dipeptidyl peptidase 4

Target id: 1612

Nomenclature: dipeptidyl peptidase 4

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

   GtoImmuPdb view: OFF :     Currently no data for dipeptidyl peptidase 4 in GtoImmuPdb

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
Previous and Unofficial Names
adenosine deaminase complexing protein 2 | bile canaliculus domain-specific membrane glycoprotein | dipeptidyl peptidase IV | DPP IV | GP110 glycoprotein | T-cell activation antigen CD26 | THAM | ADCP2 | dipeptidyl-peptidase 4
Database Links
Specialist databases
MEROPS S09.003 (Hs)
Other databases
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Cocrystal structure of dipeptidyl-peptidase 4 with an indole scaffold inhibitor
PDB Id:  4PV7
Ligand:  compound 1 [Xiao et al. 2014]
Resolution:  3.24Å
Species:  Human
References:  8
Enzyme Reaction
EC Number: 3.4.14.5
Substrates and Reaction Kinetics
Substrate Sp. Property Value Units Standard property Standard value Assay description Assay conditions Comments Reference
glucagon-like peptide 1 Hs - -

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
saxagliptin Hs Inhibition 9.2 pKi 5
pKi 9.2 (Ki 6x10-10 M) [5]
omarigliptin Hs Inhibition 9.1 pKi 1
pKi 9.1 (Ki 8x10-10 M) [1]
linagliptin Hs Inhibition 9.0 pKi 4
pKi 9.0 (Ki 1x10-9 M) [4]
compound 24dd [PMID: 20684603] Hs Inhibition 8.9 pKi 7
pKi 8.9 (Ki 1.4x10-9 M) [7]
ZY15557 Hs Competitive 8.3 pKi 6
pKi 8.3 (Ki 5.53x10-9 M) [6]
vildagliptin Hs Inhibition 7.8 pKi 5
pKi 7.8 (Ki 1.7x10-8 M) [5]
alogliptin Hs Inhibition 8.5 pIC50 9
pIC50 8.5 (IC50 3.4x10-9 M) [9]
sitagliptin Hs Inhibition 8.1 pIC50 2
pIC50 8.1 (IC50 8.6x10-9 M) [2]
compound 1 [Xiao et al. 2014] Hs Inhibition 6.6 pIC50 8
pIC50 6.6 (IC50 2.328x10-7 M) [8]
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Affinity Units Reference
begelomab Hs Binding ~10.0 pKd 3
pKd ~10.0 (Kd ~1x10-10 M) [3]

References

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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. 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 Pharmacol42 (4): 229-33. [PMID:20927248]

3. 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.

4. 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]

5. 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 Targets10 (1): 71-87. [PMID:19149538]

6. 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]

7. 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]

8. 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.

9. 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 Chem52: 205-12. [PMID:22475866]

How to cite this page

S9: Prolyl oligopeptidase: dipeptidyl peptidase 4. Last modified on 05/08/2017. Accessed on 17/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1612.