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Dipeptidyl peptidase 4
A dipeptidyl peptidase 4 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P27487]
Synonyms
EC 3.4.14.5;
ADABP;
Adenosine deaminase complexing protein 2;
ADCP-2;
Dipeptidyl peptidase IV;
DPP IV;
T-cell activation antigen CD26;
TP103
Research
Bioassay Publications (131)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 5 (3.82) | 18.2507 |
| 2000's | 49 (37.40) | 29.6817 |
| 2010's | 63 (48.09) | 24.3611 |
| 2020's | 14 (10.69) | 2.80 |
Compounds (71)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| gallic acid | Homo sapiens (human) | IC50 | 4.6500 | 1 | 1 |
| metformin | Homo sapiens (human) | IC50 | 29.0000 | 1 | 1 |
| pyrimethamine | Homo sapiens (human) | IC50 | 0.3900 | 1 | 1 |
| trimethoprim | Homo sapiens (human) | IC50 | 2.7000 | 3 | 3 |
| trimetrexate | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
| wb 4101 | Homo sapiens (human) | IC50 | 700.0000 | 1 | 1 |
| flavone | Homo sapiens (human) | IC50 | 0.1700 | 1 | 1 |
| vidarabine | Homo sapiens (human) | IC50 | 0.0620 | 1 | 1 |
| piritrexim | Homo sapiens (human) | IC50 | 0.0140 | 2 | 2 |
| baicalin | Homo sapiens (human) | IC50 | 225.0000 | 1 | 1 |
| epigallocatechin gallate | Homo sapiens (human) | IC50 | 10.2100 | 1 | 1 |
| epiroprim | Homo sapiens (human) | IC50 | 0.4800 | 1 | 1 |
| malvidin chloride | Homo sapiens (human) | IC50 | 1.4100 | 1 | 1 |
| ubenimex | Homo sapiens (human) | IC50 | 324.3000 | 1 | 1 |
| hesperetin | Homo sapiens (human) | IC50 | 0.2800 | 1 | 1 |
| sori 8895 | Homo sapiens (human) | IC50 | 0.0160 | 1 | 1 |
| 2,6-dimethylphenylphthalimide | Homo sapiens (human) | IC50 | 398.0000 | 1 | 1 |
| eriocitrin | Homo sapiens (human) | IC50 | 10.3600 | 1 | 1 |
| dehydropregnenolone acetate | Homo sapiens (human) | IC50 | 35.6000 | 1 | 1 |
| diprotin a | Homo sapiens (human) | IC50 | 3.6050 | 2 | 2 |
| diprotin a | Homo sapiens (human) | Ki | 2.2000 | 2 | 2 |
| territrem b | Homo sapiens (human) | IC50 | 0.0076 | 1 | 1 |
| 4-amino-n-(2,6-dimethylphenyl)phthalimide | Homo sapiens (human) | IC50 | 87.9000 | 1 | 1 |
| territrem c | Homo sapiens (human) | IC50 | 0.0068 | 1 | 1 |
| n-valyltryptophan | Homo sapiens (human) | IC50 | 65.6900 | 1 | 1 |
| jtp 4819 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| 1-(1-phenylcyclopentyl)methylamine | Homo sapiens (human) | IC50 | 34.3333 | 4 | 6 |
| naringenin | Homo sapiens (human) | IC50 | 0.2400 | 1 | 1 |
| cyanidin 3-o-beta-d-glucopyranoside | Homo sapiens (human) | IC50 | 0.4200 | 1 | 1 |
| resveratrol | Homo sapiens (human) | IC50 | 0.0006 | 1 | 1 |
| valine-pyrrolidide | Homo sapiens (human) | IC50 | 4.3000 | 5 | 6 |
| valine-pyrrolidide | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
| caffeic acid | Homo sapiens (human) | IC50 | 3.3700 | 1 | 1 |
| 2-(2,6-diisopropylphenyl)-5-amino-1h-isoindole-1,3-dione | Homo sapiens (human) | IC50 | 251.2000 | 1 | 1 |
| meso-1,2-diphenylethylenediamine, (r-(r*,s*))-isomer | Homo sapiens (human) | IC50 | 45.0000 | 1 | 1 |
| sitagliptin | Homo sapiens (human) | IC50 | 6.6016 | 56 | 62 |
| quercetin | Homo sapiens (human) | IC50 | 66.4600 | 2 | 2 |
| apigenin | Homo sapiens (human) | IC50 | 0.1400 | 1 | 1 |
| luteolin | Homo sapiens (human) | IC50 | 0.1200 | 1 | 1 |
| rutin | Homo sapiens (human) | IC50 | 145.0000 | 1 | 1 |
| kaempferol | Homo sapiens (human) | IC50 | 66.2450 | 2 | 2 |
| genistein | Homo sapiens (human) | IC50 | 0.4800 | 1 | 1 |
| baicalein | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| 3,7-dihydroxyflavone | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| enalaprilat anhydrous | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| manzamine a | Homo sapiens (human) | IC50 | 10.2000 | 1 | 1 |
| vildagliptin | Homo sapiens (human) | IC50 | 8.5618 | 34 | 42 |
| vildagliptin | Homo sapiens (human) | Ki | 3.6836 | 3 | 5 |
| talabostat | Homo sapiens (human) | IC50 | 0.1666 | 11 | 11 |
| talabostat | Homo sapiens (human) | Ki | 0.2866 | 6 | 7 |
| meso-1,2-diphenylethylenediamine | Homo sapiens (human) | IC50 | 75.0000 | 1 | 1 |
| sulphostin | Homo sapiens (human) | IC50 | 0.0210 | 1 | 1 |
| nvp-dpp728 | Homo sapiens (human) | IC50 | 3.4785 | 14 | 18 |
