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3-Oxo-hexahydro-1H-isoindole-4-carboxylic Acid as a Drug Chiral Bicyclic Scaffold: Structure-Based Design and Preparation of Conformationally Constrained Covalent and Noncovalent Prolyl Oligopeptidase Inhibitors.

Mcgill University

Inhibition of Human Prolyl Oligopeptidase Activity by the Cyclotide Psysol 2 Isolated from Psychotria solitudinum.

Medical University of Vienna

Structural revision of kynapcin-12 by total synthesis, and inhibitory activities against prolyl oligopeptidase and cancer cells.

Riken

Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP).

University of Antwerp

Synthesis and biological evaluation of novel (123)I-labeled 4-(4-iodophenyl)butanoyl-L-prolyl-(2S)-pyrrolidines for imaging prolyl oligopeptidase in vivo.

University of Helsinki

Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.

Merck

Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold.

University of Antwerp (Ua)

Identification of selective and potent inhibitors of fibroblast activation protein and prolyl oligopeptidase.

Tufts University Sackler School of Biomedical Sciences

P2-substituted N-acylprolylpyrrolidine inhibitors of prolyl oligopeptidase: biochemical evaluation, binding mode determination, and assessment in a cellular model of synucleinopathy.

University of Antwerp

Virtual screening and computational optimization for the discovery of covalent prolyl oligopeptidase inhibitors with activity in human cells.

Mcgill University

Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity.

University of Antwerp (Ua)

Inhibition of prolyl oligopeptidase with a synthetic unnatural dipeptide.

The University of Warwick

Inhibitors of prolyl oligopeptidases for the therapy of human diseases: defining diseases and inhibitors.

Mcgill University

Bioactive constituents from Boswellia papyrifera.

University of Karachi

Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.

Johnson & Johnson Pharmaceutical Research & Development

Synthesis, biological evaluation and structural determination of beta-aminoacyl-containing cyclic hydrazine derivatives as dipeptidyl peptidase IV (DPP-IV) inhibitors.

Korea Research Institute of Chemical Technology

Dicarboxylic acid azacycle l-prolyl-pyrrolidine amides as prolyl oligopeptidase inhibitors and three-dimensional quantitative structure-activity relationship of the enzyme-inhibitor interactions.

University of Kuopio

Quantized surface complementarity diversity (QSCD): a model based on small molecule-target complementarity.

Neogenesis

Structure-activity relationships of boronic acid inhibitors of dipeptidyl peptidase IV. 1. Variation of the P2 position of Xaa-boroPro dipeptides.

Boehringer Ingelheim Pharmaceuticals

New potent prolyl endopeptidase inhibitors: synthesis and structure-activity relationships of indan and tetralin derivatives and their analogues.

Zeria Pharmaceutical

 

Peptidyl -keto thiazole as potent thrombin inhibitors

TBA

2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5-yl}methyl)-4-fluorobenzonitrile (DSR-12727): a potent, orally active dipeptidyl peptidase IV inhibitor without mechanism-based inactivation of CYP3A.

Dainippon Sumitomo Pharma

1-((3S,4S)-4-amino-1-(4-substituted-1,3,5-triazin-2-yl) pyrrolidin-3-yl)-5,5-difluoropiperidin-2-one inhibitors of DPP-4 for the treatment of type 2 diabetes.

Pfizer

Discovery ofß-aminoacyl containing thiazolidine derivatives as potent and selective dipeptidyl peptidase IV inhibitors.

Korea Research Institute of Chemical Technology

Constrained peptidomimetics reveal detailed geometric requirements of covalent prolyl oligopeptidase inhibitors.

Mcgill University

Novel N-substituted 4-hydrazino piperidine derivative as a dipeptidyl peptidase IV inhibitor.

Torrent Pharmaceuticals

The design of potent and selective inhibitors of DPP-4: optimization of ADME properties by amide replacements.

Santhera Pharmaceuticals (Switzerland)

 

Prolyl endopeptidase inhibitors¹: N-acyl derivatives of L-thioproline-pyrrolidine

TBA

 

Synthesis of peptidyl acetals as inhibitors of prolyl endopeptidase

TBA

 

α-Ketothiazole inhibitors of prolyl endopeptidase

TBA

 

Novel in vitro and in vivo inhibitors of prolyl endopeptidase

TBA

(3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor.

Pfizer

Prolyl oligopeptidase inhibition by N-acyl-pro-pyrrolidine-type molecules.

