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List of works by Koen Augustyns

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

scientific article published on 09 February 2007

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

scientific article

Acyclic oligonucleotides: possibilities and limitations

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

scientific article published on 4 April 2012

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

scientific article published on 7 August 2007

An essential signal peptide peptidase identified in an RNAi screen of serine peptidases of Trypanosoma brucei

scientific article

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

scientific article published on 5 December 2012

Author Correction: Virtual screening for inhibitors of the human TSLP:TSLPR interaction.

scientific article

CD26/Dipeptidylpeptidase IV–targeted Therapy of Acute Lung Rejection in Rats

scientific article published on 17 August 2006

Carboxylate isosteres for caspase inhibitors: the acylsulfonamide case revisited.

scientific article

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

scientific article published on 01 May 2019

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

scientific article published on 10 August 2017

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

scientific article

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

scientific article published on 04 February 2019

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

scientific article

Design and evaluation of Trypanosoma brucei metacaspase inhibitors.

scientific article

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

scientific article published in November 2003

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

scientific article published on 28 August 2014

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

scientific article published on 20 November 2013

Development of a novel antibody-tetrazine conjugate for bioorthogonal pretargeting

scientific article published on 19 July 2016

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

scientific article published on 2 September 2009

Development of irreversible diphenyl phosphonate inhibitors for urokinase plasminogen activator

scientific article published in May 2004

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

scientific article

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

scientific article published on 11 October 2016

Dipeptidyl alpha-fluorovinyl Michael acceptors: synthesis and activity against cysteine proteases

scientific article published on 23 October 2007

Dipeptidyl peptidase 8/9-like activity in human leukocytes

scientific article published on 07 February 2007

Dipeptidyl peptidase II and leukocyte cell death.

scientific article published on 25 April 2006

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

scientific article published on 23 April 2013

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

scientific article

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

article

Enzyme activity and immunohistochemical localization of dipeptidyl peptidase 8 and 9 in male reproductive tissues

scientific article published on 02 February 2009

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

scientific article published on 21 December 2016

Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis

scientific article

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

scientific article published on March 2011

Extended Structure–Activity Relationship and Pharmacokinetic Investigation of (4-Quinolinoyl)glycyl-2-cyanopyrrolidine Inhibitors of Fibroblast Activation Protein (FAP)

article

Fluoro-Olefins as Peptidomimetic Inhibitors of Dipeptidyl Peptidases

scientific article published on 01 March 2005

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

scientific article

Functional role of the conserved active site proline of triosephosphate isomerase

scientific article

Gamma-amino-substituted analogues of 1-[(S)-2,4-diaminobutanoyl]piperidine as highly potent and selective dipeptidyl peptidase II inhibitors

scientific article

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

scientific article published on 13 December 2018

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

scientific article published on 31 March 2016

In vitro antioxidant profile of phenolic acid derivatives

scientific article published in June 2002

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

scientific article published on 2 April 2014

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

scientific article

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

scientific article published on 6 June 2016

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

scientific article published on 16 December 2009

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

scientific article

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

scientific article published on 24 May 2008

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

scientific article published on 24 May 2008

Intragraft DPP IV Inhibition Attenuates Post-transplant Pulmonary Ischemia/Reperfusion Injury After Extended Ischemia

scientific article published on 01 February 2007

Irreversible Inhibition of Dipeptidyl Peptidase 8 by Dipeptide-Derived Diaryl Phosphonates

scientific article published on 24 October 2007

Ischemia/Reperfusion Injury: The Role of CD26/Dipeptidyl-Peptidase-IV-Inhibition in Lung Transplantation

scientific article published on 01 December 2006

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).

scientific article published on March 2005

Lead Optimization of Phthalazinone Phosphodiesterase Inhibitors as Novel Antitrypanosomal Compounds

scientific article published on 26 March 2020

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

scientific article published on 3 April 2010

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

scientific article published on 18 June 2008

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

scientific article published on 23 July 2018

Novel Ferroptosis Inhibitors with Improved Potency and ADME Properties

scientific article published on 22 December 2015

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

scientific article published on September 2011

Novel drug discovery strategies for atherosclerosis that target necrosis and necroptosis.

scientific article

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

scientific article published on 31 August 2016

Novel triazine dimers with potent antitrypanosomal activity.

scientific article published on 27 November 2017

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

scientific article

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

scientific article

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

scientific article

Primary graft dysfunction in lung transplantation: the role of CD26/dipeptidylpeptidase IV and vasoactive intestinal peptide.

scientific article published in April 2009

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

article

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

scientific article published on 24 February 2010

Prolyl oligopeptidase stimulates the aggregation of alpha-synuclein

scientific article published on 15 May 2008

Prolylisoxazoles: potent inhibitors of prolyloligopeptidase with antitrypanosomal activity

scientific article published in September 2003

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

scientific article published on 01 May 2008

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

scientific article published on 12 February 2018

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

scientific article published in May 2003

Regulation of intestinal permeability: The role of proteases

scientific article published on March 2017

Repositioning the substrate activity screening (SAS) approach as a fragment-based method for identification of weak binders

scientific article

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

scientific article published on 4 February 2016

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

scientific article

Search for substrates for prolyl oligopeptidase in porcine brain

scientific article published on 5 July 2005

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

scientific article

Selective Glucocorticoid Receptor Properties of GSK866 Analogs with Cysteine Reactive Warheads

scientific article published in November 2017

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

scientific article

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

article

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

scientific article published in December 2007

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

scientific article published on 29 June 2017

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

scientific article published on 7 March 2018

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

scientific article

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

scientific article

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

scientific article

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

scientific article published on 4 February 2016

Substrate-assisted leaving group activation in enzyme-catalyzed N-glycosidic bond cleavage.

scientific article published on 28 January 2005

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

scientific article published on 4 February 2016

Synthesis and antiplasmodial activity of aminoalkylamino-substituted neocryptolepine derivatives

scientific article

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

scientific article published on 10 April 2007

Synthesis and dipeptidyl peptidase inhibition of N-(4-substituted-2,4-diaminobutanoyl)piperidines

scientific article published on 17 July 2006

Synthesis and electrophysiological characterization of cyclic morphiceptin analogues

scientific article published in May 2004

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

scientific article published on 27 December 2011

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

scientific article published on 29 March 2014

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

scientific article published on 29 July 2015

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

Synthesis of bicyclic N-arylmethyl-substituted iminoribitol derivatives as selective nucleoside hydrolase inhibitors.

scientific article published in February 2009

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

scientific article

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

scholarly article published 20 February 2018

The effect of organ-specific CD26/DPP IV enzymatic activity inhibitor-preconditioning on acute pulmonary allograft rejection.

scientific article published in August 2009

The first potent diphenyl phosphonate KLK4 inhibitors with unexpected binding kinetics

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

scientific article (publication date: 2 February 2017)

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

scientific article published on 08 December 2006

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

scientific article published on 17 September 2014

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

scientific article

Tozasertib Analogues as Inhibitors of Necroptotic Cell Death

scientific article published on 13 February 2018

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

scientific article

Virtual screening for inhibitors of the human TSLP:TSLPR interaction.

scientific article published on 8 December 2017

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

scientific article (publication date: 21 December 2016)

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

scientific article

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

scientific article published on 11 January 2019

α-ketoheterocycles as inhibitors of Leishmania mexicana cysteine protease CPB.

scientific article published on October 2010