Page last updated: 2024-08-07 17:30:24
Dipeptidyl peptidase 2
A dipeptidyl peptidase 2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9UHL4]
Synonyms
EC 3.4.14.2;
Dipeptidyl aminopeptidase II;
Dipeptidyl peptidase 7;
Dipeptidyl peptidase II;
DPP II;
Quiescent cell proline dipeptidase
Research
Bioassay Publications (38)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 1 (2.63) | 18.2507 |
2000's | 21 (55.26) | 29.6817 |
2010's | 15 (39.47) | 24.3611 |
2020's | 1 (2.63) | 2.80 |
Compounds (14)
Drugs with Inhibition Measurements
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
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
Design, synthesis, and SAR of potent and selective dipeptide-derived inhibitors for dipeptidyl peptidases.Journal of medicinal chemistry, , Nov-06, Volume: 46, Issue:23, 2003
Development of potent and selective dipeptidyl peptidase II inhibitors.Bioorganic & medicinal chemistry letters, , Oct-21, Volume: 12, Issue:20, 2002
Approaches towards the development of chimeric DPP4/ACE inhibitors for treating metabolic syndrome.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 27, Issue:11, 2017
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
(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
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
(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
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
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
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
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 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
(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
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
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
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
Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 15, Issue:13, 2005
Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 15, Issue:3, 2005
4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors.Bioorganic & medicinal chemistry letters, , Jan-05, Volume: 14, Issue:1, 2004
Identification of BR102910 as a selective fibroblast activation protein (FAP) inhibitor.Bioorganic & medicinal chemistry letters, , 04-01, Volume: 37, 2021
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
Dipeptidyl peptidase IV inhibitors for the treatment of diabetes.Journal of medicinal chemistry, , Aug-12, Volume: 47, Issue:17, 2004
Design, synthesis, and SAR of potent and selective dipeptide-derived inhibitors for dipeptidyl peptidases.Journal of medicinal chemistry, , Nov-06, Volume: 46, Issue:23, 2003
Development of potent and selective dipeptidyl peptidase II inhibitors.Bioorganic & medicinal chemistry letters, , Oct-21, Volume: 12, Issue:20, 2002
Structure-activity relationships of boronic acid inhibitors of dipeptidyl peptidase IV. 1. Variation of the P2 position of Xaa-boroPro dipeptides.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
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
Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 15, Issue:13, 2005
Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 15, Issue:3, 2005
4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors.Bioorganic & medicinal chemistry letters, , Jan-05, Volume: 14, Issue:1, 2004
1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.Journal of medicinal chemistry, , Jun-19, Volume: 46, Issue:13, 2003
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
Medicinal chemistry approaches to the inhibition of dipeptidyl peptidase-4 for the treatment of type 2 diabetes.Bioorganic & medicinal chemistry, , Mar-01, Volume: 17, Issue:5, 2009
Structure-activity relationships of boronic acid inhibitors of dipeptidyl peptidase IV. 1. Variation of the P2 position of Xaa-boroPro dipeptides.Journal of medicinal chemistry, , May-10, Volume: 39, Issue:10, 1996
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
Gamma-amino-substituted analogues of 1-[(S)-2,4-diaminobutanoyl]piperidine as highly potent and selective dipeptidyl peptidase II inhibitors.Journal of medicinal chemistry, , May-20, Volume: 47, Issue:11, 2004
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
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] |
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] |
serine-type exopeptidase activity | molecular function | Catalysis of the hydrolysis of a peptide bond not more than three residues from the N- or C-terminus of 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). [GOC:mah, https://www.ebi.ac.uk/merops/about/glossary.shtml#CATTYPE, https://www.ebi.ac.uk/merops/about/glossary.shtml#EXOPEPTIDASE] |
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 6 target(s):
Target | Category | Definition |
extracellular region | cellular component | The space external to the outermost structure of a cell. For cells without external protective or external encapsulating structures this refers to space outside of the plasma membrane. This term covers the host cell environment outside an intracellular parasite. [GOC:go_curators] |
Golgi apparatus | cellular component | A membrane-bound cytoplasmic organelle of the endomembrane system that further processes the core oligosaccharides (e.g. N-glycans) added to proteins in the endoplasmic reticulum and packages them into membrane-bound vesicles. The Golgi apparatus operates at the intersection of the secretory, lysosomal, and endocytic pathways. [ISBN:0198506732] |
azurophil granule lumen | cellular component | The volume enclosed by the membrane of an azurophil granule, a primary lysosomal granule found in neutrophil granulocytes that contains a wide range of hydrolytic enzymes and is released into the extracellular fluid. [GOC:bf, PMID:17152095] |
intracellular membrane-bounded organelle | cellular component | Organized structure of distinctive morphology and function, bounded by a single or double lipid bilayer membrane and occurring within the cell. Includes the nucleus, mitochondria, plastids, vacuoles, and vesicles. Excludes the plasma membrane. [GOC:go_curators] |
extracellular exosome | cellular component | A vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894] |
vesicle | cellular component | Any small, fluid-filled, spherical organelle enclosed by membrane. [GOC:mah, GOC:pz, GOC:vesicles] |
Active In
This protein is active in 1 target(s):
Target | Category | Definition |
vesicle | cellular component | Any small, fluid-filled, spherical organelle enclosed by membrane. [GOC:mah, GOC:pz, GOC:vesicles] |
Involved In
This protein is involved in 2 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] |
lysosomal protein catabolic process | biological process | Any cellular protein catabolic process that takes place in a lysosome. [GO_REF:0000062, GOC:bf, GOC:PARL, GOC:TermGenie, PMID:24334770] |