| nvp-dpp728 | Homo sapiens (human) | Ki | 0.0217 | 3 | 3 |
| pp-33 | Homo sapiens (human) | IC50 | 325.3000 | 1 | 1 |
| linagliptin | Homo sapiens (human) | IC50 | 0.0008 | 12 | 12 |
| alanylpyrrolidine-boronic acid | Homo sapiens (human) | IC50 | 0.5028 | 6 | 6 |
| alanylpyrrolidine-boronic acid | Homo sapiens (human) | Ki | 0.0008 | 3 | 3 |
| arisugacin | Homo sapiens (human) | IC50 | 0.0010 | 1 | 1 |
| kyp 2047 | Homo sapiens (human) | IC50 | 0.1000 | 1 | 1 |
| uamc00039 | Homo sapiens (human) | IC50 | 171.2000 | 5 | 5 |
| uamc00039 | Homo sapiens (human) | Ki | 0.0001 | 1 | 1 |
| bms 477118 | Homo sapiens (human) | IC50 | 0.0198 | 7 | 7 |
| bms 477118 | Homo sapiens (human) | Ki | 0.0006 | 6 | 6 |
| dutogliptin | Homo sapiens (human) | IC50 | 0.0250 | 1 | 1 |
| alogliptin | Homo sapiens (human) | IC50 | 5.2694 | 18 | 19 |
| gosogliptin | Homo sapiens (human) | IC50 | 1.6564 | 2 | 2 |
| 2-(2,6-diisopropylphenyl)-5-hydroxy-1h-isoindole-1,3-dione | Homo sapiens (human) | IC50 | 65.9000 | 1 | 1 |
| trelagliptin | Homo sapiens (human) | IC50 | 0.0022 | 3 | 3 |
| trelagliptin | Homo sapiens (human) | Ki | 0.0051 | 1 | 1 |
| grassystatin a | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| anagliptin | Homo sapiens (human) | IC50 | 0.0033 | 1 | 1 |
| mk-3102 | Homo sapiens (human) | IC50 | 0.0024 | 4 | 4 |
| mk-3102 | Homo sapiens (human) | Ki | 0.0008 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
2,4-Diamino-6,7-dihydro-5H-cyclopenta[d]pyrimidine analogues of trimethoprim as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.Journal of medicinal chemistry, , Mar-12, Volume: 41, Issue:6, 1998
Synthesis and biological evaluation of nonclassical 2,4-diamino-5-methylpyrido[2,3-d]pyrimidines with novel side chain substituents as potential inhibitors of dihydrofolate reductases.Journal of medicinal chemistry, , Feb-14, Volume: 40, Issue:4, 1997
2,4-Diamino-5-chloroquinazoline analogues of trimetrexate and piritrexim: synthesis and antifolate activity.Journal of medicinal chemistry, , Dec-23, Volume: 37, Issue:26, 1994
Synthesis and biological evaluation of nonclassical 2,4-diamino-5-methylpyrido[2,3-d]pyrimidines with novel side chain substituents as potential inhibitors of dihydrofolate reductases.Journal of medicinal chemistry, , Feb-14, Volume: 40, Issue:4, 1997
2,4-Diamino-5-chloroquinazoline analogues of trimetrexate and piritrexim: synthesis and antifolate activity.Journal of medicinal chemistry, , Dec-23, Volume: 37, Issue:26, 1994
Recent progress of the development of dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus.European journal of medicinal chemistry, , May-10, Volume: 151, 2018
Kinetic studies of novel inhibitors of endomorphin degrading enzymes.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 21, Issue:7, 2012
Design, Synthesis, and in Vitro Evaluation of Novel Aminomethyl-pyridines as DPP-4 Inhibitors.ACS medicinal chemistry letters, , Dec-09, Volume: 1, Issue:9, 2010
Recent developments in fragment-based drug discovery.Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
In silico fragment-based discovery of DPP-IV S1 pocket binders.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 16, Issue:5, 2006
The reversed binding of beta-phenethylamine inhibitors of DPP-IV: X-ray structures and properties of novel fragment and elaborated inhibitors.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 16, Issue:6, 2006
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
Recent developments in fragment-based drug discovery.Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
In silico fragment-based discovery of DPP-IV S1 pocket binders.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 16, Issue:5, 2006
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
Discovery of a Potent and Highly Selective Dipeptidyl Peptidase IV and Carbonic Anhydrase Inhibitor as "Antidiabesity" Agents Based on Repurposing and Morphing of WB-4101.Journal of medicinal chemistry, , 10-27, Volume: 65, Issue:20, 2022
Synthesis, in vitro evaluation, and computational simulations studies of 1,2,3-triazole analogues as DPP-4 inhibitors.Bioorganic & medicinal chemistry, , 01-01, Volume: 29, 2021
[no title available]European journal of medicinal chemistry, , Feb-15, Volume: 188, 2020
Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes.Journal of medicinal chemistry, , 03-14, Volume: 62, Issue:5, 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
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
Design, synthesis and biological evaluation of novel pyrimidinedione derivatives as DPP-4 inhibitors.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 28, Issue:12, 2018
Recent progress of the development of dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus.European journal of medicinal chemistry, , May-10, Volume: 151, 2018
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
Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure.Journal of medicinal chemistry, , Aug-25, Volume: 59, Issue:16, 2016
Discovery of novel xanthine compounds targeting DPP-IV and GPR119 as anti-diabetic agents.European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
Discovery and Rational Design of Natural-Product-Derived 2-Phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine Analogs as Novel and Potent Dipeptidyl Peptidase 4 (DPP-4) Inhibitors for the Treatment of Type 2 Diabetes.Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Novel 4-heteroaryl-antipyrines as DPP-IV inhibitors.Chemical biology & drug design, , Volume: 86, Issue:5, 2015
Synthesis and potent inhibitory activities of carboxybenzyl-substituted 8-(3-(R)-aminopiperidin-1-yl)-7-(2-chloro/cyanobenzyl)-3-methyl-3,7-dihydro-purine-2,6-diones as dipeptidyl peptidase IV (DPP-IV) inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 25, Issue:9, 2015
Synthesis of New DPP-4 Inhibitors Based on a Novel Tricyclic Scaffold.ACS medicinal chemistry letters, , Mar-12, Volume: 6, Issue:3, 2015
Applications of Fluorine in Medicinal Chemistry.Journal of medicinal chemistry, , Nov-12, Volume: 58, Issue:21, 2015
Design, synthesis and biological evaluation of novel pyrazolo-pyrimidinones as DPP-IV inhibitors in diabetes.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 25, Issue:20, 2015
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, biological screening, and molecular docking studies of piperazine-derived constrained inhibitors of DPP-IV for the treatment of type 2 diabetes.Chemical biology & drug design, , Volume: 85, Issue:4, 2015
Structure based virtual screening of MDPI database: discovery of structurally diverse and novel DPP-IV inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 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
Dipeptidyl peptidase IV and its inhibitors: therapeutics for type 2 diabetes and what else?Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
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
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 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
Design, synthesis and biological evaluation of novel aminomethyl-piperidones based DPP-IV inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 24, Issue:8, 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
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
Identification of dipeptidyl peptidase IV inhibitors: virtual screening, synthesis and biological evaluation.Chemical biology & drug design, , Volume: 84, Issue:3, 2014
Synthetic approaches to the 2011 new drugs.Bioorganic & medicinal chemistry, , Jun-01, Volume: 21, Issue:11, 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
Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity.Bioorganic & medicinal chemistry letters, , May-15, Volume: 22, Issue:10, 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
Discovery of β-aminoacyl containing thiazolidine derivatives as potent and selective dipeptidyl peptidase IV inhibitors.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 21, Issue:5, 2011
Discovery of potent dipeptidyl peptidase IV inhibitors derived from β-aminoamides bearing substituted [1,2,3]-triazolopiperidines for the treatment of type 2 diabetes.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
Synthesis and evaluation of structurally constrained imidazolidin derivatives as potent dipeptidyl peptidase IV inhibitors.European journal of medicinal chemistry, , Volume: 44, Issue:8, 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
Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 2009
The many roles for fluorine in medicinal chemistry.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
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 biological evaluation of pyrazoline analogues with beta-amino acyl group as dipeptidyl peptidase IV inhibitors.European journal of medicinal chemistry, , Volume: 43, Issue:9, 2008
A three-dimensional pharmacophore model for dipeptidyl peptidase IV inhibitors.European journal of medicinal chemistry, , Volume: 43, Issue:8, 2008
Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: close analogs of JANUVIA (sitagliptin phosphate).Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 17, Issue:12, 2007
(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
Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 17, Issue:21, 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
Recent progress of the development of dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus.European journal of medicinal chemistry, , May-10, Volume: 151, 2018
Baicalin, a prodrug able to reach the CNS, is a prolyl oligopeptidase inhibitor.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Recent progress of the development of dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes mellitus.European journal of medicinal chemistry, , May-10, Volume: 151, 2018
Baicalin, a prodrug able to reach the CNS, is a prolyl oligopeptidase inhibitor.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Proline based rationally designed peptide esters against dipeptidyl peptidase-4: Highly potent anti-diabetic agents.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 76, 2022
Modulating the selectivity of inhibitors for prolyl oligopeptidase inhibitors and fibroblast activation protein-α for different indications.European journal of medicinal chemistry, , Oct-05, Volume: 240, 2022
Anti-diabetic drugs recent approaches and advancements.Bioorganic & medicinal chemistry, , 03-01, Volume: 28, Issue:5, 2020
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
Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure.Journal of medicinal chemistry, , Aug-25, Volume: 59, Issue:16, 2016
Dipeptidyl peptidase IV and its inhibitors: therapeutics for type 2 diabetes and what else?Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 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
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
Synthetic approaches to the 2011 new drugs.Bioorganic & medicinal chemistry, , Jun-01, Volume: 21, Issue:11, 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
Long-acting peptidomimetics based DPP-IV inhibitors.Bioorganic & medicinal chemistry letters, , May-15, Volume: 22, Issue:10, 2012
Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity.Bioorganic & medicinal chemistry letters, , May-15, Volume: 22, Issue:10, 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
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
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
(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
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
Synthesis and evaluation of structurally constrained imidazolidin derivatives as potent dipeptidyl peptidase IV inhibitors.European journal of medicinal chemistry, , Volume: 44, Issue:8, 2009
Bicyclic cyanothiazolidines as novel dipeptidyl peptidase 4 inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 19, Issue:15, 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
Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 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
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
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
4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors.Bioorganic & medicinal chemistry letters, , Jan-05, Volume: 14, Issue:1, 2004
Dipeptidyl peptidase IV inhibitors for the treatment of diabetes.Journal of medicinal chemistry, , Aug-12, Volume: 47, Issue:17, 2004
Modulating the selectivity of inhibitors for prolyl oligopeptidase inhibitors and fibroblast activation protein-α for different indications.European journal of medicinal chemistry, , Oct-05, Volume: 240, 2022
