K. Augustyns

发表

Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties.

J. Foekens, A. Lambeir, P. Van der Veken, 2007, Journal of medicinal chemistry.

The Effect of a Novel Serine Protease Inhibitor on Inflammation and Intestinal Permeability in a Murine Colitis Transfer Model

A. Lambeir, I. De Meester, M. Berg, 2021, Frontiers in Pharmacology.

Local Colonic Administration of a Serine Protease Inhibitor Improves Post-Inflammatory Visceral Hypersensitivity in Rats

I. De Meester, M. Berg, Tim Boogaerts, 2021, Pharmaceutics.

A novel serine protease inhibitor as potential treatment for dry eye syndrome and ocular inflammation

L. Moons, A. Lambeir, I. De Meester, 2020, Scientific Reports.

The effect of pharmacological inhibition of Serine Proteases on neuronal networks in vitro

M. Giugliano, S. Dedeurwaerdere, P. Van der Veken, 2019, PeerJ.

The Effect of Acute Pharmacological Inhibition of Urokinase Plasminogen Activator and Neuropsin Extracellular Proteases on Neuronal Networks in vitro

M. Giugliano, S. Dedeurwaerdere, P. Van der Veken, 2018, bioRxiv.

Newly developed serine protease inhibitors decrease visceral hypersensitivity in a post‐inflammatory rat model for irritable bowel syndrome

A. Lambeir, I. De Meester, J. Timmermans, 2018, British journal of pharmacology.

Decreased levels of active uPA and KLK8 assessed by [111In]MICA‐401 binding correlate with the seizure burden in an animal model of temporal lobe epilepsy

Lore M. Peeters, A. Pitkänen, S. Dedeurwaerdere, 2017, Epilepsia.

Preclinical evaluation of [111 In]MICA-401, an activity-based probe for SPECT imaging of in vivo uPA activity.

P. Pauwels, V. Magdolen, S. Stroobants, 2016, Contrast media & molecular imaging.

The first potent diphenyl phosphonate KLK4 inhibitors with unexpected binding kinetics

V. Magdolen, A. Lambeir, R. D. Santo, 2015 .

Discovery and SAR of Novel and Selective Inhibitors of Urokinase Plasminogen Activator (uPA) with an Imidazo[1,2-a]pyridine Scaffold.

A. Lambeir, P. Van der Veken, J. Joossens, 2015, Journal of medicinal chemistry.

Synthesis and in vivo preclinical evaluation of an (18)F labeled uPA inhibitor as a potential PET imaging agent.

S. Stroobants, S. Staelens, D. Thomae, 2014, Nuclear medicine and biology.

Synthesis and evaluation of non-basic inhibitors of urokinase-type plasminogen activator (uPA).

A. Lambeir, P. Van der Veken, J. Joossens, 2012, Bioorganic & medicinal chemistry.

Structure-based protein engineering efforts with a monomeric TIM variant: the importance of a single point mutation for generating an active site with suitable binding properties.

Peter Neubauer, Koen Augustyns, Markus Alahuhta, 2008, Protein engineering, design & selection : PEDS.

Crystal structure of Porphyromonas gingivalis dipeptidyl peptidase 4 and structure-activity relationships based on inhibitor profiling.

V. Fülöp, W. Luyten, A. Lambeir, 2017, European journal of medicinal chemistry.

Dipeptidyl peptidase IV inhibitors as new therapeutic agents for the treatment of Type 2 diabetes

P. Van der Veken, A. Haemers, K. Augustyns, 2003 .

Inhibitor screening and enzymatic activity determination for autophagy target Atg4B using a gel electrophoresis-based assay.

A. Lambeir, M. Grootaert, G. D. De Meyer, 2016, European journal of medicinal chemistry.

Preclinical Evaluation of a Novel 18F-Labeled dTCO-Amide Derivative for Bioorthogonal Pretargeted Positron Emission Tomography Imaging

S. Stroobants, S. Staelens, P. Van der Veken, 2020, ACS Omega.

Novel Small Molecule-Derived, Highly Selective Substrates for Fibroblast Activation Protein (FAP).

Ruth Geiss-Friedlander, A. Lambeir, I. De Meester, 2019, ACS medicinal chemistry letters.

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

A. Lambeir, I. De Meester, L. Maes, 2013, ACS medicinal chemistry letters.

DPP8/DPP9 inhibition elicits canonical Nlrp1b inflammasome hallmarks in murine macrophages

Ruth Geiss-Friedlander, A. Lambeir, I. De Meester, 2019, Life Science Alliance.

β-Fluorinated proline derivatives : potential transition state inhibitors for proline selective serine dipeptidases

A. Haemers, K. Augustyns, P. Veken, 2003 .

Synthesis and evaluation of azaproline peptides as potential inhibitors of dipeptidyl peptidase IV and prolyl oligopeptidase

A. Lambeir, A. Haemers, K. Augustyns, 1995, Letters in Peptide Science.

Development of potent and selective dipeptidyl peptidase II inhibitors.

A. Lambeir, B. Bauvois, I. De Meester, 2002, Bioorganic & Medicinal Chemistry Letters.

Incorporation of hexose nucleoside analogues into oligonucleotides: synthesis, base-pairing properties and enzymatic stability.

P. Herdewijn, R. Busson, C. Urbanke, 1992, Nucleic acids research.

Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs).

Christophe M. L. Vande Velde, J. Heeres, P. Lewi, 2011, Bioorganic & medicinal chemistry.

