Top ▲
Target not currently curated in GtoImmuPdb
Target id: 1612
Nomenclature: dipeptidyl peptidase 4
Family: S9: Prolyl oligopeptidase
Annotation status:
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 | - | 766 | 2q23-qter | DPP4 | dipeptidyl peptidase 4 | |
Mouse | - | 760 | 2 C2-D | Dpp4 | dipeptidylpeptidase 4 | |
Rat | - | 767 | 3q21 | Dpp4 | dipeptidylpeptidase 4 |
Database Links ![]() |
|
Specialist databases | |
MEROPS | S09.003 (Hs) |
Other databases | |
BRENDA | 3.4.14.5 |
CATH/Gene3D | 3.40.50.1820 |
ChEMBL Target | CHEMBL284 (Hs) |
DrugBank Target | P27487 (Hs) |
Ensembl Gene | ENSG00000197635 (Hs), ENSMUSG00000035000 (Mm), ENSRNOG00000030763 (Rn) |
Entrez Gene | 1803 (Hs), 13482 (Mm), 25253 (Rn) |
Human Protein Atlas | ENSG00000197635 (Hs) |
KEGG Enzyme | 3.4.14.5 |
KEGG Gene | hsa:1803 (Hs), mmu:13482 (Mm), rno:25253 (Rn) |
OMIM | 102720 (Hs) |
RefSeq Nucleotide | NM_001935 (Hs), NM_010074 (Mm), NM_001159543 (Mm), NM_012789 (Rn) |
RefSeq Protein | NP_001926 (Hs), NP_034204 (Mm), NP_001153015 (Mm), NP_036921 (Rn) |
SynPHARM |
78493 (in complex with alogliptin) 81938 (in complex with compound 1 (Xiao et al. 2014)) 78503 (in complex with linagliptin) 78507 (in complex with saxagliptin) 78465 (in complex with sitagliptin) 85060 (in complex with teneligliptin) 78481 (in complex with vildagliptin) |
UniProtKB | P27487 (Hs), P28843 (Mm), P14740 (Rn) |
Wikipedia | DPP4 (Hs) |
Selected 3D Structures ![]() |
|||||||||||||
![]() |
|
Enzyme Reaction ![]() |
||||
|
Substrates and Reaction Kinetics ![]() |
||||||||||||||||||||||||
|
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 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|
Antibodies | |||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | Click column headers to sort | ||||||||||||||||||||||||||||||||||||||||||||||||
|
1. Biftu T, Sinha-Roy R, Chen P, Qian X, Feng D, Kuethe JT, Scapin G, Gao YD, Yan Y, Krueger D et al.. (2014) Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. J. Med. Chem., 57 (8): 3205-12. [PMID:24660890]
2. 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]
3. Davis JA, Singh S, Sethi S, Roy S, Mittra S, Rayasam G, Bansal V, Sattigeri J, Ray A. (2010) Nature of action of Sitagliptin, the dipeptidyl peptidase-IV inhibitor in diabetic animals. Indian J Pharmacol, 42 (4): 229-33. [PMID:20927248]
4. Di Naro AF. (2014) Anti-CD26 Antibodies and Uses Thereof. Patent number: EP2767549 A1. Assignee: Adienne S.A.. Priority date: 19/02/2013. Publication date: 20/08/2014.
5. Eckhardt M, Langkopf E, Mark M, Tadayyon M, Thomas L, Nar H, Pfrengle W, Guth B, Lotz R, Sieger P et al.. (2007) 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. J. Med. Chem., 50 (26): 6450-3. [PMID:18052023]
6. Gupta R, Walunj SS, Tokala RK, Parsa KV, Singh SK, Pal M. (2009) Emerging drug candidates of dipeptidyl peptidase IV (DPP IV) inhibitor class for the treatment of Type 2 Diabetes. Curr Drug Targets, 10 (1): 71-87. [PMID:19149538]
7. Jain MR, Joharapurkar AA, Kshirsagar SG, Patel VJ, Bahekar RH, Patel HV, Jadav PA, Patel PR, Desai RC. (2017) ZY15557, a novel, long acting inhibitor of dipeptidyl peptidase-4, for the treatment of Type 2 diabetes mellitus. Br. J. Pharmacol., 174 (14): 2346-2357. [PMID:28452143]
8. 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]
9. 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]
10. Xiao P, Guo R, Huang S, Cui H, Ye S, Zhang Z. (2014) Discovery of dipeptidyl peptidase IV (DPP4) inhibitors based on a novel indole scaffold. Chin.Chem. Lett., 25 (5): 673-676.
11. Xie H, Zeng L, Zeng S, Lu X, Zhang G, Zhao X, Cheng N, Tu Z, Li Z, Xu H et al.. (2012) Novel pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors based on pharmacokinetic property-driven optimization. Eur J Med Chem, 52: 205-12. [PMID:22475866]
12. 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 4. Last modified on 18/04/2018. Accessed on 20/02/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1612.