S9: Prolyl oligopeptidase | Enzymes | IUPHAR/BPS Guide to MALARIA PHARMACOLOGY

S9: Prolyl oligopeptidase C

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Enzymes

acylaminoacyl-peptide hydrolase Show summary »« Hide summary More detailed page go icon to follow link

dipeptidyl peptidase 4 C Show summary »« Hide summary More detailed page go icon to follow link

Target Id

1612

Nomenclature

dipeptidyl peptidase 4

Previous and unofficial names

Genes

DPP4 (Hs), Dpp4 (Mm), Dpp4 (Rn)

Ensembl ID

ENSG00000197635 (Hs), ENSMUSG00000035000 (Mm), ENSRNOG00000030763 (Rn)

UniProtKB AC

P27487 (Hs), P28843 (Mm), P14740 (Rn)

EC number

3.4.14.5

Endogenous substrates

glucagon-like peptide 1

Inhibitors

saxagliptin pK_i 9.2 [3]

linagliptin pK_i 9.0 [2]

vildagliptin pK_i 7.8 [3]

sitagliptin pIC₅₀ 8.1 [1]

Selective inhibitors

ZY15557 (Competitive) pK_i 8.3 [4]

dipeptidyl peptidase 8 Show summary »« Hide summary More detailed page go icon to follow link

Target Id

2356

Nomenclature

dipeptidyl peptidase 8

Previous and unofficial names

Genes

DPP8 (Hs), Dpp8 (Mm), Dpp8 (Rn)

Ensembl ID

ENSG00000074603 (Hs), ENSMUSG00000032393 (Mm), ENSRNOG00000019105 (Rn)

UniProtKB AC

Q6V1X1 (Hs), Q80YA7 (Mm)

EC number

3.4.14.5

dipeptidyl peptidase 9 Show summary »« Hide summary More detailed page go icon to follow link

fibroblast activation protein alpha Show summary »« Hide summary More detailed page go icon to follow link

prolyl endopeptidase Show summary »« Hide summary More detailed page go icon to follow link

prolyl endopeptidase like Show summary »« Hide summary More detailed page go icon to follow link

References

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1. 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]

2. 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]

3. 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]

4. 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]

How to cite this family page

Database page citation:

S9: Prolyl oligopeptidase. Accessed on 09/06/2023. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=758.

Concise Guide to PHARMACOLOGY citation:

Alexander SP, Fabbro D, Kelly E, Mathie A, Peters JA, Veale EL et al. (2021) THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: Enzymes. Br J Pharmacol. 178 Suppl 1:S313-S411.