Screening of a PDE-focused library identifies imidazoles with in vitro and in vivo antischistosomal activity

I. D. de Esch, R. Leurs, H. D. de Koning, 2019, International journal for parasitology. Drugs and drug resistance.

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

A. Lambeir, I. De Meester, L. Maes, 2014, Journal of medicinal chemistry.

Schistosomicidal and molluscicidal activities of aminoalkylamino substituted neo- and norneocryptolepine derivatives

L. Pieters, P. Van der Veken, A. Haemers, 2012, Pharmaceutical biology.

Synthesis and antiplasmodial activity of aminoalkylamino-substituted neocryptolepine derivatives.

L. Maes, B. Maes, L. Pieters, 2009, Journal of medicinal chemistry.

Evaluation of [18 F]BR420 and [18 F]BR351 as radiotracers for MMP-9 imaging in colorectal cancer.

S. Dedeurwaerdere, S. Staelens, S. Deleye, 2017, Journal of labelled compounds & radiopharmaceuticals.

The role of the S1 binding site of carboxypeptidase M in substrate specificity and turn-over.

A. Lambeir, K. Gilany, G. Surpateanu, 2007, Biochimica et biophysica acta.

Efforts towards an on-target version of the Groebke-Blackburn-Bienaymé (GBB) reaction for discovery of druglike urokinase (uPA) inhibitors.

A. Lambeir, Dries Van Rompaey, P. Van der Veken, 2019, Chemistry.

Caspase-3 probes for PET imaging of apoptotic tumor response to anticancer therapy.

T. Vanden Berghe, P. Vandenabeele, S. Stroobants, 2019, Organic & biomolecular chemistry.

In vivo profiling of DPP4 inhibitors reveals alterations in collagen metabolism and accumulation of an amyloid peptide in rat plasma.

A. Lambeir, I. De Meester, P. Budde, 2009, Biochemical pharmacology.

Measurement of carboxypeptidase U (active thrombin-activatable fibrinolysis inhibitor) in plasma: Challenges overcome by a novel selective assay.

K. Augustyns, S. Van Goethem, D. Hendriks, 2010, Analytical biochemistry.

Selective Glucocorticoid Receptor Properties of GSK866 Analogs with Cysteine Reactive Warheads

W. D. De Vos, R. Houtman, K. Gevaert, 2017, Front. Immunol..

Inhibition of CD26/DPP IV attenuates ischemia/reperfusion injury in orthotopic mouse lung transplants: The pivotal role of vasoactive intestinal peptide

S. Korom, V. Matheeussen, W. Weder, 2010, Peptides.

Glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase. Part 1: Substitution of the glycine carboxylic acid group.

A. Fairlamb, A. Lambeir, A. Yamani, 2002, Bioorganic & medicinal chemistry letters.

AN EFFICIENT SYNTHESIS OF ORTHOGONALLY PROTECTED SPERMIDINE

A. Yamani, A. Haemers, K. Augustyns, 2002 .

Expression and spatial heterogeneity of dipeptidyl peptidases in endothelial cells of conduct vessels and capillaries

G. D. De Keulenaer, I. De Meester, G. D. De Meyer, 2011, Biological chemistry.

Lead optimization of phthalazinone phosphodiesterase inhibitors as novel antitrypanosomal compounds.

R. Leurs, S. Gul, M. Siderius, 2020, Journal of medicinal chemistry.

Synthesis and evaluation of caffeic acid amides as antioxidants.

P. Cos, D. V. Vanden Berghe, A. Haemers, 2001, Bioorganic & medicinal chemistry letters.

Development of a novel antibody-tetrazine conjugate for bioorthogonal pretargeting.

F. Sobott, S. Stroobants, S. Staelens, 2016, Organic & biomolecular chemistry.

Fluoro-olefins as peptidomimetic inhibitors of dipeptidyl peptidases.

A. Lambeir, I. De Meester, P. Van der Veken, 2005, Journal of medicinal chemistry.

CD26/dipeptidylpeptidase IV-targeted therapy of acute lung rejection in rats.

I. De Meester, P. Vogt, S. Korom, 2006, The Journal of heart and lung transplantation : the official publication of the International Society for Heart Transplantation.

Acyclic oligonucleotides: possibilities and limitations

J. Hoogmartens, P. Herdewijn, R. Busson, 1993 .

An Essential Signal Peptide Peptidase Identified in an RNAi Screen of Serine Peptidases of Trypanosoma brucei

J. Mottram, P. Van der Veken, K. Augustyns, 2015, PloS one.

The Effect of Serine Protease Inhibitors on Visceral Pain in Different Rodent Models With an Intestinal Insult

P. Pasricha, I. De Meester, Liansheng Liu, 2022, Frontiers in Pharmacology.

Targeting ferroptosis protects against multiorgan dysfunction and death.

Y. Saeys, P. Vandenabeele, R. Seurinck, 2021 .

Structure-activity relationship studies on isoindoline inhibitors of dipeptidyl peptidases 8 and 9 (DPP8, DPP9): is DPP8-selectivity an attainable goal?

Xin Chen, A. Lambeir, I. De Meester, 2011, Journal of medicinal chemistry.

Synthesis and evaluation of novel benzotropolones as Atg4B inhibiting autophagy blockers.

G. D. De Meyer, W. Martinet, A. Kurdi, 2019, Bioorganic chemistry.

Development and evaluation of peptide-based prolyl oligopeptidase inhibitors--introduction of N-benzyloxycarbonyl-prolyl-3-fluoropyrrolidine as a lead in inhibitor design.

