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fibroblast activation protein alpha

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Target not currently curated in GtoImmuPdb

Target id: 2365

Nomenclature: fibroblast activation protein alpha

Family: S9: Prolyl oligopeptidase

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 760 2q24.2 FAP fibroblast activation protein alpha
Mouse 1 761 2 35.85 cM Fap fibroblast activation protein
Rat - 761 3q21 Fap fibroblast activation protein, alpha
Previous and Unofficial Names Click here for help
DPPIV | seprase
Database Links Click here for help
Specialist databases
MEROPS S09.007 (Hs)
Other databases
Alphafold Q12884 (Hs), P97321 (Mm)
BRENDA 3.4.21.-
CATH/Gene3D 3.40.50.1820
ChEMBL Target CHEMBL4683 (Hs), CHEMBL5769 (Mm)
Ensembl Gene ENSG00000078098 (Hs), ENSMUSG00000000392 (Mm), ENSRNOG00000005679 (Rn)
Entrez Gene 2191 (Hs), 14089 (Mm), 192203 (Rn)
Human Protein Atlas ENSG00000078098 (Hs)
KEGG Enzyme 3.4.21.-
KEGG Gene hsa:2191 (Hs), mmu:14089 (Mm), rno:192203 (Rn)
OMIM 600403 (Hs)
Pharos Q12884 (Hs)
RefSeq Nucleotide NM_004460 (Hs), NM_007986 (Mm), NM_138850 (Rn)
RefSeq Protein NP_004451 (Hs), NP_032012 (Mm), NP_620205 (Rn)
UniProtKB Q12884 (Hs), P97321 (Mm)
Wikipedia FAP (Hs)
Enzyme Reaction Click here for help
EC Number: 3.4.21.-

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
compound 9 [PMID: 20718420] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.7 pIC50 2
⤷ pIC50 7.7 (IC50 1.9x10-8 M) [2]
ARI-3099 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.4 pIC50 1
⤷ pIC50 7.4 (IC50 3.6x10-8 M) [1]

References

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1. Poplawski SE, Lai JH, Li Y, Jin Z, Liu Y, Wu W, Wu Y, Zhou Y, Sudmeier JL, Sanford DG et al.. (2013) Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase. J Med Chem, 56 (9): 3467-77. [PMID:23594271]

2. Tsai TY, Yeh TK, Chen X, Hsu T, Jao YC, Huang CH, Song JS, Huang YC, Chien CH, Chiu JH et al.. (2010) Substituted 4-carboxymethylpyroglutamic acid diamides as potent and selective inhibitors of fibroblast activation protein. J Med Chem, 53 (18): 6572-83. [PMID:20718420]

How to cite this page

S9: Prolyl oligopeptidase: fibroblast activation protein alpha. Last modified on 09/04/2018. Accessed on 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2365.