2025
117. Li, H.; Chen, S.; Claes, Z.; Lismont, C.; Vandewinkel, B.; Hussein, M. A. F.; Costa, C.F.; Imberechts, D.; Liu, Y.; Vandenberghe, W.; Verhelst, S.; Baes, M.; Fransen, M. (2025) PEX14 acts as the interface linking optineurin to cell type-selective pexophagy. J. Cell Biol., provisionally accepted.
116. Chen, S.; Sanner, M.F.; Loroch, S.; Forli, S.; Verhelst, S.H.L. (2025) Sulfoxide-diazirine (SODA) as a cleavable photoaffinity group to enable identification of photolabeled modification sites via LC-MS3. Anal. Chem., accepted.
115. Rizzollo, F.; Escamilla-Ayala, A.; Fattorelli, N.; Lysak, N.B.; More, S.; Varas, P.H.; Barrazzuol, L.; Van Den Haute, C.; Van Asselberghs, J.; Nittner, D.; Coene, J.; Venkataramani, V.; Michalke, B.; Gaillet, C.; Caneque, T.; Davidson, I.; Verhelst, S.; Vangheluwe, P.; Cali, T.; Marine, J.C.; Rodriguez, R.; Bonnereau, J.; Agostinis, P. (2025) BDH2-driven lysosome to mitochondria iron transfer shapes ferroptosis vulterability of the melanoma cell states. Nature Metabolism, accepted.
114. Mourikis, P., Benkhoff, M.; Wildeis, L.; Barcik, M.; Helten, C.; Coman, C.; Solari, F.A.; Krahn, D.; Dannenberg, L.; Ahlbrecht, S.; Zikeli, D.; Utz, A.; Trojowsky, K.; Richter, H.; Al Kassis, G.; M’Pembele, R.; Zako, S.; Huckenbeck, T.; Bauer, S.; Mchmitz, D.; Pfeiler, S.; Gerdes, N.; Dücker, S.; Pircher, J.; Zhe, Z.; Thienel, M.; Ul Ain, Q.; Keul, P.; Kirkby, N.; Sohn, D.; Budach, W.; Hohlfeld, T.; Schör, K.; Levkau, B.; Zeus, T.; Verhelst, S.H.L.; Ahrends, R.; Sickmann, A.; Mitchell, J.; Mora, S.; Manson, J.E.; Bhatt, D.L.; Landmesser, U.; Massberg, S.; Kelm, M.; Petzold, T.; Polzin, A. (2025) Icosapent ethyl reduces arterial thrombosis by inhibition of cyclooxygenase-1 induced platelet reactivity. Science Trans. Med., 17: eado0610.
.
113. Ahrends, R.; Ellis, S.R.; Verhelst, S.H.L.; Kreutz, M.R. (2025) Synaptolipidomics: Lipidomics in the study of synaptic function. TiBS, 50:156-170.
112. Korovesis, D.; Mérillat, C.; Derua, R. ; Verhelst, S.H.L. (2025) Proteome selectivity profiling of photoaffinity probes derived from imidazopyrazine-kinase inhibitors. Comms. Chem., 8: 34.
111. Gao, W.; Karsa, M.; Xiao, L.; Spurling, D.; Karsa, A.; Ronca, E.; Bongers, A.; Guo, X.; Mayoh, C.; Azfar, M.; Verhelst, S.H.L.; Tanaka, K.; Cheung; L.S, Kotecha, R.S.; Lock, R.B.; Burns, M.R.; Vangheluwe, P.; Norris, M.D.; Haber, M.; Somers, K. (2025) Polyamine depletion limits progression of acute leukaemia, Int. J. Cancer, 156: 2360-2376.
110. Azfar, M.; Gao, W.; Van den Haute, C.; Xiao, L.; Karsa, M.; Pandher, R.; Karsa, A.; Spurling, D.; Ronca, W.; Bongers, A.; Guo, X.; Mayoh, C.; Fayt; Y.; Schoofs, A.; Burns, M.; Verhelst, S.H.L.; Norris, M.D.; Haber, M.; Vangheluwe, P.; Somers, K. (2025) The polyamine transporter ATP13A3 mediates DFMO-induced polyamine uptake in neuroblastoma. Mol. Oncology, 19: 913-936.
2024
109. Ji, S.; Bach, K.; Madhav Miriyala, V.; Dohnalek, J.; Riopedre-Fernandez, M.; Lepsik, M.; Van de Plassche, M.; Vanhoutte, R.; Barniol-Xicota, M.; Moreira, R.; Strisovsky, K.*; Verhelst, S.H.L.* (2024) 4-Oxo-β-Lactams as Covalent Inhibitors of the Mitochondrial Intramembrane Protease PARL, ACS Med. Chem. Lett., 15: 2101-2106.