G. Vanhoof, I. De Meester, D. Tourwé, 1997, European journal of biochemistry.

Improved stability of a novel fluorine-18 labeled TCO analogue for pretargeted PET imaging.

S. Stroobants, S. Staelens, P. Van der Veken, 2019, Nuclear medicine and biology.

In vivo evaluation of (18)F-labeled TCO for pre-targeted PET imaging in the brain.

S. Dedeurwaerdere, S. Stroobants, S. Staelens, 2014, Nuclear medicine and biology.

The Effect of Organ-Specific CD26/DPP IV Enzymatic Activity Inhibitor-Preconditioning on Acute Pulmonary Allograft Rejection

I. De Meester, S. Korom, W. Weder, 2009, Transplantation.

Primary Graft Dysfunction in Lung Transplantation: The Role of CD26/Dipeptidylpeptidase IV and Vasoactive Intestinal Peptide

I. De Meester, S. Korom, W. Weder, 2009, Transplantation.

Intragraft DPP IV inhibition attenuates post-transplant pulmonary ischemia/reperfusion injury after extended ischemia.

I. De Meester, S. Korom, W. Weder, 2007, The Journal of heart and lung transplantation : the official publication of the International Society for Heart Transplantation.

Proteases and Their Potential Role as Biomarkers and Drug Targets in Dry Eye Disease and Ocular Surface Dysfunction

K. Augustyns, Alba Ramos-Llorca, Camilla Scarpellini, 2022, International journal of molecular sciences.

Virtual screening for inhibitors of the human TSLP:TSLPR interaction

S. Savvides, K. Verstraete, Dries Van Rompaey, 2017, Scientific Reports.

Regulation of intestinal permeability: The role of proteases

A. Lambeir, I. De Meester, B. D. De Winter, 2017, World journal of gastroenterology.

Synthesis and biochemical evaluation of guanidino-alkyl-ribitol derivatives as nucleoside hydrolase inhibitors.

J. Steyaert, W. Versées, P. Van der Veken, 2008, European journal of medicinal chemistry.

Truncation of Macrophage-derived Chemokine by CD26/ Dipeptidyl-Peptidase IV beyond Its Predicted Cleavage Site Affects Chemotactic Activity and CC Chemokine Receptor 4 Interaction*

P. Allavena, G. Opdenakker, P. Proost, 1999, The Journal of Biological Chemistry.

Hybridization specificity, enzymatic activity and biological (Ha-ras) activity of oligonucleotides containing 2,4-dideoxy-beta-D-erythro-hexopyranosyl nucleosides.

P. Herdewijn, J. Rozenski, A. Van Aerschot, 1993, Nucleic acids research.

Selective inhibitors of fibroblast activation protein (FAP) with a xanthine scaffold

A. Lambeir, J. Joossens, K. Augustyns, 2014 .

The unique properties of dipeptidyl-peptidase IV (DPP IV / CD26) and the therapeutic potential of DPP IV inhibitors.

C. Durinx, A. Lambeir, A. Haemers, 1999, Current medicinal chemistry.

Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 2: isoindoline containing inhibitors.

Xin Chen, A. Lambeir, I. De Meester, 2008, Bioorganic & medicinal chemistry letters.

Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: identification of dipeptide derived leads.

Xin Chen, A. Lambeir, I. De Meester, 2008, Bioorganic & medicinal chemistry letters.

Dipeptidyl peptidase 8/9‐like activity in human leukocytes

Xin Chen, A. Lambeir, I. De Meester, 2007, Journal of leukocyte biology.

Natural substrates of dipeptidyl peptidase IV.

C. Durinx, P. Proost, I. De Meester, 2000, Advances in experimental medicine and biology.

The development and validation of a combined kinetic fluorometric activity assay for fibroblast activation protein alpha and prolyl oligopeptidase in plasma.

A. Lambeir, I. De Meester, R. Van Elzen, 2019, Clinica chimica acta; international journal of clinical chemistry.

Influence of the Incorporation of 1-(2,3-Dideoxy-β-D-Erythro-Hexopyranosyl)-Thymine on the Enzymatic Stability and Base-Pairing Properties of Oligodeoxynucleotides

P. Herdewijn, A. Aerschot, C. Urbanke, 2010 .

Prolyl oligopeptidase of Trypanosoma brucei hydrolyzes native collagen, peptide hormones and is active in the plasma of infected mice.

Sébastien Charneau, L. Dubost, P. Grellier, 2010, Microbes and infection.

Ischemia/reperfusion injury: The role of CD26/dipeptidyl-peptidase-IV-inhibition in lung transplantation.

I. De Meester, S. Korom, W. Weder, 2006, Transplantation proceedings.

Design, synthesis, and SAR of potent and selective dipeptide-derived inhibitors for dipeptidyl peptidases.

A. Lambeir, I. De Meester, P. Van der Veken, 2003, Journal of medicinal chemistry.

Adhesion of PLGA or Eudragit/PLGA nanoparticles to Staphylococcus and Pseudomonas.

