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1.

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

De Araújo, Julianna Siciliano; da Silva, Patrícia Bernardino; Batista, Marcos Meuser; Peres, Raiza Brandão; Cardoso-Santos, Camila; Kalejaiye, Titilola D; Munday, Jane C; De Heuvel, Erik; Sterk, Geert Jan; Augustyns, Koen; Salado, Irene G; Matheeussen, An; De Esch, Iwan; De Koning, Harry P; Leurs, Rob; Maes, Louis; Soeiro, Maria de Nazaré Correia.

J Antimicrob Chemother; 75(4): 958-967, 2020 Apr 01.

Artículo en Inglés | MEDLINE | ID: mdl-31860098

2.

Design and evaluation of Trypanosoma brucei metacaspase inhibitors.

Berg, Maya; Van der Veken, Pieter; Joossens, Jurgen; Muthusamy, Venkatraj; Breugelmans, Matthias; Moss, Catherine X; Rudolf, Jana; Cos, Paul; Coombs, Graham H; Maes, Louis; Haemers, Achiel; Mottram, Jeremy C; Augustyns, Koen.

Bioorg Med Chem Lett; 20(6): 2001-6, 2010 Mar 15.

Artículo en Inglés | MEDLINE | ID: mdl-20167486

3.

Efforts towards an On-Target Version of the Groebke-Blackburn-Bienaymé (GBB) Reaction for Discovery of Druglike Urokinase (uPA) Inhibitors.

Gladysz, Rafaela; Vrijdag, Johannes; Van Rompaey, Dries; Lambeir, Anne-Marie; Augustyns, Koen; De Winter, Hans; Van der Veken, Pieter.

Chemistry; 25(53): 12380-12393, 2019 Sep 20.

Artículo en Inglés | MEDLINE | ID: mdl-31298443

4.

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

Elvas, Filipe; Vanden Berghe, Tom; Adriaenssens, Yves; Vandenabeele, Peter; Augustyns, Koen; Staelens, Steven; Stroobants, Sigrid; Van der Veken, Pieter; Wyffels, Leonie.

Org Biomol Chem; 17(19): 4801-4824, 2019 05 15.

Artículo en Inglés | MEDLINE | ID: mdl-31033991

5.

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

Tanc, Muhammet; Cleenewerck, Matthias; Kurdi, Ammar; Roelandt, Ria; Declercq, Wim; De Meyer, Guido; Augustyns, Koen; Martinet, Wim; Van der Veken, Pieter.

Bioorg Chem; 87: 163-168, 2019 06.

Artículo en Inglés | MEDLINE | ID: mdl-30884310

6.

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

Sassetti, Elisa; Durante Cruz, Cristina; Tammela, Päivi; Winterhalter, Mathias; Augustyns, Koen; Gribbon, Philip; Windshügel, Björn.

Int J Mol Sci; 20(11)2019 May 31.

Artículo en Inglés | MEDLINE | ID: mdl-31159170

7.

ClpP Protease, a Promising Antimicrobial Target.

Moreno-Cinos, Carlos; Goossens, Kenneth; Salado, Irene G; Van Der Veken, Pieter; De Winter, Hans; Augustyns, Koen.

Int J Mol Sci; 20(9)2019 May 07.

Artículo en Inglés | MEDLINE | ID: mdl-31067645

8.

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.

Missault, Stephan; Peeters, Lore; Amhaoul, Halima; Thomae, David; Van Eetveldt, Annemie; Favier, Barbara; Thakur, Anagha; Van Soom, Jeroen; Pitkänen, Asla; Augustyns, Koen; Joossens, Jurgen; Staelens, Steven; Dedeurwaerdere, Stefanie.

Epilepsia; 58(9): 1615-1625, 2017 09.

Artículo en Inglés | MEDLINE | ID: mdl-28722103

9.

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

Vazquez, Naiara; Missault, Stephan; Vangestel, Christel; Deleye, Steven; Thomae, David; Van der Veken, Pieter; Augustyns, Koen; Staelens, Steven; Dedeurwaerdere, Stefanie; Wyffels, Leonie.

J Labelled Comp Radiopharm; 60(1): 69-79, 2017 01.

Artículo en Inglés | MEDLINE | ID: mdl-28004430

10.

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

Ariën, Kevin K; Venkatraj, Muthusamy; Michiels, Johan; Joossens, Jurgen; Vereecken, Katleen; Van der Veken, Pieter; Heeres, Jan; De Winter, Hans; Heyndrickx, Leo; Augustyns, Koen; Vanham, Guido.