Boron-Containing heterocycles as promising pharmacological agents.Bioorganic & medicinal chemistry, , 06-01, Volume: 63, 2022
Identification of BR102910 as a selective fibroblast activation protein (FAP) inhibitor.Bioorganic & medicinal chemistry letters, , 04-01, Volume: 37, 2021
Integrated Synthetic, Biophysical, and Computational Investigations of Covalent Inhibitors of Prolyl Oligopeptidase and Fibroblast Activation Protein α.Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase.Journal of medicinal chemistry, , May-09, Volume: 56, Issue:9, 2013
Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity.Bioorganic & medicinal chemistry letters, , May-15, Volume: 22, Issue:10, 2012
Pro-soft Val-boroPro: a strategy for enhancing in vivo performance of boronic acid inhibitors of serine proteases.Journal of medicinal chemistry, , Apr-14, Volume: 54, Issue:7, 2011
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 characterization of constrained peptidomimetic dipeptidyl peptidase IV inhibitors: amino-lactam boroalanines.Journal of medicinal chemistry, , May-17, Volume: 50, Issue:10, 2007
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
Dipeptidyl peptidase IV and its inhibitors: therapeutics for type 2 diabetes and what else?Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
Long-acting peptidomimetics based DPP-IV inhibitors.Bioorganic & medicinal chemistry letters, , May-15, Volume: 22, Issue:10, 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
A three-dimensional pharmacophore model for dipeptidyl peptidase IV inhibitors.European journal of medicinal chemistry, , Volume: 43, Issue:8, 2008
Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 16, Issue:1, 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
1-((S)-gamma-substituted prolyl)-(S)-2-cyanopyrrolidine as a novel series of highly potent DPP-IV inhibitors.Bioorganic & medicinal chemistry letters, , May-16, Volume: 15, Issue:10, 2005
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
Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents.Bioorganic & medicinal chemistry letters, , Mar-22, Volume: 14, Issue:6, 2004
4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors.Bioorganic & medicinal chemistry letters, , Jan-05, Volume: 14, Issue:1, 2004
Dipeptidyl peptidase IV inhibitors for the treatment of diabetes.Journal of medicinal chemistry, , Aug-12, Volume: 47, Issue:17, 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
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
Proline based rationally designed peptide esters against dipeptidyl peptidase-4: Highly potent anti-diabetic agents.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 76, 2022
Therapeutic progression of quinazolines as targeted chemotherapeutic agents.European journal of medicinal chemistry, , Feb-05, Volume: 211, 2021
Synthesis and discovery of triazolo-pyridazine-6-yl-substituted piperazines as effective anti-diabetic drugs; evaluated over dipeptidyl peptidase-4 inhibition mechanism and insulinotropic activities.European journal of medicinal chemistry, , Feb-01, Volume: 187, 2020
Design and synthesis of quinazoline-3,4-(4H)-diamine endowed with thiazoline moiety as new class for DPP-4 and DPPH inhibitor.Bioorganic chemistry, , Volume: 71, 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
Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure.Journal of medicinal chemistry, , Aug-25, Volume: 59, Issue:16, 2016
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
Design, Synthesis and Biological Evaluation of Imidazo[1,2-a]pyridine Derivatives as Novel DPP-4 Inhibitors.Chemical biology & drug design, , Volume: 86, Issue:4, 2015
Synthetic approaches to the 2011 new drugs.Bioorganic & medicinal chemistry, , Jun-01, Volume: 21, Issue:11, 2013
Novel heterocyclic DPP-4 inhibitors for the treatment of type 2 diabetes.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 22, Issue:3, 2012
3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: a class of potent DPP-4 inhibitors.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 18, Issue:11, 2008
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.Journal of medicinal chemistry, , Dec-27, Volume: 50, Issue:26, 2007
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