A. Ludwig, J. Vandervoort, P. Cos, 2008, International journal of pharmaceutics.

Synthesis of (E)- and (Z)-fluoro-olefin analogues of potent dipeptidyl peptidase IV inhibitors

A. Haemers, K. Augustyns, P. Veken, 2003 .

Selected strategies to fight pathogenic bacteria

C. Supuran, J. Yli-Kauhaluoma, A. Sobolev, 2023, Journal of enzyme inhibition and medicinal chemistry.

Visceral hypersensitivity in inflammatory bowel diseases and irritable bowel syndrome: The role of proteases

A. Lambeir, I. De Meester, B. D. De Winter, 2016, World journal of gastroenterology.

Inhibitors Targeting RIPK1/RIPK3: Old and New Drugs.

P. Vandenabeele, W. Declercq, K. Augustyns, 2020, Trends in pharmacological sciences.

Design and evaluation of Trypanosoma brucei metacaspase inhibitors.

G. H. Coombs, J. Mottram, M. Berg, 2010, Bioorganic & medicinal chemistry letters.

Synthesis of Bicyclic N‐Arylmethyl‐Substituted Iminoribitol Derivatives as Selective Nucleoside Hydrolase Inhibitors

J. Steyaert, W. Versées, M. Berg, 2009, ChemMedChem.

Synthesis of 6-methyl-6H-indolo[3,2-c]isoquinoline and 6-methyl-6H-indolo[2,3-c]isoquinoline: two new unnatural isoquinoline isomers of the cryptolepine series

L. Maes, R. Dommisse, Gitte Van Baelen, 2008 .

Development of irreversible diphenyl phosphonate inhibitors for urokinase plasminogen activator.

A. Lambeir, P. Van der Veken, J. Joossens, 2004, Journal of medicinal chemistry.

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

A. Lambeir, I. De Meester, A. Haemers, 1999, Journal of medicinal chemistry.

Rapid parallel synthesis of dipeptide diphenyl phosphonate esters as inhibitors of dipeptidyl peptidases.

A. Lambeir, I. De Meester, P. Van der Veken, 2003, Journal of combinatorial chemistry.

Evaluation of Nucleoside Hydrolase Inhibitors for Treatment of African Trypanosomiasis

H. D. de Koning, J. Steyaert, M. Degano, 2010, Antimicrobial Agents and Chemotherapy.

Crystal structures of T. vivax nucleoside hydrolase in complex with new potent and specific inhibitors.

J. Steyaert, W. Versées, M. Berg, 2009, Biochimica et biophysica acta.

N-Arylmethyl substituted iminoribitol derivatives as inhibitors of a purine specific nucleoside hydrolase.

J. Steyaert, W. Versées, M. Berg, 2008, Bioorganic & medicinal chemistry.

1,2,3-Triazolylalkylribitol derivatives as nucleoside hydrolase inhibitors.

J. Steyaert, W. Versées, S. Apers, 2007, Bioorganic & medicinal chemistry letters.

A Convenient One-Pot Preparation of Disubstituted Phosphinic Acids Derived from Simple Amino Acids and Proline

A. Haemers, K. Augustyns, M. Borloo, 1995 .

Enzyme Activity and Immunohistochemical Localization of Dipeptidyl Peptidase 8 and 9 in Male Reproductive Tissues

Xin Chen, A. Lambeir, V. Dubois, 2009, The journal of histochemistry and cytochemistry : official journal of the Histochemistry Society.

Evaluation of phthalazinone phosphodiesterase inhibitors with improved activity and selectivity against Trypanosoma cruzi.

I. D. de Esch, R. Leurs, H. D. de Koning, 2019, The Journal of antimicrobial chemotherapy.

Rapid parallel synthesis of dipeptide diphenyl phosphonate esters as inhibitors of dipeptidyl peptidases.

A. Lambeir, I. De Meester, P. Van der Veken, 2003, Journal of combinatorial chemistry.

Differential characterization using readily accessible NMR experiments of novel N- and O-alkylated quinolin-4-ol, 1,5-naphthyridin-4-ol and quinazolin-4-ol derivatives with antimycobacterial activity.

Robert H Bates, Fraser Cunningham, P. Van der Veken, 2017, European journal of medicinal chemistry.

Lewis Acid Catalyzed Synthesis of N‐Protected Diphenyl 1‐Aminoalkylphosphonates.

C. Stevens, J. Joossens, A. Haemers, 2005 .

Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates.

Xin Chen, A. Lambeir, I. De Meester, 2007, Journal of medicinal chemistry.

Synthesis of 2,4-dideoxy-.beta.-D-erythro-hexopyranosyl nucleosides

P. Herdewijn, J. Rozenski, G. Janssen, 1993 .

Diphenyl phosphonate inhibitors for the urokinase-type plasminogen activator: optimization of the P4 position.

Georgiana Surpateanu, Jurgen Joossens, Koen Augustyns, 2006, Journal of medicinal chemistry.

From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.

J. Heeres, P. Lewi, G. Vanham, 2014, Bioorganic & medicinal chemistry.

In vivo effects of a potent, selective DPPII inhibitor: UAMC00039 is a possible tool for the elucidation of the physiological function of DPPII.

A. Lambeir, I. De Meester, P. Van der Veken, 2006, Advances in experimental medicine and biology.

Synthesis of γ,δ‐Aziridino α‐Amino Acid Derivatives and their Stereoselective Ring Transformation to 2‐(Aminomethyl)‐1‐aminocyclopropanecarboxylic Acid Derivatives

Yahya Nural, Sven Mangelinckx, K. Törnroos, 2014 .

Trypanothione as a target in the design of antitrypanosomal and antileishmanial agents.

