dipeptidyl peptidase 8 | S9: Prolyl oligopeptidase | IUPHAR/BPS Guide to PHARMACOLOGY

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dipeptidyl peptidase 8

Target not currently curated in GtoImmuPdb

Target id: 2356

Nomenclature: dipeptidyl peptidase 8

Family: S9: Prolyl oligopeptidase

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 898 15q22 DPP8 dipeptidyl peptidase 8
Mouse - 892 9 D Dpp8 dipeptidylpeptidase 8
Rat - - 8q24 Dpp8 dipeptidylpeptidase 8
Previous and Unofficial Names
dipeptidyl peptidase IV-related protein-1 | dipeptidyl peptidase VIII | DP8 | DPP VIII | DPRP1 | dipeptidyl-peptidase 8
Database Links
Specialist databases
MEROPS S09.018 (Hs)
Other databases
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Enzyme Reaction
EC Number:

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

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
talabostat Hs Inhibition 8.8 pKi 1
pKi 8.8 (Ki 1.5x10-9 M) [1]
compound 24dd [PMID: 20684603] Hs Inhibition 6.6 pKi 3
pKi 6.6 (Ki 2.7x10-7 M) [3]
compound 18 [PMID: 15664838] Hs Inhibition 7.9 pIC50 2
pIC50 7.9 (IC50 1.4x10-8 M) [2]
1G244 Hs Inhibition 7.8 pIC50 5
pIC50 7.8 (IC50 1.4x10-8 M) [5]
teneligliptin Hs Inhibition 6.6 pIC50 6
pIC50 6.6 (IC50 2.6x10-7 M) [6]
compound 9 [PMID: 20718420] Hs Inhibition 5.4 pIC50 4
pIC50 5.4 (IC50 3.7x10-6 M) [4]


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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. Jiaang WT, Chen YS, Hsu T, Wu SH, Chien CH, Chang CN, Chang SP, Lee SJ, Chen X. (2005) Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8. Bioorg. Med. Chem. Lett., 15 (3): 687-91. [PMID:15664838]

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 8. Last modified on 18/04/2018. Accessed on 18/10/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2356.