Pro-soft Val-boroPro: a strategy for enhancing in vivo performance of boronic acid inhibitors of serine proteases.Journal of medicinal chemistry, , Apr-14, Volume: 54, Issue:7, 2011
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
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 characterization of constrained peptidomimetic dipeptidyl peptidase IV inhibitors: amino-lactam boroalanines.Journal of medicinal chemistry, , May-17, Volume: 50, Issue:10, 2007
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
Proline based rationally designed peptide esters against dipeptidyl peptidase-4: Highly potent anti-diabetic agents.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 76, 2022
Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure.Journal of medicinal chemistry, , Aug-25, Volume: 59, Issue:16, 2016
Dipeptidyl peptidase IV and its inhibitors: therapeutics for type 2 diabetes and what else?Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
Synthesis and biological evaluation of all eight stereoisomers of DPP-IV inhibitor saxagliptin.Bioorganic & medicinal chemistry, , Feb-15, Volume: 22, Issue:4, 2014
Synthetic approaches to the 2011 new drugs.Bioorganic & medicinal chemistry, , Jun-01, Volume: 21, Issue:11, 2013
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
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
Synthesis and evaluation of structurally constrained imidazolidin derivatives as potent dipeptidyl peptidase IV inhibitors.European journal of medicinal chemistry, , Volume: 44, Issue:8, 2009
Bicyclic cyanothiazolidines as novel dipeptidyl peptidase 4 inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 19, Issue:15, 2009
Potent non-nitrile dipeptidic dipeptidyl peptidase IV inhibitors.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 17, Issue:23, 2007
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
Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.Journal of medicinal chemistry, , Jul-28, Volume: 48, Issue:15, 2005
Proline based rationally designed peptide esters against dipeptidyl peptidase-4: Highly potent anti-diabetic agents.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 76, 2022
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
Surrogating and redirection of pyrazolo[1,5-a]pyrimidin-7(4H)-one core, a novel class of potent and selective DPP-4 inhibitors.Bioorganic & medicinal chemistry, , 02-15, Volume: 26, Issue:4, 2018
Synthetic Approaches to the New Drugs Approved During 2015.Journal of medicinal chemistry, , 08-10, Volume: 60, Issue:15, 2017
Comparative Analysis of Binding Kinetics and Thermodynamics of Dipeptidyl Peptidase-4 Inhibitors and Their Relationship to Structure.Journal of medicinal chemistry, , Aug-25, Volume: 59, Issue:16, 2016
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
Design, Synthesis and Biological Evaluation of Imidazo[1,2-a]pyridine Derivatives as Novel DPP-4 Inhibitors.Chemical biology & drug design, , Volume: 86, Issue:4, 2015
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
Synthetic approaches to the 2011 new drugs.Bioorganic & medicinal chemistry, , Jun-01, Volume: 21, Issue:11, 2013
Highly potent dipeptidyl peptidase IV inhibitors derived from Alogliptin through pharmacophore hybridization and lead optimization.European journal of medicinal chemistry, , Volume: 68, 2013
Novel pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors based on pharmacokinetic property-driven optimization.European journal of medicinal chemistry, , Volume: 52, 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
Synthesis and evaluation of structurally constrained imidazolidin derivatives as potent dipeptidyl peptidase IV inhibitors.European journal of medicinal chemistry, , Volume: 44, Issue:8, 2009
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
Synthetic Approaches to the New Drugs Approved During 2015.Journal of medicinal chemistry, , 08-10, Volume: 60, Issue:15, 2017
Rapid generation of a novel DPP-4 inhibitor with long-acting properties: SAR study and PK/PD evaluation.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV.Journal of medicinal chemistry, , Jan-27, Volume: 54, Issue:2, 2011
Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes.Journal of medicinal chemistry, , 07-09, Volume: 63, Issue:13, 2020
