Publications

2010-1995

S. Weinert, S. Jabs, C. Supanchart, M. Schweizer, N. Gimber, M. Richter, J. Rademann, T. Stauber, U. Kornak, T. J. Jentsch,
„Lysosomal Pathology and Osteopetrosis upon Loss of H⁺-Driven Lysosomal Cl^- Accumulation", Science 2010, 1401-1403.

Ahsanullah, J. Rademann
„Cyclative cleavage of azido-peptidyl-phosphoranes delivers locked cis-triazolyl-cyclopeptides as privileged protein binders”, Angew. Chem. 2010, in press.

A. Schreiber, S. Rolle, L. Peripelittschenko, J. Rademann, W. Schneider, F. C. Luft, R. Kettritz
„Phosphoinositol-3-kinase y plays a fundamental role in antineutrophil cytoplasmic antoantibody (ANCA)-induced necrotizing crescentic glomerulonephritis"
Kidney Int. 2010, 77, 118-128.

G. Stübs, B. Rupp, R. R. Schumann, N. W. J. Schröder, J. Rademann
„Chemoenzymatic synthesis of a glycolipid antigen library and elucidation of the immunoreactive epitope for construction of a vaccine against Lyme Disease"
Chemistry- A European Journal 2010, 16, 3536-3544.
Pubmed

A. El-Dahshan, Ahsanullah, J. Rademann
„Access to peptidylketones and - diketones via C-alkylations and C-acylations of polymer-supported phosphorus ylides followed by hydrolytic or oxidative cleavage"
Biopolymers-Peptide Science 2010, 94, 220-228.

M. Grättinger, P. Gribbon, J. Lenz, R. Frank, J. P. von Kries, R. Kühne, J. Rademann
„Advancing academic drug discovery“
Screening 2009, 10, 17-19.

M. Schmidt,  J. Rademann
„Dynamic, template-assisted strategies in fragment-based drug discovery"
Trends in Biotechnol. 2009, 27, 512-521.
Pubmed

M. Schmidt, A. El-Dahshan, S. Keller, J. Rademann
„Selective identification of cooperatively binding fragments in a high-throughput ligation assay enables the evolution of a picomolar caspase-3 inhibitor”
Angew. Chem. 2009, 121, 6464-6467; Angew. Chem. Int. Ed. 2009, 48, 6346-6349.
PubMed

Ahsanullah, P. Schmieder, R. Kühne, J. Rademann,
„Metal-free, regioselective triazole ligations deliver locked cis-peptide mimetics”
Angew. Chem. 2009, 121, 5143-5147; Angew. Chem. Int. Ed. 2009, 48, 5042-5045.
PubMed

I. R. Ruttekolk, F. Duchardt, R. Fischer, K.-H. Wiesmüller, J. Rademann, R. Brock
„HPMA as a scaffold for the modular assembly of functional peptide polymers by native chemical ligation”
Bioconj. Chem. 2008, 19, 2081-2087.
PubMed

V. Uryga-Polowy, D. Kosslick, C. Freund, J. Rademann
„Resin-bound aminofluorescein for C-terminal labeling of peptides: high-affinity polarization probes binding to polyproline-specific GYF domains.”
Chembiochem. 2008, 9, 2452-2462.
PubMed

K. Hellmuth, S. Grosskopf, C. T. Lum, M. Würtele, N. Röder, J. P. von Kries, M. Rosario, J. Rademann, W. Birchmeier
„Specific Inhibitors of the Protein Tyrosine Phosphatase Shp2 Identified by High-throughput Docking”
Proc. Nat. Acad. Sci. USA 2008, 105, 7275-7280.
PubMed

J. Rademann
„Combinatorial Chemistry - Concepts and Methods for Tasks of Molecular Optimization” in: Encyclopedic Reference of Molecular Pharmacology, S. Offermanns, W. Rosenthal (Eds.),
257-261, Springer, Heidelberg, 2008.

S. Beligny, J. Rademann
„Oxidizing and reducing agents”, in: The power of functional resins in organic synthesis, J. Tulla-Puche and F. Albericio (eds.)
Wiley-VCH, Weinheim 2008, 83-99.

M. Schmidt, A. Isidro-Llobet, A. El-Dahshan, M. Lisurek, J. Tan, R. Hilgenfeld, J. Rademann
„Sensitized detection of inhibitory fragments and iterative development of non-peptidic protease inhibitors by Dynymic Ligation Screening”
Angew. Chem. 2008, 120, 3319-3323; Angew. Chem. Int. Ed. 2008, 47, 3275-3278.
PubMed

M. Lisurek, B. Rupp, J. Wichard, M. Neuenschwander, J. P. von Kries, R. Frank, J. Rademann, R. Kühne
„Design of chemical libraries with potentially bioactive compounds applying a maximum Common Substructure (MCS) concept."
Mol. Divers. 2009.
PubMed

L. M. Podust, J. P. von Kries, A. N. Eddine, Y. Kim, L. V. Yermalitskaya, R. Kuehne, H. Ouellet, T. Warrier, M. Alteköster, J. S. Lee, J. Rademann, H. Oschkinat, S. H. Kaufmann, M .R. Waterman
„Small-Moelcule Scaffolds for CYP51 Inhibitors Identified by High-Througput Screening and Defined by X-Ray Crystallography”
Antimicrob Agents Chemother. 2007, 51, 3915-3923.
PubMed