Chinoin

Baicalin, a prodrug able to reach the CNS, is a prolyl oligopeptidase inhibitor.

Institut De Recerca BiomèDica De Barcelona

Discovery of conformationally rigid 3-azabicyclo[3.1.0]hexane-derived dipeptidyl peptidase-IV inhibitors.

Ranbaxy Research Laboratories

New bioactive diterpene polyesters from Euphorbia decipiens.

University of Karachi

Synthesis and structure-activity relationship of N-acyl-Gly-, N-acyl-Sar- and N-blocked-boroPro inhibitors of FAP, DPP4, and POP.

Genentech

Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor.

Tufts University School of Medicine

Synthesis and characterization of the novel fluorescent prolyl oligopeptidase inhibitor 4-fluoresceinthiocarbamoyl-6-aminocaproyl-L-prolyl-2(S)-(hydroxyacetyl)pyrrolidine.

University of Kuopio

A cyclopent-2-enecarbonyl group mimics proline at the P2 position of prolyl oligopeptidase inhibitors.

University of Kuopio

Potent and selective proline derived dipeptidyl peptidase IV inhibitors.

Merck

Diastereoselective synthesis and configuration-dependent activity of (3-substituted-cycloalkyl)glycine pyrrolidides and thiazolidides as dipeptidyl peptidase IV inhibitors.

Merck Research Laboratories

2-Imidazole as a Substitute for the Electrophilic Group Gives Highly Potent Prolyl Oligopeptidase Inhibitors.

University of Helsinki

Prolylisoxazoles: potent inhibitors of prolyloligopeptidase with antitrypanosomal activity.

University of Antwerp

New prolyl oligopeptidase inhibitors developed from dicarboxylic acid bis(l-prolyl-pyrrolidine) amides.

University of Kuopio

Dicarboxylic acid bis(L-prolyl-pyrrolidine) amides as prolyl oligopeptidase inhibitors.

University of Kuopio

Identification of BR102910 as a selective fibroblast activation protein (FAP) inhibitor.

Sungkyunkwan University

Discovery of novel berberine derivatives with balanced cholinesterase and prolyl oligopeptidase inhibition profile.

University of Defense

Discovery of a Beetroot Protease Inhibitor to Identify and Classify Plant-Derived Cystine Knot Peptides.

Medical University of Vienna

Tetrazole as a Replacement of the Electrophilic Group in Characteristic Prolyl Oligopeptidase Inhibitors.

University of Helsinki

Automated parallel synthesis of a tetrahydroisoquinolin-based library: potential prolyl endopeptidase inhibitors.

Université

Structure-activity relationship of diaryl phosphonate esters as potent irreversible dipeptidyl peptidase IV inhibitors.

University of Antwerp (Uia)

Integrated Synthetic, Biophysical, and Computational Investigations of Covalent Inhibitors of Prolyl Oligopeptidase and Fibroblast Activation Protein ?.

Mcgill University

Isoquinoline Alkaloids from Berberis vulgaris as Potential Lead Compounds for the Treatment of Alzheimer's Disease.

Charles University

Dual inhibition of human leukocyte elastase and lipid peroxidation: in vitro and in vivo activities of azabicyclo[2.2.2]octane and perhydroindole derivatives.

Institut De Recherche Servier

Discovery of covalent prolyl oligopeptidase boronic ester inhibitors.

Mcgill University

New prolyl endopeptidase inhibitors: in vitro and in vivo activities of azabicyclo[2.2.2]octane, azabicyclo[2.2.1]heptane, and perhydroindole derivatives.

Institut De Recherche Servier

Synthesis and structure-activity relationships of peptidyl alpha-keto heterocycles as novel inhibitors of prolyl endopeptidase.

Meiji Seika Kaisha

Pyrrolidinyl pyridone and pyrazinone analogues as potent inhibitors of prolyl oligopeptidase (POP).

Glaxosmithkline

Synthesis of polyozellin, a prolyl oligopeptidase inhibitor, and its structural revision.

Riken Csrs

Approaches towards the development of chimeric DPP4/ACE inhibitors for treating metabolic syndrome.

Ranbaxy Laboratories

Evaluation of the activities of pyrimethamine analogs against Plasmodium vivax and Plasmodium falciparum dihydrofolate reductase-thymidylate synthase using in vitro enzyme inhibition and bacterial complementation assays.

National Center For Genetic Engineering and Biotechnology At Thailand