Discovery of a Natural-Product-Derived Preclinical Candidate for Once-Weekly Treatment of Type 2 Diabetes.Journal of medicinal chemistry, , 03-14, Volume: 62, Issue:5, 2019
Discovery and Rational Design of Natural-Product-Derived 2-Phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine Analogs as Novel and Potent Dipeptidyl Peptidase 4 (DPP-4) Inhibitors for the Treatment of Type 2 Diabetes.Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
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 11 target(s):
| Target | Category | Definition |
|---|
| virus receptor activity | molecular function | Combining with a virus component and mediating entry of the virus into the cell. [GOC:bf, GOC:dph, PMID:7621403, UniProtKB-KW:KW-1183] |
| protease binding | molecular function | Binding to a protease or a peptidase. [GOC:hjd] |
| 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 endopeptidase activity | molecular function | Catalysis of the hydrolysis of internal, alpha-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). [GOC:mah, https://www.ebi.ac.uk/merops/about/glossary.shtml#CATTYPE] |
| signaling receptor binding | molecular function | Binding to one or more specific sites on a receptor molecule, a macromolecule that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:bf, GOC:ceb, ISBN:0198506732] |
| 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] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| protein homodimerization activity | molecular function | Binding to an identical protein to form a homodimer. [GOC:jl] |
| chemorepellent activity | molecular function | Providing the environmental signal that initiates the directed movement of a motile cell or organism towards a lower concentration of that signal. [GOC:ai] |
Located In
This protein is located in 13 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] |
| lysosomal membrane | cellular component | The lipid bilayer surrounding the lysosome and separating its contents from the cell cytoplasm. [GOC:ai] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| focal adhesion | cellular component | A cell-substrate junction that anchors the cell to the extracellular matrix and that forms a point of termination of actin filaments. In insects focal adhesion has also been referred to as hemi-adherens junction (HAJ). [GOC:aruk, GOC:bc, ISBN:0124325653, ISBN:0815316208, PMID:10419689, PMID:12191915, PMID:15246682, PMID:1643657, PMID:16805308, PMID:19197329, PMID:23033047, PMID:26923917, PMID:28796323, PMID:8314002] |
| cell surface | cellular component | The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| apical plasma membrane | cellular component | The region of the plasma membrane located at the apical end of the cell. [GOC:curators] |
| lamellipodium | cellular component | A thin sheetlike process extended by the leading edge of a migrating cell or extending cell process; contains a dense meshwork of actin filaments. [ISBN:0815316194] |
| endocytic vesicle | cellular component | A membrane-bounded intracellular vesicle formed by invagination of the plasma membrane around an extracellular substance. Endocytic vesicles fuse with early endosomes to deliver the cargo for further sorting. [GOC:go_curators, PMID:19696797] |
| lamellipodium membrane | cellular component | The portion of the plasma membrane surrounding a lamellipodium. [GOC:mah] |
| membrane raft | cellular component | Any of the small (10-200 nm), heterogeneous, highly dynamic, sterol- and sphingolipid-enriched membrane domains that compartmentalize cellular processes. Small rafts can sometimes be stabilized to form larger platforms through protein-protein and protein-lipid interactions. [PMID:16645198, PMID:20044567] |
| intercellular canaliculus | cellular component | An extremely narrow tubular channel located between adjacent cells. An instance of this is the secretory canaliculi occurring between adjacent parietal cells in the gastric mucosa of vertebrates. [ISBN:0721662544] |
| 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] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Involved In
This protein is involved in 20 target(s):
| Target | Category | Definition |
|---|
