Page last updated: 2024-08-07 17:16:04
Dipeptidyl peptidase 8
A dipeptidyl peptidase 8 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q6V1X1]
Synonyms
DP8;
EC 3.4.14.5;
Dipeptidyl peptidase IV-related protein 1;
DPRP-1;
Dipeptidyl peptidase VIII;
DPP VIII;
Prolyl dipeptidase DPP8
Research
Bioassay Publications (50)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 19 (38.00) | 29.6817 |
| 2010's | 29 (58.00) | 24.3611 |
| 2020's | 2 (4.00) | 2.80 |
Compounds (16)
Drugs with Inhibition Measurements
Synthesis, nitric oxide release, and dipeptidyl peptidase-4 inhibition of sitagliptin derivatives as new multifunctional antidiabetic agents.Bioorganic & medicinal chemistry letters, , 12-15, Volume: 28, Issue:23-24, 2018
Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling.European journal of medicinal chemistry, , Oct-20, Volume: 139, 2017
Approaches towards the development of chimeric DPP4/ACE inhibitors for treating metabolic syndrome.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 27, Issue:11, 2017
Design, Synthesis, and Pharmacological Evaluation of Fused β-Homophenylalanine Derivatives as Potent DPP-4 Inhibitors.ACS medicinal chemistry letters, , May-14, Volume: 6, Issue:5, 2015
Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.European journal of medicinal chemistry, , Oct-30, Volume: 86, 2014
Design, synthesis and biological evaluation of hetero-aromatic moieties substituted pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.European journal of medicinal chemistry, , Mar-21, Volume: 75, 2014
Discovery of Imigliptin, a Novel Selective DPP-4 Inhibitor for the Treatment of Type 2 Diabetes.ACS medicinal chemistry letters, , Aug-14, Volume: 5, Issue:8, 2014
(R)-3-amino-1-((3aS,7aS)-octahydro-1H-indol-1-yl)-4-(2,4,5-trifluorophenyl)butan-1-one derivatives as potent inhibitors of dipeptidyl peptidase-4: design, synthesis, biological evaluation, and molecular modeling.Bioorganic & medicinal chemistry, , Dec-01, Volume: 22, Issue:23, 2014
Discovery of C-(1-aryl-cyclohexyl)-methylamines as selective, orally available inhibitors of dipeptidyl peptidase IV.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 24, Issue:3, 2014
Synthesis and biological evaluation of novel benzyl-substituted (S)-phenylalanine derivatives as potent dipeptidyl peptidase 4 inhibitors.Bioorganic & medicinal chemistry, , Sep-15, Volume: 21, Issue:18, 2013
Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors.Bioorganic & medicinal chemistry, , Oct-01, Volume: 20, Issue:19, 2012
Synthesis and evaluation of [(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]cyclohexanes and 4-[(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]piperidines as DPP-4 inhibitors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 21, Issue:6, 2011
Structure-activity relationship studies on isoindoline inhibitors of dipeptidyl peptidases 8 and 9 (DPP8, DPP9): is DPP8-selectivity an attainable goal?Journal of medicinal chemistry, , Aug-25, Volume: 54, Issue:16, 2011
Substituted 4-carboxymethylpyroglutamic acid diamides as potent and selective inhibitors of fibroblast activation protein.Journal of medicinal chemistry, , Sep-23, Volume: 53, Issue:18, 2010
(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 20, Issue:12, 2010
Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 2009
Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 19, Issue:7, 2009
Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: identification of dipeptide derived leads.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 18, Issue:14, 2008
(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 17, Issue:1, 2007
Modeling assisted rational design of novel, potent, and selective pyrrolopyrimidine DPP-4 inhibitors.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 17, Issue:14, 2007
Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 17, Issue:12, 2007
Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: close analogs of JANUVIA (sitagliptin phosphate).Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 17, Issue:12, 2007
Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 16, Issue:12, 2006
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.Journal of medicinal chemistry, , Jan-13, Volume: 48, Issue:1, 2005
Identification and structure-activity relationship exploration of uracil-based benzoic acid and ester derivatives as novel dipeptidyl Peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus.European journal of medicinal chemistry, , Dec-05, Volume: 225, 2021
Rapid generation of novel benzoic acid-based xanthine derivatives as highly potent, selective and long acting DPP-4 inhibitors: Scaffold-hopping and prodrug study.European journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
