabetes mellitus (MONDO:0005148)

Orphanet (3): Malaria (Orphanet:673), Osteopetrosis and related disorders (Orphanet:2781), Rare hemorrhagic disorder due to a platelet anomaly (Orphanet:248326)

HPO phenotypes

5 total (6 of 5 shown, HPO-id order):

HPOTerm
HP:0000007Autosomal recessive inheritance
HP:0001873Thrombocytopenia
HP:0001892Abnormal bleeding
HP:0001902Giant platelets
HP:0003010Prolonged bleeding time
HP:0011002Osteopetrosis

GWAS associations

45 associations (top):

StudyTraitp-value
GCST000407_1Left ventricular mass3.000000e-06
GCST001632_4Response to fenofibrate8.000000e-08
GCST002043_2HDL cholesterol6.000000e-10
GCST003542_206Night sleep phenotypes3.000000e-06
GCST004599_53Mean platelet volume5.000000e-12
GCST004601_98Red blood cell count2.000000e-12
GCST004602_54Mean corpuscular volume1.000000e-13
GCST004603_39Platelet count4.000000e-12
GCST005991_90Platelet count2.000000e-17
GCST005992_31Mean corpuscular hemoglobin concentration4.000000e-11
GCST005999_16Aspartate aminotransferase levels3.000000e-14
GCST006005_13High density lipoprotein cholesterol levels5.000000e-21
GCST006585_627Blood protein levels1.000000e-06
GCST006611_151HDL cholesterol3.000000e-27
GCST006804_111Red cell distribution width2.000000e-17
GCST008047_5Platelet count3.000000e-09
GCST008075_12HDL cholesterol levels x alcohol consumption (regular vs non-regular drinkers) interaction (2df)6.000000e-45
GCST008075_147HDL cholesterol levels x alcohol consumption (regular vs non-regular drinkers) interaction (2df)6.000000e-51
GCST008075_98HDL cholesterol levels x alcohol consumption (regular vs non-regular drinkers) interaction (2df)5.000000e-08
GCST008084_166HDL cholesterol levels x alcohol consumption (drinkers vs non-drinkers) interaction (2df)2.000000e-08
GCST008084_63HDL cholesterol levels x alcohol consumption (drinkers vs non-drinkers) interaction (2df)5.000000e-08
GCST008085_189HDL cholesterol levels in current drinkers5.000000e-06
GCST008085_71HDL cholesterol levels in current drinkers2.000000e-07
GCST010396_259Gut microbiota (bacterial taxa, hurdle binary method)2.000000e-07
GCST010396_277Gut microbiota (bacterial taxa, hurdle binary method)4.000000e-06
GCST010796_591Electrocardiogram morphology (amplitude at temporal datapoints)3.000000e-08
GCST011010_14Electrocardiographic traits (multivariate)5.000000e-09
GCST011348_13High density lipoprotein cholesterol levels1.000000e-18
GCST011351_11Aspartate aminotransferase levels1.000000e-12
GCST012032_7Platelet count6.000000e-08

EFO canonical traits (14, from GWAS)

EFO IDTrait name
EFO:0008205left ventricular structural measurement
EFO:0004612high density lipoprotein cholesterol measurement
EFO:0004305erythrocyte count
EFO:0004309platelet count
EFO:0004528mean corpuscular hemoglobin concentration
EFO:0004736aspartate aminotransferase measurement
EFO:0009188Red cell distribution width
EFO:0004329alcohol drinking
EFO:0007874gut microbiome measurement
EFO:0004327electrocardiography
EFO:0005090basophil count
EFO:0004509hemoglobin measurement
EFO:0010701mean reticulocyte volume
EFO:0007985platelet crit

MeSH disease descriptors (3)

DescriptorNameTree numbers
D003924Diabetes Mellitus, Type 2C18.452.394.750.149; C19.246.300
D010022OsteopetrosisC05.116.099.708.702.678
C564245Platelet Glycoprotein IV Deficiency (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL1744526 (SINGLE PROTEIN)

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: other protein — CD molecules

Most potent curated ligand interactions (2 total), top 2:

LigandActionAffinityParameter
peptide 1 [PMID: 31774287]Antagonist7.1pKd
compound 3c [PMID: 30360354]Antagonist5.6pIC50

ChEMBL bioactivities

1 potent at pChembl≥5 of 1 total, top 1 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
5.40IC504000nMCHEMBL6161924

CTD chemical–gene interactions

186 total (human), top 30 by PubMed support.

