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fatty acid binding protein 4

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Target id: 2534

Nomenclature: fatty acid binding protein 4

Family: Fatty acid-binding proteins

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 132 8q21.13 FABP4 fatty acid binding protein 4
Mouse - 132 3 2.56 cM Fabp4 fatty acid binding protein 4, adipocyte
Rat - 132 2q23 Fabp4 fatty acid binding protein 4
Previous and Unofficial Names Click here for help
adipocyte lipid-binding protein | adipocyte protein aP2 | AFABP | ALBP
Database Links Click here for help
Alphafold P15090 (Hs), P04117 (Mm), P70623 (Rn)
CATH/Gene3D 2.40.128.20
ChEMBL Target CHEMBL2083 (Hs), CHEMBL1075118 (Mm), CHEMBL2021755 (Rn)
Ensembl Gene ENSG00000170323 (Hs), ENSMUSG00000062515 (Mm), ENSRNOG00000010805 (Rn)
Entrez Gene 2167 (Hs), 11770 (Mm), 79451 (Rn)
Human Protein Atlas ENSG00000170323 (Hs)
KEGG Gene hsa:2167 (Hs), mmu:11770 (Mm), rno:79451 (Rn)
OMIM 600434 (Hs)
Pharos P15090 (Hs)
RefSeq Nucleotide NM_001442 (Hs), NM_024406 (Mm)
RefSeq Protein NP_001433 (Hs), NP_077717 (Mm)
SynPHARM 82981 (in complex with HTS01037)
UniProtKB P15090 (Hs), P04117 (Mm), P70623 (Rn)
Wikipedia FABP4 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of mouse adipocyte fatty acid binding ptortin bound by inhibitor.
PDB Id:  3HK1
Ligand:  HTS01037
Resolution:  1.7Å
Species:  Mouse
References:  1
Rank order of potency (Human)
oleic acid, palmitic acid, stearic acid, linoleic acid > α-linolenic acid, arachidonic acid  [4]

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

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
HM50316 Small molecule or natural product Primary target of this compound Hs Inhibition >9.0 pKi 2
⤷ pKi >9.0 (Ki <1x10-9 M) [2]
compound 13 [PMID: 17502136] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.7 pKi 5
⤷ pKi 8.7 (Ki 2x10-9 M) [5]
HTS01037 Small molecule or natural product Click here for species-specific activity table Mm Inhibition 6.2 pKi 1
⤷ pKi 6.2 (Ki 6.7x10-7 M) [1]
bindarit Small molecule or natural product Immunopharmacology Ligand Hs Binding 4.7 pKi 3
⤷ pKi 4.7 (Ki 1.9x10-5 M) [3]
Description: Measuring displacement of [3H]-oleic acid from hFABP4 in a competitive binding assay.
View species-specific inhibitor tables
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Immune regulation
Immuno Process:  Cytokine production & signalling

References

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1. Hertzel AV, Hellberg K, Reynolds JM, Kruse AC, Juhlmann BE, Smith AJ, Sanders MA, Ohlendorf DH, Suttles J, Bernlohr DA. (2009) Identification and characterization of a small molecule inhibitor of Fatty Acid binding proteins. J Med Chem, 52 (19): 6024-31. [PMID:19754198]

2. Liu X, Huang X, Lin W, Wang D, Diao Y, Li H, Hui X, Wang Y, Xu A, Wu D et al.. (2011) New aromatic substituted pyrazoles as selective inhibitors of human adipocyte fatty acid-binding protein. Bioorg Med Chem Lett, 21 (10): 2949-52. [PMID:21481589]

3. Oddi S, Scipioni L, Totaro A, Angelucci C, Dufrusine B, Sabatucci A, Tortolani D, Coletta I, Alisi MA, Polenzani L et al.. (2019) The anti-inflammatory agent bindarit acts as a modulator of fatty acid-binding protein 4 in human monocytic cells. Sci Rep, 9 (1): 15155. [PMID:31641194]

4. Richieri GV, Ogata RT, Kleinfeld AM. (1994) Equilibrium constants for the binding of fatty acids with fatty acid-binding proteins from adipocyte, intestine, heart, and liver measured with the fluorescent probe ADIFAB. J Biol Chem, 269 (39): 23918-30. [PMID:7929039]

5. Sulsky R, Magnin DR, Huang Y, Simpkins L, Taunk P, Patel M, Zhu Y, Stouch TR, Bassolino-Klimas D, Parker R et al.. (2007) Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP). Bioorg Med Chem Lett, 17 (12): 3511-5. [PMID:17502136]

How to cite this page

Fatty acid-binding proteins: fatty acid binding protein 4. Last modified on 18/07/2020. Accessed on 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2534.