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Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 898 | 15q22.31 | DPP8 | dipeptidyl peptidase 8 | |
Mouse | - | 892 | 9 C | 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 | |
Alphafold | Q6V1X1 (Hs), Q80YA7 (Mm) |
BRENDA | 3.4.14.5 |
CATH/Gene3D | 3.40.50.1820 |
ChEMBL Target | CHEMBL4657 (Hs) |
Ensembl Gene | ENSG00000074603 (Hs), ENSMUSG00000032393 (Mm), ENSRNOG00000019105 (Rn) |
Entrez Gene | 54878 (Hs), 74388 (Mm) |
Human Protein Atlas | ENSG00000074603 (Hs) |
KEGG Enzyme | 3.4.14.5 |
KEGG Gene | hsa:54878 (Hs), mmu:74388 (Mm) |
OMIM | 606819 (Hs) |
Pharos | Q6V1X1 (Hs) |
RefSeq Nucleotide | NM_017743 (Hs), NM_130434 (Hs), NM_197960 (Hs), NM_197961 (Hs), NM_028906 (Mm) |
RefSeq Protein | NP_932064 (Hs), NP_932065 (Hs), NP_569118 (Hs), NP_060213 (Hs), NP_083182 (Mm) |
UniProtKB | Q6V1X1 (Hs), Q80YA7 (Mm) |
Wikipedia | DPP8 (Hs) |
Enzyme Reaction | ||||
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Substrates and Reaction Kinetics | ||||||||||||||||||||||||||||||||||||
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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 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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1. Ajami K, Pitman MR, Wilson CH, Park J, Menz RI, Starr AE, Cox JH, Abbott CA, Overall CM, Gorrell MD. (2008) Stromal cell-derived factors 1alpha and 1beta, inflammatory protein-10 and interferon-inducible T cell chemo-attractant are novel substrates of dipeptidyl peptidase 8. FEBS Lett, 582 (5): 819-25. [PMID:18275857]
2. Benramdane S, De Loose J, Beyens O, Van Rymenant Y, Vliegen G, Augustyns K, De Winter H, De Meester I, Van der Veken P. (2022) Vildagliptin-Derived Dipeptidyl Peptidase 9 (DPP9) Inhibitors: Identification of a DPP8/9-Specific Lead. ChemMedChem, 17 (15): e202200097. [PMID:35760756]
3. Benramdane S, De Loose J, Filippi N, Espadinha M, Beyens O, Rymenant YV, Dirkx L, Bozdag M, Feijens PB, Augustyns K et al.. (2023) Highly Selective Inhibitors of Dipeptidyl Peptidase 9 (DPP9) Derived from the Clinically Used DPP4-Inhibitor Vildagliptin. J Med Chem, 66 (18): 12717-12738. [PMID:37721854]
4. 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]
5. 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]
6. 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]
7. 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]
8. 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]
9. Van Goethem S, Matheeussen V, Joossens J, Lambeir AM, Chen X, De Meester I, Haemers A, Augustyns K, Van der Veken P. (2011) Structure-activity relationship studies on isoindoline inhibitors of dipeptidyl peptidases 8 and 9 (DPP8, DPP9): is DPP8-selectivity an attainable goal?. J Med Chem, 54 (16): 5737-46. [PMID:21711053]
10. 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]
11. 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]
S9: Prolyl oligopeptidase: dipeptidyl peptidase 8. Last modified on 10/10/2023. Accessed on 19/09/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2356.