Dr. ir. Dirk T.S. Rijkers

 

Academic Guest

Location:

HCI G-322 (Lab); HCI G-329 (Office)

Phone:

+41-44-633 4167

e-mail:

Dirk Rijkers

Education

8/1985-8/1990:

Eindhoven University of Technology (TU/e), chemical engineering with a major in bioorganic chemistry with Prof. Dr. H.M. Buck; master thesis: 'Synthesis and conformational analysis of well-defined phosphate-methylated d(Cp*Gp*Cp*G) tetramers as model compounds for the B→Z conformational change of natural DNA' (graduation August 28, 1990)

10/1990-9/1994:

Catholic University of Nijmegen (Radboud University Nijmegen), PhD degree in bioorganic chemistry with Prof. Dr. G.I. Tesser; thesis: 'Synthetic substrates for thrombin: Peptide p-nitroanilides in the continuous monitoring of the thrombin generation curve' (graduation January 10, 1995)

10/1994-9/1997:

Post-doc at Maastricht University (the Netherlands) with Prof. Dr. H.C. Hemker and Dr. S. Béguin; 'Implementation of the endogenous thrombin potential (ETP) as a routine coagulation assay in the clinical chemistry laboratory' and 'Application of snake venoms in the ETP assay'

10/1997-9/2000:

Post-doc at Utrecht University with Prof. Dr. Rob M.J. Liskamp in collaboration with Dr. J.A.J. den Hartog and Dr. G. Visser, Solvay Pharmaceuticals, Weesp, The Netherlands; 'Design and synthesis of peptide-based corticotrophin releasing factor (CRF) antagonists'

10/2000-9/2003:

Junior assistant professor medicinal chemistry with Prof. Dr. Rob M.J. Liskamp

10/2003-present:

Assistant professor medicinal chemistry and chemical biology with Prof. Dr. Rob M.J. Liskamp

4/2008-3/2009:

Visiting professor at the Eidgen÷ssische Technische Hochschule (ETH) Zürich, Switzerland with Prof. Dr. Franšois Diederich (Laboratory for Organic Chemistry)

Peptide-based acetylenic scaffolding

My research interests at Utrecht University (with Prof. Dr. Rob M.J. Liskamp) include the following topics: Development of synthetic methodology for the chemoselective ligation of unprotected peptide fragments; the design of peptides and peptidomimetics that inhibit amyloid fibrillogenesis; the incorporation of covalent constraints for the synthesis of cyclic peptides via transition metal catalyzed C-C bond formation; the design of bionanomaterials by the self-assembly of amyloid-based peptides; the synthesis of peptide-based biopolymers and their application in drug delivery/targeting; chemical approaches for the analysis of the phosphoproteome. In collaboration with Prof. Dr. Franšois Diederich (ETH Zürich), the synthesis and properties of peptide-based acetylenic scaffolds will be explored and studied.

Publications

A selection of main publications:

A.J. Brouwer, R.C. Elgersma, M. Jagodzinska, D.T.S. Rijkers, R.M.J. Liskamp, Bioorg. Med. Chem. Lett. 2008, 18, 78-84. Delayed fibril formation of amylin(20-29) by incorporation of alkene dipeptidosulfonamide isosteres obtained by solid phase olefin cross metathesis.

N. Ghalit, J.F. Reichwein, H.W. Hilbers, E. Breukink, D.T.S. Rijkers, R.M.J. Liskamp, ChemBioChem 2007, 8, 1540-1554. Synthesis of bicyclic alkene-/alkane-bridged nisin mimics by ring-closing metathesis and their biochemical evaluation as lipid II binders: toward the design of potential novel antibiotics.

I. Dijkgraaf, A.Y. Rijnders, A. Soede, A.C. Dechesne, G.W. van Esse, A.J. Brouwer, F.H.M. Corstens, O.C. Boerman, D.T.S. Rijkers, R.M.J. Liskamp, Org. Biomol. Chem. 2007, 5, 935-944. Synthesis of DOTA-conjugated multivalent cyclic-RGD peptide dendrimers via 1,3-dipolar cycloaddition and their biological evaluation: implications for tumor targeting and tumor imaging purposes.

M. van Dijk, K. Mustafa, A.C. Dechesne, C.F. van Nostrum, W.E. Hennink, D.T.S. Rijkers, R.M.J. Liskamp, Biomacromolecules 2007, 8, 327-330. Synthesis of peptide-based polymers by microwave-assisted cycloaddition backbone polymerization.