108. Waeterschoot, J.; Barniol-Xicota, M.; Verhelst, S.; Baatsen, P; Koos, P.; Lammertyn, J.; Casadevall-i-Solvas, X. (2024) Lipid vesicle formation by encapsulation of SMALPs in surfactant-stabilised droplets. Heliyon, 10: e37915.
107. Monnens, Y.; Theodoropoulou, A.; Rosier, K.; Bhalla, K.; Mahy, A.; Vanhoutte, R.; Meulemans, S.; Cavani, E.; Antanasijevic, A.; Lemmens, I.; Lee, J.A.; Spellicy, C.J.; Schroer, R.J.; Maselli, R.A.; Laverty, C.G.; Agostinis, P.; Pagliarini, D.J.; Verhelst, S.; Marcaida, M.J.; Rochtus, A.; Dal Peraro, M.; Creemers J.W.M. (2024) Missense variants in CMS22 patients reveal that PREPL has both enzymatic and non-enzymatic functions. J. Clin. Invest. Insight., 10: e179276.
106. Kahler, J.P.; Ji, S.; Speelman-Rooms, F.; Vanhoutte, R.; Verhelst, S.H.L. (2024) Phosphinate Esters as Novel Warheads for Quenched Activity-Based Probes Targeting Serine Proteases, ACS Chem Biol., 19: 1409-1415.
105. Skorenski, M.; Ji, S.; Verhelst, S.H.L. (2024) Covalent activity-based probes for imaging of serine proteases. Biochem. Soc. Trans., 24: 923-935.
104. Coene, J.; Wilms, S.; Verhelst, S.H.L. (2024) Photoactivatable protease inhibitors: current status and perspectives, Chem. Eur. J., 30: e202303999.
103. Sneyers, F.; Speelman-Rooms, F., Verhelst, S.H.L.; Bootman, M.D.; Bultynck, G. (2024) Cellular effects of BAPTA: is it only about Ca2+ chelation? Biochem. Biophys. Acta, Mol. Cell Res. 1871: 119589.
2023
102. Yang, J.; Carvalho, L.A.R.; Chen, S.; Ji, S.; Moreira, R.; Verhelst, S.H.L. (2023) 4-Oxo-β-Lactams as Novel Inhibitors for Rhomboid Proteases. ChemBioChem, 24: e202300418. Selected as Very Important Paper.
101. Verhelst, S.H.L. and Prothiwa, M. (2023) Chemical Probes for Profiling of MALT1 Protease Activity. ChemBioChem, 24: e202300444.
100. Ji, S. and Verhelst, S.H.L. (2023) Furin-targeting activity-based probes with phosphonates and phosphinate esters as warheads. Org. Biomol. Chem., 21: 6492-6502.
99. Fritsch, S.D.; Sukhbaatar, N.; Gonzales, K.; Träger, M.; Tran, L.; Brandstetter, S.; Wilson, J. L.; Forisch, S.; Mayr, H.; Braun, C.; Bauer, R.; Weiszmann, J.; Brenner, M.; Vanhoutte, R.; Hofmann, M.; Pirnes-Karhu, S.; Magnes, C.; Weckwerth, W.; Bock, C.; Klavins, K.; Hengstschläger, M.; Schabbauer, G.; Egger, G.; Pirinen, E.; Verhelst, S.; Weichhart, T. (2023) A commensal metabolism by macrophages to support colonic epithelial homeostasis, Cell Metabolism, 35: 1931-1943.
98. Korovesis, D.; Beard, H.A.; Gaspar, V.; Chen, S.; Zahédi, R.P.; Verhelst, S.H.L. (2023) Mapping peptide-protein interactions by amine-reactive cleavable photoaffinity reagents. ACS Omega, 8: 25487-25495.
97. Li, B.-Y.; Su, K.; Van Meervelt, L.; Verhelst, S.H.L.; Ismalaj, E.; De Borggraeve, W.M.; Demaerel, J. (2023) Ex situ generation of thiazyl trifluoride (NSF3) as a gaseous SuFEx hub. Angew. Chem. Int. Ed., 62: e202305093.
96. Chen, S.; Liang, C.; Yu, W.; Kopczynski, D.; Loroch, S.; Verhelst, S. H. L. (2023) Pepstatin-based probes for photoaffinity labeling of aspartic proteases and application in target identification. ACS Chem. Biol., 18: 686-692.
95. Sukhbaatar, N.; Schöller, M.; Fritsch, S.D.; Linke, M.; Horer, S.; Träger, M.; Mazic, M.; Forisch, S.; Gonzales, K.; Kahler, J.P.; Binder, C.; Lassnig, C.; Strobl, B.; Mueller, M.; Scheiber-Mojdehkar, B.; Gundacker, C.; Dabsch, S.; Kain, R.; Hengstschläger, M.; Verhelst, S.; Weiss, G.; Theurl, I.; Weichhart, T. (2023) Duodenal macrophages control dietary iron uptake via local degradation of transferrin, Blood, 141: 2878-2890.