A. Yamani, A. Haemers, K. Augustyns, 2001, Current pharmaceutical design.

Dipeptide-derived diphenyl phosphonate esters: mechanism-based inhibitors of dipeptidyl peptidase IV.

A. Lambeir, I. De Meester, A. Haemers, 1996, Biochimica et Biophysica Acta.

Synthesis of a new branched chain hexopyranosyl nucleoside: 1-[2′,3′-dideoxy-3′-C-(hydroxymethyl)-α-D-erythro-pentopyranosyl]-thymine

P. Herdewijn, R. Busson, J. Rozenski, 1994 .

A Convenient One-Pot Preparation of Disubstituted Phosphinic Acids Derived from Simple Amino Acids and Proline.

A. Haemers, K. Augustyns, M. Borloo, 1996 .

Dipeptidyl α-fluorovinyl Michael acceptors: Synthesis and activity against cysteine proteases

Gareth D. Westrop, Koen Augustyns, Alisa Krishtal, 2007 .

Development and in vitro evaluation of a vaginal microbicide gel formulation for UAMC01398, a novel diaryltriazine NNRTI against HIV-1.

Patrick Augustijns, Paul J Lewi, Jurgen Joossens, 2014, Antiviral research.

The use of supersaturation for the vaginal application of microbicides: a case study with dapivirine.

P. Augustijns, J. Brouwers, K. Augustyns, 2014, Journal of pharmaceutical sciences.

In Vitro Antioxidant Profile of Phenolic Acid Derivatives

L. Pieters, A. Vlietinck, P. Cos, 2002, Free radical research.

In Vitro Antioxidant Profile of Phenolic Acid Derivatives.

L. Pieters, A. Vlietinck, P. Cos, 2002, Free radical research.

Novel triazine dimers with potent antitrypanosomal activity.

J. Heeres, P. Lewi, L. Maes, 2018, European journal of medicinal chemistry.

Molecular, functional and structural properties of the prolyl oligopeptidase of Trypanosoma cruzi (POP Tc80), which is required for parasite entry into mammalian cells.

B. Maigret, J. F. da Silveira, N. Martins, 2005, The Biochemical journal.

Novel selective glucocorticoid receptor agonists (SEGRAs) with a covalent warhead for long-lasting inhibition.

W. Vanden Berghe, P. Van der Veken, J. Joossens, 2016, Bioorganic & medicinal chemistry letters.

Substrate Activity Screening (SAS) and Related Approaches in Medicinal Chemistry

A. Lambeir, J. Joossens, K. Augustyns, 2016, ChemMedChem.

α‐Ketoheterocycles as Inhibitors of Leishmania mexicana Cysteine Protease CPB

G. H. Coombs, J. Mottram, M. Berg, 2010, ChemMedChem.

The use of time‐averaged 3JHH restrained molecular dynamics (tar‐MD) simulations for the conformational analysis of five‐membered ring systems: Methodology and applications

Koen Augustyns, Pieter M. S. Hendrickx, Francisco Corzana, 2009, J. Comput. Chem..

Substrate-assisted Leaving Group Activation in Enzyme-catalyzed N-Glycosidic Bond Cleavage*

J. Steyaert, P. Geerlings, W. Versées, 2005, Journal of Biological Chemistry.

Inhibitors of the Purine Salvage Pathway: A Valuable Approach for Antiprotozoal Chemotherapy?

M. Berg, P. Van der Veken, A. Haemers, 2010, Current medicinal chemistry.

Synthesis and anti-HIV evaluation of 2',3'-dideoxyribo-5-chloropyrimidine analogues: reduced toxicity of 5-chlorinated 2',3'-dideoxynucleosides.

E. De Clercq, G. Janssen, J. Balzarini, 1990, Journal of medicinal chemistry.

Influence of the incorporation of (S)-9-(3,4-dihydroxybutyl)adenine on the enzymatic stability and base-pairing properties of oligodeoxynucleotides.

A. Van Schepdael, P. Herdewijn, C. Urbanke, 1991, Nucleic acids research.

Structures of purine nucleosidase from Trypanosoma brucei bound to isozyme-specific trypanocidals and a novel metalorganic inhibitor.

M. Degano, M. Berg, P. Van der Veken, 2013, Acta crystallographica. Section D, Biological crystallography.

Synthesis and Anti-HIV Evaluation of 2′,3′-Dideoxyribo-5-chloropyrimidine Analogues: Reduced Toxicity of 5-Chlorinated 2′,3′-Dideoxynucleosides.

P. Herdewijn, G. Janssen, A. Aerschot, 1990 .

Hexopyranosyl-like oligonucleotides

P. Herdewijn, A. Aerschot, K. Augustyns, 1994 .

RIPK1-dependent cell death: a novel target of the Aurora kinase inhibitor Tozasertib (VX-680)

P. Vandenabeele, N. Takahashi, M. Vuylsteke, 2018, Cell Death & Disease.

ATG4B inhibitors with a benzotropolone core structure block autophagy and augment efficiency of chemotherapy in mice

G. D. De Meyer, W. Martinet, A. Kurdi, 2017, Biochemical pharmacology.

The Potential Role of Regulated Cell Death in Dry Eye Diseases and Ocular Surface Dysfunction

K. Augustyns, Caroline Lanthier, Greta Klejborowska, 2023, International journal of molecular sciences.

Discovery of Novel, Drug-Like Ferroptosis Inhibitors with in Vivo Efficacy.

