2017

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. A modular and generalizable route to potent, selective and pharmacologically compliant inhibitors of rhomboid proteases, Cell Chem. Biol., accepted.

55. Van Kersavond, T.; Nguyen, M. ; Verhelst, S. H. L. Synthesis and application of activity-based probes for proteases, Methods Mol. Biol. 1574: 255-266.

54. Wolf, E. V.; Verhelst, S. H. L. 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. Cleavable linkers in chemical proteomics applications. Methods Mol. Biol., 1491: 185-203.

52. Verhelst, S. H. L. Intramembrane proteases as drug targets. FEBS J., 284: 1489-1502.

2016

51. Verdoes, M.; Verhelst, S. H. L. Detection of protease activity in cells and animals. Biochemical Biophysical Acta, 1864: 130-142.

50. Wolf, E. V.; Verhelst, S. H. L. 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

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.