94. Yang, J.; Korovesis, K.; Ji, S.; Kahler, J.P., Vanhoutte, R.*; Verhelst, S.H.L.* (2023) Efficient synthesis of an alkyne fluorophosphonate activity-based probe and applications in dual colour serine hydrolase labelling. Isr. J. Chem., 63: e202200094.
93. Kahler, J.P.; Aloi, D.; Miedes Aliaga, J.; Kerselaers, S.; Voets, T.; Vriens, J.*; Verhelst, S.*; Barniol-Xicota, M.* (2023) Clotrimazole-based modulators of the TRPM3 ion channel reveal narrow structure-activity relationship, ACS Chem. Biol., 18: 456-464.
92. Houdou, M.; Jacobs, N.; Coene, J.; Azfar, M.; Vanhoutte, R.; Van den Haute, C.; Eggermont, J.; Daniëls, V.; Verhelst, S. H. L.*; Vangheluwe, P.* (2023) Novel green fluorescent polyamines to analyze ATP13A2 and ATP13A3 activity in the mammalian polyamine transport system. Biomolecules, 13:337.
91. Vanhoutte, R.; Barniol-Xicota, M.; Chiu, W.; Vangeel, L.; Jochmans, D.; De Jonghe, S.; Zidane, H.; Barr, H.M.; London, N.; Neyts, J.; Verhelst, S.H.L. (2023) Azapeptide activity-based probes for the SARS-CoV-2 main protease enable visualization of inhibition in infected cells, Chem. Sci., 14: 1666-1672.
Featured on the front cover.
90. Solari, F. A.; Krahn, D.; Swieringa, F.; Verhelst, S. H. L.; Rassaf, T.; Tasdogan, T.; Zahedi, R. P.; Lorenz, K.; Renné, T; Heemskerk, J. W. M.; Sickmann, A. (2023) Multi-OMICS approaches to study platelet mechanisms, Curr. Opin. Chem. Biol., 73:102253.
2022
89. Codony, S.; Entrena, J.-M.; Calvó-Tusell, C.; Jora, B.; González Cano, R.; Osuna, S.; Corpas, R.; Morisseau, C.; Perez, B.; Barniol-Xicota, M.; Griñán-Ferré, C.; Pérez, C.; Rodríguez-Franco, M. I.; Martinez, A. L.; Loza, M.; Pallàs, M. ; Verhelst, S. H. L.; Sanfeliu, C.; Feixas, F.; Hammock, B.; Brea, J.; Cobos, E.; Vazquez, S. (2022) Synthesis, in vitro profiling and in vivo evaluation of benzohomoadamantane-based ureas for visceral pain: a new indication for soluble epoxide hydrolase inhibitors, J. Med. Chem., 65:13660-13680.
88. Vanhoutte, R.; Verhelst, S. H. L. (2022) Combinatorial Optimization of Activity-Based Probes for Acyl Protein Thioesterases 1 and 2, ACS Med. Chem. Lett., 13: 1144-1150.
87. Li, B.-Y.; Voets, L.; Van Lommel, R.; Hoppenbrouwers, F.; Alonso, M.; Verhelst, S. H. L.; De Borggraeve, W. M.; Demaerel, J. (2022) SuFEx-enabled, chemoselective synthesis of triflates, triflamides and triflimidates. Chem. Sci., 13: 2270-2279.
86. Rufo, N.; Korovesis, D.; Van Eygen, S.; Derua, R.; Garg, A.D.; Finotello, F.; Vara-Perez, M.; Dewaele, M., De Witte, P.A.; Alexopoulos, L.; Janssens, S.; Sinkkonen, L.; Sauter, T.; Verhelst, S. H. L., Agostinis, P. (2021) The IRE1 inhibitor KIRA6 curtails the inflammatory trait of immunogenic anticancer treatments by targeting HSP60 independent of IRE1. Cell Death Diff., 29: 230-245.
2021
85. Kahler, J.P.; Verhelst, S. H. L. (2021) Phosphinate esters as novel warheads for activity-based probes targeting serine proteases. RSC Chem. Biol., 2: 1285-1290.
84. Korovesis, D.; Beard, H. A.; Mérillat, C.; Verhelst, S. H. L. (2021) Probes for photoaffinity labeling of kinases. ChemBioChem, 2206-2218. Selected as ‘very important paper’.
83. Beard, H. A.; Korovesis, D.; Chen, S.; Verhelst, S. H. L. (2021) Cleavable linkers and their application in MS-based target identification. Mol. Omics, 17: 197-209.
82. Yang, J.; Mendowicz, R. J.; Verhelst, S. H. L. (2021) Tagged benzoxazin-4-ones as novel activity-based probes for serine proteases. ChemBioChem, 22: 1578-1581. Selected as ‘very important paper’.