A.J. Poot, E. Ruijter, T. Nuijens, E.H.C. Dirksen, A.J.R. Heck, M. Slijper, D.T.S. Rijkers, R.M.J. Liskamp, Proteomics 2006, 6, 6394-6399. Selective enrichment of Ser/Thr-phosphorylated peptides in the presence of Ser/Thr-glycosylated peptides.

R.C. Elgersma, T. Meijneke, G. Posthuma, D.T.S. Rijkers, R.M.J. Liskamp, Chem. Eur. J. 2006, 12, 3714-3725. Self-assembly of amylin(20-29) amide bond derivatives to helical ribbons and peptide nanotubes rather than fibril formation.

H.T. ten Brink, D.T.S. Rijkers, R.M.J. Liskamp, J. Org. Chem. 2006, 71, 1817-1824. Synthesis of alkyne-bridged cyclic tripeptides toward constrained mimics of vancomycin.

P. van der Veken, E.H.C. Dirksen, E. Ruijter, R.C. Elgersma, A.J.R. Heck, D.T.S. Rijkers, M. Slijper, R.M.J. Liskamp, ChemBioChem 2005, 6, 2271-2280. Development of a novel chemical probe for the selective enrichment of phosphorylated serine- and threonine-containing peptides.

D.T.S. Rijkers, G.W. van Esse, R. Merkx, A.J. Brouwer, H.J.F. Jacobs, R.J. Pieters, R.M.J. Liskamp, Chem. Commun. 2005, 4581-4583. Efficient microwave-assisted synthesis of multivalent dendrimeric peptides using cycloaddition reaction (click) chemistry.

N. Ghalit, A.J. Poot, A. FŘrstner, D.T.S. Rijkers, R.M.J. Liskamp, Org Lett. 2005, 7, 2961-2964. Ring-closing alkyne metathesis approach toward the synthesis of alkyne mimics of thioether A, B, C and DE-ring systems of the lantibiotic nisin Z.

R. Merkx, A.J. Brouwer, D.T.S. Rijkers, R.M.J. Liskamp, Org. Lett. 2005, 7, 1125-1128. Highly efficient coupling of β-substituted aminoethane sulfonyl azides with thio acids, towards a new chemical ligation reaction.

N. Ghalit, D.T.S. Rijkers, J. Kemmink, C. Versluis, R.M.J. Liskamp, Chem. Commun. 2005, 192-194. Pre-organization induced synthesis of a crossed alkene-bridged nisin Z DE-ring mimic by ring-closing metathesis.

D.T.S. Rijkers, J.A.W. Kruijtzer, M. van Oostenbrugge, E. Ronken, J.A.J. den Hartog, R.M.J. Liskamp, ChemBioChem 2004, 5, 340-348. Structure-activity studies on the corticotropin releasing factor antagonist astressin, leading to a minimal sequence necessary for antagonistic activity.

R. Merkx, D.T.S. Rijkers, J. Kemmink, R.M.J. Liskamp, Tetrahedron Lett. 2003, 44, 4515-4518. Chemoselective coupling of peptide fragments using the Staudinger ligation.

D.T.S. Rijkers, J.W.M. H÷ppener, G. Posthuma, C.J.M. Lips, R.M.J. Liskamp, Chem. Eur. J. 2002, 8, 4285-4291. Inhibition of amyloid fibril formation of human amylin by N-alkylated amino acid and α-hydroxy acid residue containing peptides.

M.R.R. de Planque, J.-W.P. Boots, D.T.S. Rijkers, R.M.J. Liskamp, D.V. Greathouse, J.A. Killian, Biochemistry 2002, 41, 8396-8404. The effects of hydrophobic mismatch between phosphatidylcholine bilayers and transmembrane α-helical peptides depend on the nature of interfacially exposed aromatic and charged residues.

S. Wielders, M. Mukherjee, J. Michiels, D.T.S. Rijkers, J.P. Cambus, R.W.C. Knebel, V. Kakkar, H.C. Hemker, S. BÚguin, Thromb. Haemostas. 1997, 77, 629-636. The routine determination of the endogenous thrombin potential, first results in different forms of hyper- and hypocoagulation.

D.T.S. Rijkers, H.P.H.M. Adams, H.C. Hemker, G.I. Tesser, Tetrahedron 1995, 51, 11235-11250. A convenient synthesis of amino acid p-nitroanilides; synthons in the synthesis of protease substrates.

Last update: July 2008