Identification of novel uracil derivatives incorporating benzoic acid moieties as highly potent Dipeptidyl Peptidase-IV inhibitors.Bioorganic & medicinal chemistry, , 02-15, Volume: 27, Issue:4, 2019
Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling.European journal of medicinal chemistry, , Oct-20, Volume: 139, 2017
Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.European journal of medicinal chemistry, , Oct-30, Volume: 86, 2014
Synthesis and biological evaluation of pyrrolidine-2-carbonitrile and 4-fluoropyrrolidine-2-carbonitrile derivatives as dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes.Bioorganic & medicinal chemistry, , Dec-01, Volume: 21, Issue:23, 2013
Synthesis and biological evaluation of novel benzyl-substituted (S)-phenylalanine derivatives as potent dipeptidyl peptidase 4 inhibitors.Bioorganic & medicinal chemistry, , Sep-15, Volume: 21, Issue:18, 2013
Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors.Bioorganic & medicinal chemistry, , Oct-01, Volume: 20, Issue:19, 2012
Structure-activity relationship studies on isoindoline inhibitors of dipeptidyl peptidases 8 and 9 (DPP8, DPP9): is DPP8-selectivity an attainable goal?Journal of medicinal chemistry, , Aug-25, Volume: 54, Issue:16, 2011
Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 20, Issue:12, 2010
Substituted 4-carboxymethylpyroglutamic acid diamides as potent and selective inhibitors of fibroblast activation protein.Journal of medicinal chemistry, , Sep-23, Volume: 53, Issue:18, 2010
(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 20, Issue:12, 2010
Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 2009
Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 19, Issue:7, 2009
Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: identification of dipeptide derived leads.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 18, Issue:14, 2008
Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 16, Issue:12, 2006
Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the trJournal of medicinal chemistry, , Oct-19, Volume: 49, Issue:21, 2006
2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]- 1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 15, Issue:3, 2005
Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 15, Issue:13, 2005
Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase.Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013
Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety.Journal of medicinal chemistry, , Oct-09, Volume: 51, Issue:19, 2008
Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 17, Issue:2, 2007
2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]- 1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 15, Issue:3, 2005
Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 15, Issue:13, 2005
Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling.European journal of medicinal chemistry, , Oct-20, Volume: 139, 2017
Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes.ACS medicinal chemistry letters, , May-12, Volume: 7, Issue:5, 2016
Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors.Bioorganic & medicinal chemistry, , Oct-01, Volume: 20, Issue:19, 2012
4-Substituted boro-proline dipeptides: synthesis, characterization, and dipeptidyl peptidase IV, 8, and 9 activities.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 22, Issue:17, 2012
Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety.Journal of medicinal chemistry, , Oct-09, Volume: 51, Issue:19, 2008
Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling.European journal of medicinal chemistry, , Oct-20, Volume: 139, 2017
Structure-activity relationship studies on isoindoline inhibitors of dipeptidyl peptidases 8 and 9 (DPP8, DPP9): is DPP8-selectivity an attainable goal?Journal of medicinal chemistry, , Aug-25, Volume: 54, Issue:16, 2011
Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: identification of dipeptide derived leads.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 18, Issue:14, 2008
Synthesis and dipeptidyl peptidase inhibition of N-(4-substituted-2,4-diaminobutanoyl)piperidines.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 16, Issue:18, 2006
Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors.Bioorganic & medicinal chemistry, , Oct-01, Volume: 20, Issue:19, 2012
(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 20, Issue:12, 2010
Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the trJournal of medicinal chemistry, , Oct-19, Volume: 49, Issue:21, 2006