81. Van Kersavond, T.; Konopatzki, R.; Van de Plassche, M. A. T.; Yang, J.; Verhelst, S. H. L. (2021) Rapid synthesis of internal peptidyl a-ketoamides by on resin oxidation for the construction of rhomboid protease inhibitors. RSC Adv., 11: 4196-4199.
80. Barniol-Xicota, M.; Verhelst, S. H. L. (2021) Comparative analysis of maleic acid copolymer-based lipid nanodiscs reveals preferential lipid and protein solubilization. Communications Biol., 4: 218.
79. Hamouda, N.N.; Van Den Haute, C.; Vanhoutte, R.; Sannerud, R.; Azfar, M.; Mayer, R.; Cortes-Calabuig, A.; Swinnen, J. V.; Agostinis, P.; Baekelandt, V.; Annaert, W.; Impens, F.; Verhelst, S. H. L.; Eggermont, J.; Martin, S.; Vangheluwe, P. (2021) ATP13A3 is a new member of the mammalian polyamine transport system. J. Biol. Chem., 296:100182.
2020
78. Verhelst, S. H. L.; Bonger, K. M.; Willems, L. I. (2020) Bioorthogonal reactions in activity-based protein profiling. Molecules, 25: 5994.
77. Korovesis, D.; Rufo, N.; Derua, R.; Agostinis, P.; Verhelst, S. H. L. (2020) Photoaffinity labeling for off-target profiling of kinase inhibitors: low selectivity profile of the IRE1 targeting imidazopyrazine-based KIRA6 inhibitor. ACS Chem. Biol., 15: 3106–3111.
76. Vanhoutte, R.; Van de Plassche, M. A. T.; Verhelst, S. H. L. (2020) Rapid solid phase construction of serine hydrolase probes results in selective activity-based probes for acyl protein thioesterases-1/2. J. Med. Chem., 63: 11845-11853.
75. Chakrabarty, S.; Verhelst, S. H. L. (2020) Controlled inhibition of apoptosis by photoactivatable caspase inhibitors. Cell Chem. Biol., 27: 1434-1440. Highlighted in The Scientist magazine, January 2021.
74. Kahler, J.P.; Lenders, S.; Van de Plassche, M. A. T.; Verhelst, S. H. L. (2020) Facile synthesis of aminomethyl phosphinate esters as serine protease inhibitors with primed site interaction. ACS Med. Chem. Lett., 11: 1739-1744.
73. Van de Plassche, M. A. T.; Barniol-Xicota, M.; Verhelst, S. H. L. (2020) Peptidyl Acyloxymethyl Ketones as Activity-Based Probes for the Main Protease of SARS-CoV-2. ChemBioChem, 21: 3383-3388. Indicated as Very Important Paper; Featured on the front cover; Highlighted in The Voice, International Student Publication, based in Leuven, January 2021.
72. Van de Plassche, M.; O’Neill, T. J.; Seeholzer, T.; Turk, B.; Krappmann, D.; Verhelst, S. H. L. (2020) Use of non-natural amino acids for the design and synthesis of a selective, cell-permeable MALT1 activity-based probe, J. Med. Chem., 6:3996-4004.
71. Kahler, J. P.; Vanhoutte, R.; Verhelst, S. H. L. (2020) Activity-based protein profiling of serine protease in immune cells. Arch. Immunol. Ther. Exp., accepted.
70. Barniol-Xicota, M.; Verhelst, S. H. L. Isolation of intramembrane proteases in membrane-like environments. Biochem. Biophys. Acta – Biomembranes , 1862(4):183-193 .
69. Van Veen, S.; Martin, S.; Van den Haute, C. Benoy, V.; Schuermans, M.; Lyons, J.; Vanhoutte, R.; Kahler, J. P.; Decuypere, J.-P.; Swinnen, J.; Annaert, W. Agostinis, P.; Ghesquière, B.; Verhelst, S.; Baekelandt, V.; Eggermont, J.; Vangheluwe, P. ATP13A2 deficiency disrupts lysosomal polyamine export. Nature, 578:419-424.
2019
68. Beard, H.; Barniol-Xicota, M.; Yang, J.; Verhelst, S. H. L. (2019) Discovery of cellular roles of intramembrane proteases, ACS Chem. Biol., 14: 2372-2388.
67. Mnatsakanyan, R.; Markoutsa, S.; Wallbrunn, K.; Roos, A.; Verhelst, S. H. L.; Zahedi, R. P. (2019) Proteome-wide detection of S-nitrosylation targets and motifs using bioorthogonal cleavable-linker-based enrichment and switch technique. Nature Comm., 10: 2195.
66. Chakrabarty, S.; Kahler, J. P.; Van de Plassche, M. A. T.; Vanhoutte, R.; Verhelst, S. H. L. (2019) Recent advances in activity-based protein profiling of proteases, Curr. Top. Microbiol. Immunol., 420: 253-281.
