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fatty acid synthase

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Target id: 2608

Nomenclature: fatty acid synthase

Family: 2.3.1.- Acyltransferases

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 2511 17q25.3 FASN fatty acid synthase
Mouse - 2504 11 84.56 cM Fasn fatty acid synthase
Rat - 2505 10q32.3 Fasn fatty acid synthase
Previous and Unofficial Names Click here for help
FAS
Database Links Click here for help
Alphafold P49327 (Hs), P19096 (Mm), P12785 (Rn)
BRENDA 2.3.1.85
CATH/Gene3D 1.10.1470.20, 3.40.47.10
ChEMBL Target CHEMBL4158 (Hs), CHEMBL1795189 (Mm), CHEMBL3783 (Rn)
DrugBank Target P49327 (Hs)
Ensembl Gene ENSG00000169710 (Hs), ENSMUSG00000025153 (Mm), ENSRNOG00000045636 (Rn)
Entrez Gene 2194 (Hs), 14104 (Mm), 50671 (Rn)
Human Protein Atlas ENSG00000169710 (Hs)
KEGG Enzyme 2.3.1.85
KEGG Gene hsa:2194 (Hs), mmu:14104 (Mm), rno:50671 (Rn)
OMIM 600212 (Hs)
Pharos P49327 (Hs)
RefSeq Nucleotide NM_004104 (Hs), NM_007988 (Mm), NM_017332 (Rn)
RefSeq Protein NP_004095 (Hs), NP_032014 (Mm), NP_059028 (Rn)
SynPHARM 82454 (in complex with GSK2194069)
UniProtKB P49327 (Hs), P19096 (Mm), P12785 (Rn)
Wikipedia FASN (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  X-ray structure of human Fatty Acid Synthase Psi/KR Tri-Domain complexed with NADPH and GSK2194069.
PDB Id:  4PIV
Ligand:  GSK2194069
Resolution:  2.3Å
Species:  Human
References:  2
Enzyme Reaction Click here for help
EC Number: 2.3.1.85

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
orlistat Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 6.6 pKi 1
⤷ pKi 6.6 (Ki 2.8x10-7 M) [1]
Description: Inhibition of recombinant FASN thioesterase domain by fluorogenic assay
GSK2194069 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 8.1 pIC50 2
⤷ pIC50 8.1 (IC50 7.7x10-9 M) [2]
orlistat Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 5.9 pIC50 3
⤷ pIC50 5.9 (IC50 1.35x10-6 M) [3]
Description: Inhibition of FAS thioesterase domain by fluorogenic assay
Immuno Process Associations
Immuno Process:  Immune system development
Immuno Process:  Cytokine production & signalling

References

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1. Abramson HN. (2011) The lipogenesis pathway as a cancer target. J Med Chem, 54 (16): 5615-38. [PMID:21726077]

2. Hardwicke MA, Rendina AR, Williams SP, Moore ML, Wang L, Krueger JA, Plant RN, Totoritis RD, Zhang G, Briand J et al.. (2014) A human fatty acid synthase inhibitor binds β-ketoacyl reductase in the keto-substrate site. Nat Chem Biol, 10 (9): 774-9. [PMID:25086508]

3. Richardson RD, Ma G, Oyola Y, Zancanella M, Knowles LM, Cieplak P, Romo D, Smith JW. (2008) Synthesis of novel beta-lactone inhibitors of fatty acid synthase. J Med Chem, 51 (17): 5285-96. [PMID:18710210]

How to cite this page

2.3.1.- Acyltransferases: fatty acid synthase. Last modified on 01/10/2021. Accessed on 04/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2608.