P. Vandenabeele, Samya Van Coillie, L. Maes, 2018, Journal of medicinal chemistry.

Search for substrates for prolyl oligopeptidase in porcine brain

B. Devreese, J. Beeumen, A. Lambeir, 2005, Peptides.

The power metric: a new statistically robust enrichment-type metric for virtual screening applications with early recovery capability

Julio Cesar Dias Lopes, Koen Augustyns, Hans De Winter, 2017, Journal of Cheminformatics.

Dipeptidyl peptidases in atherosclerosis: expression and role in macrophage differentiation, activation and apoptosis

W. Martinet, G. Meyer, V. Matheeussen, 2013, Basic Research in Cardiology.

The therapeutic potential of inhibitors of dipeptidyl peptidase IV (DPP IV) and related proline-specific dipeptidyl aminopeptidases.

P. Van der Veken, A. Haemers, K. Augustyns, 2005, Current medicinal chemistry.

Chemically diverse activity-based probes with unexpected inhibitory mechanisms targeting trypsin-like serine proteases

G. Boeckxstaens, A. Lambeir, I. De Meester, 2023, Frontiers in Chemistry.

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

A. Lambeir, I. De Meester, P. Van der Veken, 2012, Bioorganic & medicinal chemistry letters.

Vaginal expression of efflux transporters and the potential impact on the disposition of microbicides in vitro and in rabbits.

M. Baes, P. la Colla, P. Augustijns, 2014, Molecular pharmaceutics.

Novel Ferroptosis Inhibitors with Improved Potency and ADME Properties.

T. Vanden Berghe, P. Vandenabeele, P. Van der Veken, 2016, Journal of medicinal chemistry.

Carboxylate isosteres for caspase inhibitors: the acylsulfonamide case revisited.

A. Lambeir, M. Lamkanfi, L. Vande Walle, 2017, Organic & biomolecular chemistry.

Targeting ferroptosis protects against experimental (multi)organ dysfunction and death

Y. Saeys, T. Vanden Berghe, P. Vandenabeele, 2022, Nature communications.

Dipeptidyl peptidase II and leukocyte cell death.

A. Lambeir, I. De Meester, D. Schrijvers, 2006, Biochemical pharmacology.

Kinetic Investigation of Chemokine Truncation by CD26/Dipeptidyl Peptidase IV Reveals a Striking Selectivity within the Chemokine Family*

C. Durinx, P. Proost, A. Lambeir, 2001, The Journal of Biological Chemistry.

Novel drug discovery strategies for atherosclerosis that target necrosis and necroptosis

G. D. De Meyer, W. Martinet, P. Van der Veken, 2018, Expert opinion on drug discovery.

A New Approach Towards the Synthesis of 3-Amino-6-(hetero)arylpyridazines Based on Palladium Catalyzed Cross-coupling Reactions

R. Dommisse, B. Maes, A. Haemers, 2000 .

Searching for New Leads for Tuberculosis: Design, Synthesis, and Biological Evaluation of Novel 2-Quinolin-4-yloxyacetamides.

Robert H Bates, Fraser Cunningham, P. Van der Veken, 2016, Journal of medicinal chemistry.

Optimization of hydantoins as potent antimycobacterial decaprenylphosphoryl-β-D-ribose oxidase (DprE1) inhibitors.

Robert H Bates, Fraser Cunningham, P. Van der Veken, 2020, Journal of medicinal chemistry.

Identification and Profiling of Hydantoins-A Novel Class of Potent Antimycobacterial DprE1 Inhibitors.

Christophe M. L. Vande Velde, Robert H Bates, Fraser Cunningham, 2018, Journal of medicinal chemistry.

Strecker-Derived Methodology for Library Synthesis of N-Acylated α-Aminonitriles

B. Maes, P. Van der Veken, K. Augustyns, 2021, ACS omega.

Diaryltriazine non-nucleoside reverse transcriptase inhibitors are potent candidates for pre-exposure prophylaxis in the prevention of sexual HIV transmission.

Paul J Lewi, Jurgen Joossens, Koen Augustyns, 2013, The Journal of antimicrobial chemotherapy.

Sorafenib tosylate inhibits directly necrosome complex formation and protects in mouse models of inflammation and tissue injury

P. Vandenabeele, S. Fulda, J. Bräsen, 2017, Cell Death and Disease.

To Target or Not to Target Schistosoma mansoni Cyclic Nucleotide Phosphodiesterase 4A?

Georgi K. Kanev, I. D. de Esch, R. Leurs, 2023, International journal of molecular sciences.

Kinetic investigation of human dipeptidyl peptidase II (DPPII)-mediated hydrolysis of dipeptide derivatives and its identification as quiescent cell proline dipeptidase (QPP)/dipeptidyl peptidase 7 (DPP7).

A. Lambeir, I. De Meester, B. Leiting, 2005, The Biochemical journal.

Pyrrolidides: synthesis and structure-activity relationship as inhibitors of dipeptidyl peptidase IV

A. Haemers, Koen Augustyns, G. Vanhoof, 1997 .

Identification and Characterization of Approved Drugs and Drug-Like Compounds as Covalent Escherichia coli ClpP Inhibitors

M. Winterhalter, B. Windshügel, K. Augustyns, 2019, International journal of molecular sciences.

ClpP Protease, a Promising Antimicrobial Target

P. Van der Veken, K. Augustyns, Carlos Moreno-Cinos, 2019, International journal of molecular sciences.

Glutathione-like tripeptides as inhibitors of glutathionylspermidine synthetase. Part 2: substitution of the glycine part.