65. Van Kersavond, T.; Konopatzki, R.; Chakrabarty, S.; Blank-Landeshammer, B.; Sickmann, A.; Verhelst, S. H. L. (2019) Short peptides with uncleavable peptide bond mimetics as photoactivatable protease inhibitors. Molecules, 24: 206.
2018
64. Barniol-Xicota, M.; Verhelst, S. H. L. (2018) Stable and Functional Rhomboid Proteases in Lipid Nanodiscs by Using Diisobutylene/Maleic Acid Copolymers. J. Am. Chem. Soc., 140: 14557-14561.
63. Arutyunova, E.; Jiang, Z.; Yang, J.; Kulepa, A. N.; Young, H. S.; Verhelst, S.; O’Donoghue, A. J.; Lemieux, M. J. (2018) Internally quenched peptide as new model substrate for rhomboid intramembrane proteases, Biol. Chem., 399: 1389-1397.
62. Goncalves, P.; Verhelst, S. H. L. (2018) Chemical probes targeting proteases for imaging and diagnostics in cancer, in: Extracellular Targeting of Cell Signaling in Cancer: Strategies Directed at MET and RON Receptor Tyrosine Kinase Pathways (Eds. Janetka, J. W.; Benson, R. M.), Wiley-VCH, chapter 12, 351-376.
61. Nguyen, M. T. N.; Shema, G.; Zahedi, R. P.; Verhelst, S. H. L. (2018) Protease specificity profiling in a pipette tip using “charged-synchronized” proteome-derived peptide libraries, J. Proteome Res., 17: 1923-1933.
60. Vanhoutte, R.; Kahler, J. P.; Martin, S.; Van Veen, S.; Verhelst, S. H. L. (2018) Clickable polyamine derivatives as chemical probes for the polyamine transport system, ChemBioChem, 19: 907-911. Featured as inside back cover.
59. Shema, G.; Nguyen, M. T. N.; Solari, F. A.; Loroch, S.; Venne, A. S.; Kollipara, L.; Sickmann, A.; Vehelst, S. H. L.; Zahedi, R. P. (2018) Simple, scalable and ultra-sensitive tip-based identification of protease substrates, Mol. Cell. Proteomics, 17: 826-834.
58. Yang, J.; Barniol-Xicota, M.; Nguyen, M. T. N.; Tichá, A.; Strisovsky, K.; Verhelst, S. H. L. (2018) Benzoxazin-4-ones as novel, easily accessible inhibitors for rhomboid proteases, Bioorg. Med. Chem. Lett., 28: 1423-1427.
2017
57. Goel, P.; Jumpertz, T.; Mikles, D. C.; Tichá, A.; Nguyen, M. T. N.; Verhelst, S.; Hubalek, M.; Johnson, D. C.; Bachovchin, D. A.; Ogorek, I.; Pietrzik, C. U.; Strisovsky, K.; Schmidt, B.; Weggen, S. (2017) Discovery and biological evaluation of potent and selective N-methylene saccharin-derived inhibitors for rhomboid intramembrane proteases, Biochemistry, 56: 6713-6725.
56. Tichá, A.; Stanchev, S.; Vinothkumar, K. R.; Mikles, D. C.; Pachl, P.; Švehlová, K.; Nguyen, M. T. N.; Verhelst, S. H. L.; Johnson, D. C.; Bachovchin, D. A.; Lepšík, M.; Majer, P.; Strisovsky, K. (2017) A modular and generalizable route to potent, selective and pharmacologically compliant inhibitors of rhomboid proteases, Cell Chem. Biol., 24: 1523-1536. Highlighted in: Cell Chem. Biol., 24: 1431-1433.
55. Van Kersavond, T.; Nguyen, M. ; Verhelst, S. H. L. (2017) Synthesis and application of activity-based probes for proteases, Methods Mol. Biol. 1574: 255-266.
54. Wolf, E. V.; Verhelst, S. H. L. (2017) Activity-based protein profiling, in: Chemoselective and Bioorthogonal Ligation Reactions: Concepts and Applications (Eds Algar, R.; Dawson, P.; Medintz, I.), Wiley-VCH.
53. Yang, Y.; Fonovic, M.; Verhelst, S. H. L. (2017) Cleavable linkers in chemical proteomics applications. Methods Mol. Biol., 1491: 185-203.
52. Verhelst, S. H. L. (2017) Intramembrane proteases as drug targets. FEBS J., 284: 1489-1502.
2016
51. Verdoes, M.; Verhelst, S. H. L.(2016) Detection of protease activity in cells and animals. Biochemical Biophysical Acta, 1864: 130-142.
50. Wolf, E. V.; Verhelst, S. H. L. (2016) Inhibitors of rhomboid proteases. Biochimie, 122:38-47. Recommended by Faculty of 1000.
2015
49. Nguyen, M.; Van Kersavond, T.; Verhelst, S. H. L. (2015) Chemical tools for the study of intramembrane proteases. ACS Chem. Biol., 10: 2423-2434.