| behavioral fear response | biological process | An acute behavioral change resulting from a perceived external threat. [GOC:dph, PMID:9920659] |
| response to hypoxia | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating lowered oxygen tension. Hypoxia, defined as a decline in O2 levels below normoxic levels of 20.8 - 20.95%, results in metabolic adaptation at both the cellular and organismal level. [GOC:hjd] |
| proteolysis | biological process | The hydrolysis of proteins into smaller polypeptides and/or amino acids by cleavage of their peptide bonds. [GOC:bf, GOC:mah] |
| cell adhesion | biological process | The attachment of a cell, either to another cell or to an underlying substrate such as the extracellular matrix, via cell adhesion molecules. [GOC:hb, GOC:pf] |
| positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
| negative regulation of extracellular matrix disassembly | biological process | Any process that decreases the rate, frequency or extent of extracellular matrix disassembly. Extracellular matrix disassembly is a process that results in the breakdown of the extracellular matrix. [GOC:BHF, GOC:dph, GOC:tb] |
| peptide hormone processing | biological process | The generation of a mature peptide hormone by posttranslational processing of a prohormone. [GOC:mah] |
| receptor-mediated endocytosis of virus by host cell | biological process | Any receptor-mediated endocytosis that is involved in the uptake of a virus into a host cell; successive instances of virus endocytosis result in the accumulation of virus particles within the cell. [GOC:bf, GOC:jl, ISBN:0781702534] |
| T cell costimulation | biological process | The process of providing, via surface-bound receptor-ligand pairs, a second, antigen-independent, signal in addition to that provided by the T cell receptor to augment T cell activation. [ISBN:0781735149] |
| regulation of cell-cell adhesion mediated by integrin | biological process | Any process that modulates the frequency, rate, or extent of cell-cell adhesion mediated by integrin. [GOC:add] |
| locomotory exploration behavior | biological process | The specific movement from place to place of an organism in response to a novel environment. [GOC:sart, PMID:17151232] |
| psychomotor behavior | biological process | The specific behavior of an organism that combines cognitive functions and physical movement. For example, driving a car, throwing a ball, or playing a musical instrument. [GOC:nhn, GOC:pr, PMID:17159989, Wikipedia:Psychomotor_learning] |
| T cell activation | biological process | The change in morphology and behavior of a mature or immature T cell resulting from exposure to a mitogen, cytokine, chemokine, cellular ligand, or an antigen for which it is specific. [GOC:mgi_curators, ISBN:0781735149] |
| endothelial cell migration | biological process | The orderly movement of an endothelial cell into the extracellular matrix to form an endothelium. [GOC:go_curators] |
| symbiont entry into host cell | biological process | The process by which a symbiont breaches the plasma membrane or cell envelope and enters the host cell. The process ends when the symbiont or its genome is released into the host cell. [GOC:jl] |
| receptor-mediated virion attachment to host cell | biological process | The process by which a virion attaches to a host cell by binding to a receptor on the host cell surface. [ISBN:0879694971] |
| negative chemotaxis | biological process | The directed movement of a motile cell or organism towards a lower concentration of a chemical. [GOC:ai, GOC:bf, GOC:isa_complete] |
| membrane fusion | biological process | The membrane organization process that joins two lipid bilayers to form a single membrane. [GOC:dph, GOC:tb] |
| negative regulation of neutrophil chemotaxis | biological process | Any process that decreases the frequency, rate, or extent of neutrophil chemotaxis. Neutrophil chemotaxis is the directed movement of a neutrophil cell, the most numerous polymorphonuclear leukocyte found in the blood, in response to an external stimulus, usually an infection or wounding. [GOC:dph, GOC:tb] |
| glucagon processing | biological process | The formation of mature glucagon by proteolysis of the precursor proglucagon. [PMID:28719828] |