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Publications
2011
Fonovic, M.; Verhelst, S. H. L. (2011) Novel cleavable activity-based probes
suitable for proteomics-based discovery. Methods.
Mol. Biol., in press.
Haedke, U.; Götz, M.; Baer, P.; Verhelst, S. H. L. (2011) Alkyne
derivatives of isocoumarins as clickable activity-based probes for
serine proteases. Bioorg. Med. Chem., in press.
2010
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
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.
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.
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..
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
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.
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.
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.
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.
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.
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.
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
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.
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.
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.
2005
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.
Verhelst, S. H. L.; Bogyo, M.
(2005) Dissecting protein function using chemical proteomic methods. QSAR Comb. Sci., 24: 261-269.
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.
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.
Verhelst, S. H. L.; Bogyo, M.
(2005) Chemical proteomics applied to target identification and drug
discovery. Biotechniques, 38:
175-177.
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.
2004
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.
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.
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
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
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
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.
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
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.
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Last updated: March 2011
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