48. Wolf, E. V.; Zeissler, A.; Verhelst, S. H. L. (2015) Inhibitor fingerprinting of rhomboid proteases by activity-based protein profiling reveals inhibitor selectivity and rhomboid autoprocessing. ACS Chem. Biol., 10: 2325-2333.
47. Wolf, E. V.; Seybolt, M.; Hadravova, R.; Strisovsky, K.; Verhelst, S. H. L. (2015) Activity-based protein profiling of rhomboid proteases in liposomes. ChemBioChem, 16: 1616-1621.
46. Serim, S.; Baer, P.; Verhelst, S. H. L. (2015) Mixed Alkyl Aryl Phosphonate Esters as Quenched Fluorescent Activity-Based Probes for Serine Proteases. Org. Biomol. Chem., 13: 2293-2299.
45. Eitelhuber, A. C.; Vosyka, O.; Nagel, D.; Bognar, M.; Lenze, D.; Lammens, K.; Schlauderer, F.; Hlahla, D.; Hopfner, K.-P.; Lenz, G.; Hummel, M.; Verhelst, S. H. L.; Krappmann, D. (2015) Activity-based probes for detection of active MALT1 paracaspase in immune cells and lymphomas. Chem. Biol., 22: 129-138.
2014
44. Choo, J. A. L.; Thong, S. Y.; Yap, J.; Van Esch, W. J. E.; Raida, M.; Meijers, R.; Lescar, J.; Verhelst, S. H. L.; Grotenbreg, G. M. (2014) Bioorthonogal Cleavage and Exchange of Major Histocompatibility Complex Ligands employing Azobenzene-containing (Abc) peptides. Angew. Chem. Int. Ed., 53:13390-13394.
43. Haedke, U. R.; Frommel, S. C.; Hansen, F.; Hahne, H.; Kuster, B.; Bogyo, M.; Verhelst, S. H. L. (2014) Phosphoramidates as novel activity-based probes for serine proteases. ChemBioChem, 15: 1106-1110. Recommended by Faculty of 1000.
2013
42. Yang, Y.; Yang, X.; Verhelst, S. H. L. (2013) Comparative analysis of click chemistry mediated activity-based protein profiling in cell lysates. Molecules, 18: 12599-12608. Special issue Advances in Click Chemistry.
41. Serim, S.; Mayer, S. V.; Verhelst, S. H. L. (2013) Tuning Activity-Based Probe Selectivity for Serine Proteases by On-Resin ‘Click’ Construction of Peptide Diphenyl Phosphonates. Org. Biomol. Chem., 11: 5714-5721.
40. Wolf, E. V.; Zeissler, A.; Vosyka, O.; Zeiler, E.; Sieber, S. A.; Verhelst, S. H. L. (2013) A new class of rhomboid protease inhibitors discovered by activity-based fluorescence polarization. PLoS ONE, 8: e72307.
39. Schlauderer, F.; Lammens, K.; Nagel, D.; Vincendeau, M.; Eitelhuber, A. C.; Verhelst, S. H. L.; Kling, D.; Chrusciel, A.; Ruland, J.; Krappmann, D.; Hopfner, K. P. (2013) Structural analysis of phenothiazine derivatives as allosteric inhibitors of the MALT1 paracaspase. Angew. Chem. Int. Ed., 52: 10384-10387.
38. Yang, Y.; Verhelst. S. H. L. (2013) Cleavable trifunctional biotin reagents for protein labeling, capture and release. Chem. Commun. 49: 5366. Selected as ‘hot article’.
37. Verhelst, S. H. L. (2013) Probing functional tyrosines. Chem. Biol., 20: 457-458. Commentary on: Chem. Biol. 2013, 20: 541-548.
36. Vosyka, O.; Vinothkumar, K. R.; Küttler, E. V.; Brouwer, A. J.; Liskamp, R. J. M.; Verhelst, S. H. L. (2013) Activity-based probes for rhomboid proteases discovered in a mass spectrometry-based assay. Proc. Natl. Acad. Sci. USA, 110: 2472-2477.
35. Lu, H.; Wang, Z.; Shabab, M.; Oeljeklaus, J.; Verhelst, S. H.; Kaschani, F.; Kaiser, M.; Bogyo, M.; Van der Hoorn, R. A. (2013) A substrate-insipred probe monitors translocation, activation and subcellular localization of bacterial type III effector protease AvrPphB. Chem. Biol., 20: 168-176. Highlighted in: Chem. Biol. 2013, 20: 137-138.
34. Battenberg, O. A.; Yang, Y.; Verhelst, S. H. L.; Sieber, S. A. (2013) Target profiling of 4-hydroxyderricin in S. aureus reveals seryl-tRNA synthetase binding and inhibition by covalent modification. Mol. Biosyst., 9: 343-351.
