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dipeptidyl peptidase 9

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Target not currently curated in GtoImmuPdb

Target id: 2357

Nomenclature: dipeptidyl peptidase 9

Family: S9: Prolyl oligopeptidase

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 863 19p13.3 DPP9 dipeptidyl peptidase 9
Mouse - 862 17 D Dpp9 dipeptidylpeptidase 9
Rat - - 9q11 Dpp9 dipeptidyl peptidase 9
Previous and Unofficial Names Click here for help
dipeptidyl peptidase IX | DP9 | DPP IX | DPRP2 | dipeptidyl-peptidase 9
Database Links Click here for help
Specialist databases
MEROPS S09.019 (Hs)
Other databases
Alphafold Q86TI2 (Hs), Q8BVG4 (Mm)
BRENDA 3.4.14.5
CATH/Gene3D 3.40.50.1820
ChEMBL Target CHEMBL4793 (Hs), CHEMBL3259484 (Mm)
Ensembl Gene ENSG00000142002 (Hs), ENSMUSG00000001229 (Mm), ENSRNOG00000050748 (Rn)
Entrez Gene 91039 (Hs), 224897 (Mm), 301130 (Rn)
Human Protein Atlas ENSG00000142002 (Hs)
KEGG Enzyme 3.4.14.5
KEGG Gene hsa:91039 (Hs), mmu:224897 (Mm), rno:301130 (Rn)
OMIM 608258 (Hs)
Orphanet ORPHA353250 (Hs)
Pharos Q86TI2 (Hs)
RefSeq Nucleotide NM_139159 (Hs), NM_172624 (Mm)
RefSeq Protein NP_631898 (Hs), NP_766212 (Mm)
UniProtKB Q86TI2 (Hs), Q8BVG4 (Mm)
Wikipedia DPP9 (Hs)
Enzyme Reaction Click here for help
EC Number: 3.4.14.5

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
talabostat Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 9.1 pKi 1
⤷ pKi 9.1 (Ki 7.6x10-10 M) [1]
compound 24dd [PMID: 20684603] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.7 pKi 3
⤷ pKi 6.7 (Ki 1.9x10-7 M) [3]
ICeD-2 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.1 pIC50 4
⤷ pIC50 9.1 (IC50 9x10-10 M) [4]
1G244 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.3 pIC50 6
⤷ pIC50 7.3 (IC50 5.3x10-8 M) [6]
teneligliptin Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.3 pIC50 7
⤷ pIC50 6.3 (IC50 5.4x10-7 M) [7]
compound 9 [PMID: 20718420] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.6 pIC50 5
⤷ pIC50 5.6 (IC50 2.7x10-6 M) [5]
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Idiopathic pulmonary fibrosis
Disease Ontology: DOID:0050156
Orphanet: ORPHA2032
References:  2

References

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1. Connolly BA, Sanford DG, Chiluwal AK, Healey SE, Peters DE, Dimare MT, Wu W, Liu Y, Maw H, Zhou Y et al.. (2008) Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety. J Med Chem, 51 (19): 6005-13. [PMID:18783201]

2. Fingerlin TE, Murphy E, Zhang W, Peljto AL, Brown KK, Steele MP, Loyd JE, Cosgrove GP, Lynch D, Groshong S et al.. (2013) Genome-wide association study identifies multiple susceptibility loci for pulmonary fibrosis. Nat Genet, 45 (6): 613-20. [PMID:23583980]

3. Meng W, Brigance RP, Chao HJ, Fura A, Harrity T, Marcinkeviciene J, O'Connor SP, Tamura JK, Xie D, Zhang Y et al.. (2010) Discovery of 6-(aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as potent, selective dipeptidyl peptidase-4 (DPP4) inhibitors. J Med Chem, 53 (15): 5620-8. [PMID:20684603]

4. Moore KP, Schwaid AG, Tudor M, Park S, Beshore DC, Converso A, Shipe WD, Anand R, Lan P, Moningka R et al.. (2022) A Phenotypic Screen Identifies Potent DPP9 Inhibitors Capable of Killing HIV-1 Infected Cells. ACS Chem Biol, 17 (9): 2595-2604. [PMID:36044633]

5. 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]

6. Wu JJ, Tang HK, Yeh TK, Chen CM, Shy HS, Chu YR, Chien CH, Tsai TY, Huang YC, Huang YL et al.. (2009) Biochemistry, pharmacokinetics, and toxicology of a potent and selective DPP8/9 inhibitor. Biochem Pharmacol, 78 (2): 203-10. [PMID:19439267]

7. Yoshida T, Akahoshi F, Sakashita H, Kitajima H, Nakamura M, Sonda S, Takeuchi M, Tanaka Y, Ueda N, Sekiguchi S et al.. (2012) Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. Bioorg Med Chem, 20 (19): 5705-19. [PMID:22959556]

How to cite this page

S9: Prolyl oligopeptidase: dipeptidyl peptidase 9. Last modified on 31/10/2022. Accessed on 22/03/2023. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2357.