ChemicalActions (top 5)PubMed papers
Rosiglitazoneaffects cotreatment, decreases reaction, increases expression, increases reaction, affects reaction (+1 more)16
bisphenol Aincreases methylation, increases activity, increases response to substance, affects reaction, decreases reaction (+2 more)9
Tetradecanoylphorbol Acetateaffects cotreatment, increases expression, decreases reaction, increases reaction, decreases expression9
Troglitazonedecreases expression, decreases reaction, increases expression6
Oleic Acidaffects cotreatment, increases expression, decreases reaction6
Tetrachlorodibenzodioxindecreases ubiquitination, decreases reaction, increases expression, affects cotreatment, decreases expression5
Valproic Aciddecreases reaction, increases expression, increases methylation5
Palmitic Aciddecreases reaction, increases expression, affects cotreatment, decreases expression5
Pioglitazoneincreases expression, affects reaction, affects cotreatment, decreases expression, decreases reaction4
Amiodaroneincreases expression, decreases expression4
Aflatoxin B1decreases expression, decreases methylation, increases expression4
2-chloro-5-nitrobenzanilidedecreases expression, decreases reaction, affects cotreatment, increases expression3
Resveratroldecreases expression, decreases reaction, increases expression3
Acetylcysteineincreases expression, decreases reaction3
Dexamethasonedecreases reaction, affects reaction, affects binding, increases reaction, increases expression3
Estradiolaffects cotreatment, increases expression, decreases expression3
Quercetinaffects cotreatment, decreases reaction, increases expression, decreases expression3
Tamoxifenaffects cotreatment, increases expression, decreases reaction, affects binding, decreases expression3
Tobacco Smoke Pollutiondecreases expression3
fluorotelomer sulfonic acidsincreases uptake, decreases expression2
sodium arsenatedecreases expression, increases abundance2
perfluorooctanoic acidincreases expression2
nickel sulfatedecreases expression2
perfluorooctane sulfonic acidincreases uptake, increases expression2
2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-oneincreases expression, affects cotreatment, decreases reaction2
2-(2-amino-3-methoxyphenyl)-4H-1-benzopyran-4-oneincreases expression, decreases reaction2
GW 7647affects cotreatment, increases expression2
T 0070907decreases reaction, increases expression2
15-deoxyprostaglandin J2increases reaction, affects cotreatment, increases expression2
bisphenol Bdecreases expression, increases expression2

ChEMBL screening assays

6 unique, capped per target: 5 binding, 1 functional

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1764258BindingAntagonist activity at human CD36-oxLDL binding at 1 uM after 2 hrs by ELISASynthesis and structure-activity relationship of N-(2-arylethyl) isoquinoline derivatives as human scavenger receptor CD36 antagonists. — Eur J Med Chem
CHEMBL1764260FunctionalAntagonist activity at human CD36 expressed in insect Sf9 cells assessed as inhibition of DiL-acetylated LDL uptake at 10 ug/ml after 5 hrs by fluorometric analysisSynthesis and structure-activity relationship of N-(2-arylethyl) isoquinoline derivatives as human scavenger receptor CD36 antagonists. — Eur J Med Chem

Cellosaurus cell lines

9 cell lines: 7 cancer cell line, 1 spontaneously immortalized cell line, 1 induced pluripotent stem cell

First 10 cell lines (id-ordered, not curated):

CellosaurusNameCategorySex
CVCL_8848CHO-CD36Spontaneously immortalized cell lineFemale
CVCL_B5FYSYSUSCi002-AInduced pluripotent stem cellFemale
CVCL_B7WHAbcam Raji CD36 KOCancer cell lineMale
CVCL_B9X2Abcam THP-1 CD36 KOCancer cell lineMale
CVCL_C0UPHP-NakCancer cell lineFemale
CVCL_C6Z0Abcam PC-3 CD36 KOCancer cell lineMale
CVCL_E8DSBPS Bioscience THP-1 CD36 KOCancer cell lineMale
CVCL_SH71HAP1 CD36 (-) 1Cancer cell lineMale
CVCL_XM58HAP1 CD36 (-) 2Cancer cell lineMale

Clinical trials (associated diseases)

300 trials via MONDO — disease-level, not drug-specific.