J Antimicrob Chemother; 71(5): 1159-68, 2016 May.

Artículo en Inglés | MEDLINE | ID: mdl-26850721

11.

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

Busek, Petr; Vanickova, Zdislava; Hrabal, Petr; Brabec, Marek; Fric, Premysl; Zavoral, Miroslav; Skrha, Jan; Kmochova, Klara; Laclav, Martin; Bunganic, Bohus; Augustyns, Koen; Van Der Veken, Pieter; Sedo, Aleksi.

Pancreatology; 16(5): 829-38, 2016.

Artículo en Inglés | MEDLINE | ID: mdl-27320722

12.

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

Ryabtsova, Oksana; Joossens, Jurgen; Van Der Veken, Pieter; Vanden Berghe, Wim; Augustyns, Koen; De Winter, Hans.

Bioorg Med Chem Lett; 26(20): 5032-5038, 2016 10 15.

Artículo en Inglés | MEDLINE | ID: mdl-27612544

13.

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

Maggi, Agnese; Ruivo, Eduardo; Fissers, Jens; Vangestel, Christel; Chatterjee, Sneha; Joossens, Jurgen; Sobott, Frank; Staelens, Steven; Stroobants, Sigrid; Van Der Veken, Pieter; Wyffels, Leonie; Augustyns, Koen.

Org Biomol Chem; 14(31): 7544-51, 2016 Aug 21.

Artículo en Inglés | MEDLINE | ID: mdl-27431745

14.

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

Gladysz, Rafaela; Cleenewerck, Matthias; Joossens, Jurgen; Lambeir, Anne-Marie; Augustyns, Koen; Van der Veken, Pieter.

Chembiochem; 15(15): 2238-47, 2014 Oct 13.

Artículo en Inglés | MEDLINE | ID: mdl-25154878

15.

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

Grammen, Carolien; Baes, Myriam; Haenen, Steven; Verguts, Jasper; Augustyns, Koen; Zydowsky, Thomas; La Colla, Paolo; Augustijns, Patrick; Brouwers, Joachim.

Mol Pharm; 11(12): 4405-14, 2014 Dec 01.

Artículo en Inglés | MEDLINE | ID: mdl-25327902

16.

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

Venkatraj, Muthusamy; Ariën, Kevin K; Heeres, Jan; Joossens, Jurgen; Dirié, Bertrand; Lyssens, Sophie; Michiels, Johan; Cos, Paul; Lewi, Paul J; Vanham, Guido; Maes, Louis; Van der Veken, Pieter; Augustyns, Koen.

Bioorg Med Chem; 22(19): 5241-8, 2014 Oct 01.

Artículo en Inglés | MEDLINE | ID: mdl-25199582

17.

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

Giannese, Francesca; Berg, Maya; Van der Veken, Pieter; Castagna, Valeria; Tornaghi, Paola; Augustyns, Koen; Degano, Massimo.

Acta Crystallogr D Biol Crystallogr; 69(Pt 8): 1553-66, 2013 Aug.

Artículo en Inglés | MEDLINE | ID: mdl-23897478

18.

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

Ariën, Kevin K; Venkatraj, Muthusamy; Michiels, Johan; Joossens, Jurgen; Vereecken, Katleen; Van der Veken, Pieter; Abdellati, Saïd; Cuylaerts, Vicky; Crucitti, Tania; Heyndrickx, Leo; Heeres, Jan; Augustyns, Koen; Lewi, Paul J; Vanham, Guido.

J Antimicrob Chemother; 68(9): 2038-47, 2013 Sep.

Artículo en Inglés | MEDLINE | ID: mdl-23645585

19.

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

Matheeussen, Veerle; Waumans, Yannick; Martinet, Wim; Van Goethem, Sebastiaan; Van der Veken, Pieter; Scharpé, Simon; Augustyns, Koen; De Meyer, Guido R Y; De Meester, Ingrid.

Basic Res Cardiol; 108(3): 350, 2013 May.

Artículo en Inglés | MEDLINE | ID: mdl-23608773

20.

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

Ryabtsova, Oxana; Jansen, Koen; Van Goethem, Sebastiaan; Joossens, Jurgen; Cheng, Jonathan D; Lambeir, Anne-Marie; De Meester, Ingrid; Augustyns, Koen; Van der Veken, Pieter.

Bioorg Med Chem Lett; 22(10): 3412-7, 2012 May 15.

Artículo en Inglés | MEDLINE | ID: mdl-22525314

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