A. Fairlamb, A. Lambeir, A. Yamani, 2002, Bioorganic & medicinal chemistry letters.

Investigation on the stability of the Dde protecting group used in peptide synthesis: migration to an unprotected lysine.

K. Augustyns, W. Kraas, G. Jung, 2009, The journal of peptide research : official journal of the American Peptide Society.

Synthesis and preclinical evaluation of an 18F labeled PDE7 inhibitor for PET neuroimaging.

S. Dedeurwaerdere, S. Stroobants, S. Staelens, 2015, Nuclear medicine and biology.

Tozasertib Analogues as Inhibitors of Necroptotic Cell Death.

P. Vandenabeele, N. Takahashi, W. Nerinckx, 2018, Journal of medicinal chemistry.

RIPK1-dependent cell death: a novel target of the Aurora kinase inhibitor Tozasertib (VX-680)

P. Vandenabeele, N. Takahashi, M. Vuylsteke, 2018, Cell Death & Disease.

When PERK inhibitors turn out to be new potent RIPK1 inhibitors: critical issues on the specificity and use of GSK2606414 and GSK2656157

M. Bertrand, P. Vandenabeele, D. Rojas-Rivera, 2017, Cell Death and Differentiation.

Repositioning the Substrate Activity Screening (SAS) Approach as a Fragment‐Based Method for Identification of Weak Binders

Rafaela Gladysz, Matthias Cleenewerck, Jurgen Joossens, 2014, Chembiochem : a European journal of chemical biology.

Optimization of the pharmacokinetic properties of potent anti-trypanosomal triazine derivatives.

L. Maes, P. Van der Veken, G. Caljon, 2018, European journal of medicinal chemistry.

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

V. Fülöp, V. Baekelandt, A. Lambeir, 2012, Journal of medicinal chemistry.

Resistance and cross-resistance profile of the diaryltriazine NNRTI and candidate microbicide UAMC01398.

J. Heeres, G. Vanham, L. Heyndrickx, 2016, The Journal of antimicrobial chemotherapy.

Prolyl oligopeptidase stimulates the aggregation of α-synuclein

V. Baekelandt, B. Devreese, A. Lambeir, 2008, Peptides.

Synthesis and electrophysiological characterization of cyclic morphiceptin analogues.

J. Tytgat, P. Van der Veken, A. Haemers, 2004, Biochemical pharmacology.

From PERK to RIPK1: Design, synthesis and evaluation of novel potent and selective necroptosis inhibitors

M. Bertrand, P. Van der Veken, K. Augustyns, 2023, Frontiers in Chemistry.

Increased tissue and circulating levels of dipeptidyl peptidase-IV enzymatic activity in patients with pancreatic ductal adenocarcinoma.

M. Brabec, J. Škrha, M. Zavoral, 2016, Pancreatology : official journal of the International Association of Pancreatology (IAP) ... [et al.].

PRINCIPLES OF PHARMACOLOGY

K. Augustyns, A. Haemers, A. Haemers, 1937 .

Polymer-assisted solution-phase parallel synthesis of dipeptide p-nitroanilides and dipeptide diphenyl phosphonates

A. Haemers, K. Augustyns, P. Veken, 2001 .

A Novel Ferroptosis Inhibitor UAMC-3203, a Potential Treatment for Corneal Epithelial Wound

A. Urtti, Kati-Sisko Vellonen, M. Ruponen, 2022, Pharmaceutics.

Effect of erythrophagocytosis-induced ferroptosis during angiogenesis in atherosclerotic plaques

P. Guns, L. Roth, G. D. De Meyer, 2023, Angiogenesis.

Synthesis and Evaluation of a Zr-89-Labeled Monoclonal Antibody for Immuno-PET Imaging of Amyloid-β Deposition in the Brain

S. Dedeurwaerdere, M. Mercken, S. Stroobants, 2016, Molecular Imaging and Biology.

Development and characterization of a solid dispersion film for the vaginal application of the anti-HIV microbicide UAMC01398.

P. Augustijns, J. Brouwers, K. Ariën, 2014, International journal of pharmaceutics.

Spectrophores as one-dimensional descriptors calculated from three-dimensional atomic properties: applications ranging from scaffold hopping to multi-target virtual screening

Rafaela Gladysz, Koen Augustyns, Hans De Winter, 2018, Journal of Cheminformatics.

SYNTHESIS OF PEPTIDYL ACETALS AS INHIBITORS OF PROLYL ENDOPEPTIDASE

A. Haemers, K. Augustyns, S. Scharpe, 1995 .

In Vivo Amyloid-β Imaging in the APPPS1–21 Transgenic Mouse Model with a 89Zr-Labeled Monoclonal Antibody

S. Dedeurwaerdere, M. Mercken, S. Stroobants, 2016, Front. Aging Neurosci..

Exploration of the active site of dipeptidyl peptidase IV from Porphyromonas gingivalis. Comparison with the human enzyme.

V. Fülöp, A. Lambeir, I. De Meester, 2003, Advances in experimental medicine and biology.

Inhibitors of proline-specific dipeptidyl peptidases: DPP IV inhibitors as a novel approach for the treatment of Type 2 diabetes

Koen Augustyns, Pieter Van der Veken, P. Van der Veken, 2005 .

Prolyl peptidases related to dipeptidyl peptidase IV: potential of specific inhibitors in drug discovery.