TrialPhaseStatusTitle
NCT06630572PHASE4TERMINATEDRifaximin in Cirrhosis: Effects on Endotoxin and Haemostatic Indexes
NCT00006163PHASE4COMPLETEDComputer-assisted Diabetes Self-management Interventions
NCT00036504PHASE4COMPLETEDEfficacy and Safety of Twice-Daily Insulin Lispro Low Mixture Compared to a Once-Daily Long Acting Insulin Comparator in Patients Who Have Been Using One or More Oral Antihyperglycemic Agents Without Insulin
NCT00044460PHASE4COMPLETEDEfficacy and Safety In Poorly Controlled Type 2 Diabetics
NCT00095446PHASE4COMPLETEDNovoLog Observation Trial in Subjects With Type 1 and Type 2 Diabetes
NCT00101751PHASE4COMPLETEDINITIATE Plus (INITiation of Insulin to Reach A1c TargEt) Study
NCT00110370PHASE4COMPLETEDComparing Pre-Mixed Insulin With Insulin Glargine Combined With Rapid-Acting Insulin in Patients With Type 2 Diabetes
NCT00110448PHASE4COMPLETEDJapanese Primary Prevention of Atherosclerosis With Aspirin for Diabetes (JPAD) Trial
NCT00118950PHASE4COMPLETEDEffect of Metformin Versus Repaglinide Treatment in Non-Obese Type 2 Diabetic Patients Uncontrolled by Diet
NCT00118963PHASE4COMPLETEDEffect of Repaglinide Versus Metformin Treatment in Non-Obese Patients With Type-2-Diabetes
NCT00121966PHASE4COMPLETEDSouth Danish Diabetes Study: Evaluation of the Antidiabetic Treatment of Type 2 Diabetes Mellitus
NCT00123604PHASE4COMPLETEDVascular Effects of Carvedilol Versus Metoprolol in Hypertensive Patients With Type 2 Diabetes
NCT00123643PHASE4COMPLETEDVascular Effects of Rosiglitazone Versus Glyburide in Type 2 Diabetic Patients
NCT00124397PHASE4COMPLETEDAtorvastatin and Endothelial Function in Type 2 Diabetes Mellitus (ATTEND-Study)
NCT00129233PHASE4COMPLETEDComparison of Valsartan With Amlodipine in Hypertensive Patients With Glucose Intolerance
NCT00133718PHASE4COMPLETEDA 2 Year Trial of Patients With Type 2 Diabetes Focusing on Cardiovascular Diagnostics and Metabolic Control
NCT00135070PHASE4TERMINATEDHospital In-Patient Insulin Study
NCT00141232PHASE4COMPLETEDEvaluating Atorvastatin With Omega-3 Fatty Acids in Cardiovascular Risk Reduction in Patients With Type 2 Diabetes
NCT00144144PHASE4UNKNOWNA Study on Ca Blocker Versus AII Antagonists in Hypertension With Type 2 Diabetes
NCT00149331PHASE4COMPLETEDThe Effects of Two Education Strategies About Insulin on Patient Preferences and Perceptions About Insulin Therapy
NCT00162357PHASE4COMPLETEDPost-PCI:Cardiac Imaging in Patients With Diabetes to Detect Coronary Artery Blockages Previously Opened by Angioplasty
NCT00174681PHASE4COMPLETEDTulip Study: Testing the Usefulness of Lantus When Initiated Prematurely In Patients With Type 2 Diabetes
NCT00174824PHASE4COMPLETEDComparison of Insulin Glargine and NPH Human Insulin in Progression of Diabetic Retinopathy in Type 2 Diabetic Patients
NCT00177398PHASE4COMPLETEDEffect of Glargine Insulin on Glucose Control in Hospitalized Patients Who Receive Tube Feedings
NCT00179400PHASE4COMPLETEDThe Role of Acute Combined PPAR Alpha and Gamma Stimulation on Insulin Action in Humans
NCT00184561PHASE4COMPLETEDEffectiveness and Safety of Biphasic Insulin Aspart 70/30 in Subjects With Type 2 Diabetes
NCT00184626PHASE4COMPLETEDComparison of Insulin Glargine Versus Biphasic Insulin Aspart 30/70 or Biphasic Insulin Aspart 30/70 in Combination With Metformin in Subjects With Type 2 Diabetes.
NCT00191178PHASE4COMPLETEDEffects of Insulin in Perceived Mood Symptoms in Patients With Type 2 Diabetes
NCT00191282PHASE4COMPLETEDHyperglycemia and Cardiovascular Outcomes With Type 2 Diabetes
NCT00191464PHASE4COMPLETEDLong-Term Effects of Insulin Plus Metformin Regimens on the Overall and Postprandial Glycemic Control of Patients With Type 2 Diabetes
NCT00192803PHASE4UNKNOWNNon-Insulin Dependent Diabetes Mellitus (NIDDM) and Angiotensin Converting Enzyme 2 (ACE2): Diabetic Patients Treated With Antihypertensive Drugs
NCT00202033PHASE4COMPLETEDImpact of Self-Monitoring Blood Glucose Frequency on Glycemic Control in Patients With Type 2 Diabetes
NCT00205660PHASE4COMPLETEDChanges in Adiposity, Metabolic Measures From Atypicals to Aripiprazole
NCT00212290PHASE4COMPLETEDInsulin Resistance and Central Nervous System (CNS) Function in Type 2 Diabetes
NCT00212303PHASE4COMPLETEDExercise Training in Type 2 Diabetes and Hypertension
NCT00225342PHASE4WITHDRAWNStudy Protocol for Rosiglitazone Versus Gliclazide in Diabetics With Angina
NCT00238472PHASE4COMPLETEDA Pilot Study to Evaluate the Effects of Nateglinide vs. Glibenclamide on Renal Hemodynamics and Albumin Excretion
NCT00239538PHASE4COMPLETEDSMOOTH - Blood Pressure Control in Diabetic/Obese Patients
NCT00240253PHASE4COMPLETEDA Study Evaluating the Efficacy and Safety of Adding Symlin® to Lantus® (Insulin Glargine) in Subjects With Type 2 Diabetes
NCT00240422PHASE4COMPLETEDTrial to Compare the Effects of Either Telmisartan (40-80 mg PO Once Daily) or Ramipril (5-10 mg PO Once Daily) on Renal Endothelial Dysfunction in Hypertensive Patients With Type 2 Diabetes