33. Haedke, U.; Küttler, E. V.; Vosyka, O.; Yang, Y.; Verhelst, S. H. L. (2013) Tuning probe selectivity for chemical proteomics applications. Curr. Opin. Chem. Biol., 17: 102-109.
32. Yang, Y.; Hahne, H.; Küster, B.; Verhelst, S. H. L. (2013) A Simple and Effective Cleavable Linker for Chemical Proteomics Applications. Mol. Cell. Proteomics, 12: 237-244.
2012
31. Serim, S.; Haedke, U.; Verhelst, S. H. L. (2012) Activity-based probes for the study of proteases: recent advances and developments. ChemMedChem, 7: 1146-1159.
30. Haedke, U.; Götz, M.; Baer, P.; Verhelst, S. H. L. (2012) Alkyne derivatives of isocoumarins as clickable activity-based probes for serine proteases. Bioorg. Med. Chem., 20: 633-640.
2010
29. Vinothkumar, K. R.; Strisovsky, K.; Andreeva, A.; Christova, Y.; Verhelst, S. H. L.; Freeman, M. (2010) The structural basis for catalysis and substrate specificity of a rhomboid protease. EMBO J., 29: 3797-3809.
2009
(work from post-doc, PhD and undergraduate)
28. Ravindran, S.; Lodoen, M. B.; Verhelst, S. H. L.; Bogyo, M.; Boothroyd, J. C. (2009) 4-Bromophenacyl bromide specifically inhibits rhoptry secretion during Toxoplasma invasion. PlosOne, 4: e8143.
27. Beckham, S. A.; Piedrafita, D.; Phillips, C. I.; Samarawickrema, N.; Law, R. H. P.;Smooker, P. M.; Quinsey, N. S.; Irving, J. A.; Greenwood, S.; Verhelst, S. H. L.; Bogyo, M.; Turk, B.; Coetzer, T. H.; Wijeyewickrema, L. C.; Spithill, T. W.; Pike R. N. (2009) A major Cathepsin B protease from the liver fluke Fasciola hepatica exhibits novel biochemical properties and plays a vital role in the survival of newly excysted juvenile forms in vitro. Int. J. Biochem. Cell Biol., 41: 1601-1612.
26. Kaschani, F.; Verhelst, S. H. L.; Van Swieten, P. F.; Wang, Z.; Kaiser, M.; Overkleeft, H. S.; Bogyo, M.; Van der Hoorn, R. A. L. (2009) Minitags for small molecules: detecting targets of reactive small molecules in living plant tissues using click-chemistry. The Plant Journal, 57:373-385.
25. Yang, Z.; Fonovic, M.; Verhelst, S. H. L.; Blum, G.; Bogyo, M. (2009) Evaluation of a,b-unsaturated ketone-based probes for papain-family cysteine proteases. Bioorg. Med. Chem., 17: 1071-1078.
2007
24. Burster, T.; Marin-Esteban, V.; Boehm, B. O.; Dunn, S.; Rotzschke, O.; Falk, K.; Weber, E.; Verhelst, S. H. L.; Kalbacher, H.; Driessen, C. (2007) Design of protease-resistant myelin basic protein-derived peptides by cleavage site directed amino acid substitutions. Biochem. Pharm., 74: 1514-1523.
23. Fonovic, M.; Verhelst, S. H. L.; Sorum, M. T.; Bogyo, M. (2007) Proteomic evaluation of chemically cleavable activity based probes. Mol. Cell. Proteomics, 6: 1761-1770.
22. Sadaghiani, A. M.; Verhelst, S. H. L.; Gocheva, V.; Hill, K.; Majerova, E.; Stinson, S.; Joyce, J. A.; Bogyo, M. (2007) Design, synthesis and evaluation of in vivo potency and selectivity of epoxysuccinyl-based inhibitors of papain family cysteine proteases. Chem. Biol., 14: 499-511.
21. Verhelst, S. H. L.; Fonovic, M.; Bogyo, M. (2007) A mild chemically cleavable linker system for functional proteomic applications. Angew. Chem. Int. Ed., 46: 1284-1286.
20. Cuerrier, D.; Moldoveanu, T.; Campbell, R. L.; Kelly, J.; Yoruk, B.; Verhelst, S. H. L. ; Greenbaum, D.; Bogyo, M.; Davies, P. L. (2007) Development of calpain-specific inactivators by screening of positional-scanning epoxide libraries. J. Biol. Chem., 282: 9600-9611.
19. Sexton, K. B.; Kato, D.; Berger, A.; Fonovic, M.; Verhelst, S. H. L.; Bogyo, M. (2007) Specificity of aza-peptide electrophile activity-based probes of caspases. Cell Death Differ., 14: 727-732.
18. Sadaghiani, A. M.; Verhelst, S. H. L.; Bogyo, M. (2007) Tagging and detection strategies for activity-based proteomics. Curr. Opin. Chem. Biol., 11: 20-28.