P. Van der Veken, A. Haemers, K. Augustyns, 2007, Current topics in medicinal chemistry.

A new synthetic method for proline diphenyl phosphonates

A. Lambeir, A. Haemers, K. Augustyns, 1995 .

Structural determinants for ligand binding and catalysis of triosephosphate isomerase.

R. Wierenga, A. Lambeir, I. Kursula, 2001, European journal of biochemistry.

Development of a sensitive and selective assay for the determination of procarboxypeptidase U (thrombin-activatable fibrinolysis inhibitor) in plasma.

K. Augustyns, T. Olsson, S. Van Goethem, 2010, Analytical biochemistry.

Prolylisoxazoles: potent inhibitors of prolyloligopeptidase with antitrypanosomal activity.

S. Croft, A. Lambeir, P. Van der Veken, 2003, Bioorganic & medicinal chemistry letters.

Vildagliptin‐Derived Dipeptidyl Peptidase 9 (DPP9) Inhibitors: Identification of a DPP8/9‐Specific Lead

I. De Meester, P. Van der Veken, K. Augustyns, 2022, ChemMedChem.

Purification and characterization of a dipeptidyl peptidase 9-like enzyme from bovine testes

Xin Chen, A. Lambeir, J. Creemers, 2007 .

In Vitro and In Situ Activity-Based Labeling of Fibroblast Activation Protein with UAMC1110-Derived Probes

O. De Wever, A. Lambeir, I. De Meester, 2021, Frontiers in Chemistry.

The role of CD26/DPP IV in preservation of early pulmonary graft function.

I. De Meester, S. Korom, W. Weder, 2006, Advances in experimental medicine and biology.

Probing for improved selectivity with dipeptide-derived inhibitors of dipeptidyl peptidases 8 and 9: the impact of P1-variation

Xin Chen, A. Lambeir, J. Joossens, 2016 .

Functional role of the conserved active site proline of triosephosphate isomerase.

P. Neubauer, R. Wierenga, A. Lambeir, 2007, Biochemistry.

Ferroptosis contributes to multiple sclerosis and its pharmacological targeting suppresses experimental disease progression

T. Vanden Berghe, P. Vandenabeele, H. Bayır, 2023, Cell Death & Differentiation.

Preclinical evaluation of [ ]MICA-401, an activity-based probe for SPECT imaging of in vivo uPA activity Reference:

S. Stroobants, S. Staelens, D. Thomae, 2017 .

α-Amino Diphenyl Phosphonates as Novel Inhibitors of Escherichia coli ClpP Protease.

M. Winterhalter, B. Windshügel, P. Van der Veken, 2019, Journal of medicinal chemistry.

Synthesis, evaluation and structure-activity relationships of triazine dimers as novel antiviral agents.

J. Heeres, P. Lewi, G. Vanham, 2012, Bioorganic & medicinal chemistry letters.

author-version of: Increased tissue and circulating levels of dipeptidyl peptidase-IV enzymatic activity in patients with pancreatic ductal adenocarcinoma

M. Brabec, M. Zavoral, K. Augustyns, 2022 .

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

A. Lambeir, I. De Meester, L. Maes, 2014, Journal of medicinal chemistry.

Purification and characterization of dipeptidyl peptidase IV-like enzymes from bovine testes.

Xin Chen, A. Lambeir, I. De Meester, 2008, Frontiers in bioscience : a journal and virtual library.

author-version of: Increased tissue and circulating levels of dipeptidyl peptidase-IV enzymatic activity in patients with pancreatic ductal adenocarcinoma

M. Brabec, M. Zavoral, K. Augustyns, 2022 .

Structures of purine nucleosidase from Trypanosoma brucei bound to isozyme-specific trypanocidals and a novel metalorganic inhibitor.

M. Degano, M. Berg, P. Van der Veken, 2013, Acta crystallographica. Section D, Biological crystallography.

Beyond ferrostatin-1: a comprehensive review of ferroptosis inhibitors.

T. Vanden Berghe, Behrouz Hassannia, K. Augustyns, 2023, Trends in pharmacological sciences.

Reverse transcriptase inhibitors as microbicides.

J. Heeres, P. Lewi, G. Vanham, 2012, Current HIV research.

Evaluation of Nucleoside Hydrolase Inhibitors for Treatment of African Trypanosomiasis

H. D. de Koning, J. Steyaert, M. Degano, 2010, Antimicrobial Agents and Chemotherapy.

Synthesis of 1-(2,4-dideoxy-β-D-erythro-hexopyranosyl)thymine and its incorporation into oligonucleotides

A. Aerschot, K. Augustyns, Piet Herdwijn, 1992 .

Characterization of Structurally Diverse 18F-Labeled d-TCO Derivatives as a PET Probe for Bioorthogonal Pretargeted Imaging

P. Van der Veken, K. Augustyns, C. Vangestel, 2023, ACS omega.

Synthesis of Bicyclic N‐Arylmethyl‐Substituted Iminoribitol Derivatives as Selective Nucleoside Hydrolase Inhibitors

J. Steyaert, W. Versées, M. Berg, 2009, ChemMedChem.

Asymmetric synthesis of γ-chloro-α,β-diamino- and β,γ-aziridino-α-aminoacylpyrrolidines and -piperidines via stereoselective Mannich-type additions of N-(diphenylmethylene)glycinamides across α-chloro-N-sulfinylimines

Sven Mangelinckx, K. Törnroos, P. Van der Veken, 2012, Beilstein journal of organic chemistry.