Identification and structure-activity relationship exploration of uracil-based benzoic acid and ester derivatives as novel dipeptidyl Peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus.European journal of medicinal chemistry, , Dec-05, Volume: 225, 2021
Structural optimization of pyrazolo[1,5-a]pyrimidine derivatives as potent and highly selective DPP-4 inhibitors.European journal of medicinal chemistry, , Dec-15, Volume: 208, 2020
Rapid generation of novel benzoic acid-based xanthine derivatives as highly potent, selective and long acting DPP-4 inhibitors: Scaffold-hopping and prodrug study.European journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
Identification of novel uracil derivatives incorporating benzoic acid moieties as highly potent Dipeptidyl Peptidase-IV inhibitors.Bioorganic & medicinal chemistry, , 02-15, Volume: 27, Issue:4, 2019
Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes.ACS medicinal chemistry letters, , May-12, Volume: 7, Issue:5, 2016
Discovery of Imigliptin, a Novel Selective DPP-4 Inhibitor for the Treatment of Type 2 Diabetes.ACS medicinal chemistry letters, , Aug-14, Volume: 5, Issue:8, 2014
Novel pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors based on pharmacokinetic property-driven optimization.European journal of medicinal chemistry, , Volume: 52, 2012
Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors.Bioorganic & medicinal chemistry, , Oct-01, Volume: 20, Issue:19, 2012
Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV.Journal of medicinal chemistry, , Jan-27, Volume: 54, Issue:2, 2011
The highly potent and selective dipeptidyl peptidase IV inhibitors bearing a thienopyrimidine scaffold effectively treat type 2 diabetes.European journal of medicinal chemistry, , Volume: 46, Issue:1, 2011
Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV.Journal of medicinal chemistry, , May-17, Volume: 50, Issue:10, 2007
Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 25, Issue:24, 2015
Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.Journal of medicinal chemistry, , Apr-24, Volume: 57, Issue:8, 2014
Enables
This protein enables 4 target(s):
| Target | Category | Definition |
|---|
| aminopeptidase activity | molecular function | Catalysis of the hydrolysis of a single N-terminal amino acid residue from a polypeptide chain. [https://www.ebi.ac.uk/merops/about/glossary.shtml#AMINOPEPTIDASE, PMID:24157837] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| serine-type peptidase activity | molecular function | Catalysis of the hydrolysis of peptide bonds in a polypeptide chain by a catalytic mechanism that involves a catalytic triad consisting of a serine nucleophile that is activated by a proton relay involving an acidic residue (e.g. aspartate or glutamate) and a basic residue (usually histidine). [https://www.ebi.ac.uk/merops/about/glossary.shtml#CATTYPE] |
| dipeptidyl-peptidase activity | molecular function | Catalysis of the hydrolysis of N-terminal dipeptides from a polypeptide chain. [GOC:mb, https://www.ebi.ac.uk/merops/about/glossary.shtml#DIPEPTIDYL-PEPTIDASE] |
Located In
This protein is located in 2 target(s):
| Target | Category | Definition |
|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Involved In
This protein is involved in 4 target(s):
| Target | Category | Definition |
|---|
| proteolysis | biological process | The hydrolysis of proteins into smaller polypeptides and/or amino acids by cleavage of their peptide bonds. [GOC:bf, GOC:mah] |
| apoptotic process | biological process | A programmed cell death process which begins when a cell receives an internal (e.g. DNA damage) or external signal (e.g. an extracellular death ligand), and proceeds through a series of biochemical events (signaling pathway phase) which trigger an execution phase. The execution phase is the last step of an apoptotic process, and is typically characterized by rounding-up of the cell, retraction of pseudopodes, reduction of cellular volume (pyknosis), chromatin condensation, nuclear fragmentation (karyorrhexis), plasma membrane blebbing and fragmentation of the cell into apoptotic bodies. When the execution phase is completed, the cell has died. [GOC:cjm, GOC:dhl, GOC:ecd, GOC:go_curators, GOC:mtg_apoptosis, GOC:tb, ISBN:0198506732, PMID:18846107, PMID:21494263] |
| immune response | biological process | Any immune system process that functions in the calibrated response of an organism to a potential internal or invasive threat. [GO_REF:0000022, GOC:add] |
| negative regulation of programmed cell death | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of programmed cell death, cell death resulting from activation of endogenous cellular processes. [GOC:jl] |