dipeptidyl peptidase 9

Target id: 2357

Nomenclature: dipeptidyl peptidase 9

Family: S9: Prolyl oligopeptidase

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for dipeptidyl peptidase 9 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 892 19p13.3 DPP9 dipeptidyl peptidase 9
Mouse - 862 17 D Dpp9 dipeptidylpeptidase 9
Rat - - 9q11 Dpp9 dipeptidyl peptidase 9
Previous and Unofficial Names
dipeptidyl peptidase IX | DP9 | DPP IX | DPRP2 | dipeptidyl-peptidase 9
Database Links
Specialist databases
MEROPS S09.019 (Hs)
Other databases
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 3.4.14.5

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
talabostat Hs Inhibition 9.1 pKi 1
pKi 9.1 (Ki 7.6x10-10 M) [1]
compound 24dd [PMID: 20684603] Hs Inhibition 6.7 pKi 3
pKi 6.7 (Ki 1.9x10-7 M) [3]
1G244 Hs Inhibition 7.3 pIC50 5
pIC50 7.3 (IC50 5.3x10-8 M) [5]
teneligliptin Hs Inhibition 6.3 pIC50 6
pIC50 6.3 (IC50 5.4x10-7 M) [6]
compound 9 [PMID: 20718420] Hs Inhibition 5.6 pIC50 4
pIC50 5.6 (IC50 2.7x10-6 M) [4]
Clinically-Relevant Mutations and Pathophysiology
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. 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]

5. 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]

6. 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 18/04/2018. Accessed on 21/07/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2357.