J. Joossens

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.

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.

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.

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.

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.

Synthesis and antiplasmodial activity of aminoalkylamino-substituted neocryptolepine derivatives.

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

Selective Glucocorticoid Receptor Properties of GSK866 Analogs with Cysteine Reactive Warheads

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

Solid and solution phase syntheses of the 2-cyanopyrrolidide DPP-IV inhibitor NVP-DPP728

A. Tartar, N. Willand, J. Joossens, 2002 .

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

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

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.

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.

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.

Regulation of intestinal permeability: The role of proteases

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

Inhibition of dipeptidyl-peptidase IV catalyzed peptide truncation by Vildagliptin ((2S)-{[(3-hydroxyadamantan-1-yl)amino]acetyl}-pyrrolidine-2-carbonitrile).

Xin Chen, A. Lambeir, I. De Meester, 2005, Biochemical pharmacology.

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

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

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.

Design and evaluation of Trypanosoma brucei metacaspase inhibitors.

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

Development of irreversible diphenyl phosphonate inhibitors for urokinase plasminogen activator.

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

Evaluation of Nucleoside Hydrolase Inhibitors for Treatment of African Trypanosomiasis

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

Evaluation of nucleoside hydrolase inhibitors for the treatment of 1 African trypanosomiasis

J. Steyaert, M. Degano, W. Versées, 2010 .

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

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

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.

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.

Novel triazine dimers with potent antitrypanosomal activity.

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

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.

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.

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.

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.

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.

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

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

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.

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.

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.

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..

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 .

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.

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.

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.