2006
17. Sadaghiani, A. M.; Verhelst, S. H. L.; Bogyo, M. (2006) Solid phase methods for the preparation of epoxysuccinate-based inhibitors of cysteine proteases. J. Comb. Chem., 8: 802-804.
16. Yuan, F.; Verhelst, S. H. L.; Blum, G.; Coussens, L. M.; Bogyo, M. (2006) A selective activity-based probe for the papain family cysteine protease dipeptidyl peptidase I/cathepsin C. J. Am. Chem. Soc., 128: 5616-5617.
15. Verhelst, S. H. L.; Witte, M. D.; Arastu-Kapur, S.; Fonovic, M.; Bogyo, M. (2006) Novel aza peptide inhibitors and active site probes of papain family cysteine proteases. ChemBioChem, 7: 943-950.
2005
14. Kato, D.;* Verhelst, S. H. L.;* Sexton, K. B.; Bogyo, M. (2005) A general solid phase method for the preparation of diverse azapeptide probes directed against cysteine proteases. Org. Lett., 7: 5649-5652. * equal authorship.
13. Verhelst, S. H. L.; Bogyo, M. (2005) Solid phase synthesis of double headed epoxysuccinyl activity based probes for selective targeting of papain family cysteine proteases. ChemBioChem, 6: 824-827.
12. Verhelst, S. H. L.; Bogyo, M. (2005) Dissecting protein function using chemical proteomic methods. QSAR Comb. Sci., 24: 261-269.
11. Verhelst, S. H. L.; Bogyo, M. (2005) Chemical proteomics applied to target identification and drug discovery. Biotechniques, 38: 175-177.
10. Chehade, K. A. H.; Baruch, A.; Verhelst, S. H. L., Bogyo, M. (2005) An improved preparation of the activity-based probe JPM-OEt and in situ applications. Synthesis, 240-244.
9. Timmer, M. S. M.; Verhelst, S. H. L.; Grotenbreg, G. M.; Overhand, M.; Overkleeft, H. S. (2005) Carbohydrates as versatile platforms in the construction of small compound libraries. Pure & Applied Chem., 77: 1173-1182.
2004
8. Verhelst, S. H. L.; Magnée, L.; Wennekes, T.; Wiedenhof, W.; Van der Marel, G. A.; Overkleeft, H. S.; Van Boeckel, C. A. A.; Van Boom, J. H. (2004) Glycosylation of cyclitols: novel analogs of aminoglycoside antibiotics. Eur. J. Org. Chem. 11: 2404-2410.
7. Verhelst, S. H. L.; Michiels, P. J. A.; Van der Marel, G. A.; Van Boeckel, C. A. A.; Van Boom, J. H. (2004) Surface plasmon resonance evaluation of various aminoglycoside – RNA hairpin interactions reveals low degree of selectivity. ChemBioChem, 5: 937-942.
6. Verhelst, S. H. L.; Wennekes, T.; Van der Marel, G. A.; Overkleeft, H. S.; Van Boeckel, C. A. A.; Van Boom, J. H. (2004) Synthesis of orthogonally protected 2-deoxystreptamine stereoisomers. Tetrahedron 60: 2813-2822.
2003
5. Verhelst, S. H. L.; Paez Martinez, B.; Timmer, M. S. M.; Lodder, G.; Van der Marel, G. A.; Overkleeft, H. S.; Van Boom, J. H. (2003) A short chiral route towards polyhydroxylated indolizidines and quinolizidines. J. Org. Chem. 68: 9598-9603.
2002
4. Verhelst, S. H. L.; Wiedenhof, W.; Ovaa, H.; Van der Marel, G. A.; Overkleeft, H. S.; Van Boeckel, C. A. A.; Van Boom, J. H. (2002) A stereoselective route towards highly functionalized 4,6-diaminocyclohexene derivatives. Tetrahedron Lett. 43: 6451-6455.
2000
3. Shi, G. P.; Bryant, R. A. R.; Riese, R.; Verhelst, S.; Driessen, C.; Li, Z. Q.; Brömme, D.; Ploegh, H. L.; Chapman, H. A. (2000) Role for cathepsin F in invariant chain processing and major histocompatability complex class II peptide loading by macrophages. J. Exp. Med. 191: 1177-1185.
2. Bogyo, M.; Verhelst, S.; Bellingard-Dubouchaud, V.; Toba, S.; Greenbaum, D. (2000) Selective targeting of lysosomal cysteine proteases with radiolabeled electrophilic substrate analogs. Chem. Biol. 7: 27-38.
1999
1. Overkleeft, H. S.; Verhelst, S. H. L.; Pieterman, E.; Meeuwenoord, N. J.; Overhand, M.; Cohen, L. H.; Van der Marel, G. A.; Van Boom, J. H. (1999) Design and synthesis of a protein: farnesyltransferase inhibitor based on sugar amino acids. Tetrahedron Lett. 40: 4103-4106.