A. El-Dahshan, S. Weik, J. Rademann
„C-acylations of polymeric phosphoranylidene acetates for C-terminal variation of peptide carboxylic acids”
Org Lett. 2007, 9, 949-952.
PubMed

J. Howe, J. Bauer, J. Andrä, A. B. Schromm, M. Ernst, M. Rössle, U. Zähringer, J. Rademann, K. Brandenburg
„Biophysical characterization of synthetic rhamnolipids”
FEBS Journal 2006, 273, 5101-5112.
PubMed

J. Bauer, K. Brandenburg, U. Zähringer, J. Rademann
„Chemical synthesis of a glycolipid library by a solid phase strategy allows to elucidate the structural specificity of immune stimulation by rhamnolipids”
Chem. Eur. J. 2006, 12, 7116-7124. 
PubMed

S. I. Al-Gharabli, S. T. Ali Shah, S. Weik, M. Schmidt, J. R.Mesters, D. Kuhn, G. Klebe, R. Hilgenfeld, J. Rademann
“An efficient method for the synthesis of peptide aldehyde libraries employed in the discovery of reversible SARS coronavirus main protease (SARS-CoV Mpro) inhibitors”
ChemBioChem 2006, 7, 1048-1055.
PubMed

J. Andrä, J. Rademann, J. Howe, M. H. J. Koch, H. Heine, U. Zähringer, K. Brandenburg
“Endotoxin-like properties of a rhamnolipid exotoxin from Burkholderia (Pseudomonas) plantarii – immune cell stimulation and biophysical characterization”
Biological Chemistry 2006, 387, 301-310.
PubMed

S. Weik, T. Luksch, A. Evers, J. Böttcher, A. Hasilik, H.-G. Löffler, G. Klebe, J. Rademann
„The potential of P1 site alterations in peptidomimetic protease inhibitors as suggested by virtual screening and explored by the use of CC-coupling l inker reagents”
ChemMedChem 2006, 1,445-457.
PubMed

S. T. Ali Shah, P. Merkel, H. Ragge, M. Duszenko, J. Rademann, W. Voelter
“Stereospecific synthesis of chiral 2,3-dihydro-1,4-benzodithiine and methyl-2,3-dihydro-1,4-benzodithiine derivatives and their toxic effects on trypanosoma brucei”
ChemBioChem 2005, 6, 1438-1441.
PubMed

J. Rademann, S. Weik et al.
“1,2-Diamines for the treatment of Alzheimer´s disease”
Patentanmeldung EP 04012182.4 der Böhringer Ingelheim International GmbH am 22.05.2004. 

M. Manger, M. Scheck, H. Prinz, J.-P. von Kries, T. Langer, K. Saxena, H. Schwalbe, A. Fürstner, J. Rademann, H. Waldmann
“Discovery of Mycobacterium tuberculosis Protein Tyrosine Phosphatase A (MptpA) Inhibitors Based on Natural Product Insp ired and Fragment Based Approaches“
ChemBioChem 2005, 6, 1749-1753.
PubMed

H.-J. Egelhaaf, J. Rademann
„Understanding supported reactions in spherical compartments: A general algorithm to model and determine rate constants, diffusion coefficients and spatial product distributions”
J. Comb. Chem. 2005, 7, 929-941. 
PubMed

J. Bauer, J. Rademann
„Hydrophobically assisted switching phase synthesis: The flexible combination of solid-phase and solution-phase reactions employed for oligosaccharide preparation”
J. Am. Chem. Soc. 2005, 127, 7296-7297. 
Pubmed

G. Sorg, B. Thern, O. Mader, J. Rademann, G. Jung
„Progress in the preparation of peptide aldehydes via polymer supported IBX oxidation and scavenging by threonyl resin”
J. Pept. Science 2005, 11, 142-152. 
PubMed

M. Barth, R. Fischer, R. Brock, J. Rademann
“Reversible cross-linking of hyperbranched polymers: A strategy for the combinatorial decoration of multivalent scaffolds”
Angew. Chem. 2005, 117, 1584-1588; Angew. Chem. Int. Ed.  2005, 44, 1560-1563.
PubMed

J. Smerdka, J. Rademann, G. Jung
„Polymer-bound alkyltriazenes for mild racemization-free esterification of amino acid and peptide derivatives”
J. Pept. Science 2004, 10, 603-611. 
PubMed

J. Rademann
“Organic protein chemistry: drug discovery through the chemical modification of proteins”
Angew. Chem. 2004, 116, 4654-4656; Angew. Chem. Int. Ed.  2004, 43, 4554-4556.
PubMed

M. Barth, T. Ali Shah, J. Rademann
“High Loading Polymer Reagents based on Polycationic Ultragels. Polymer-Supported Reductions and Oxidations with Increased Efficiency”
Tetrahedron – Combinatorial Chemistry Symposium 2004, 60, 8703 -8709.

M. Barth, J. Rademann
“Tailoring Ultraresins based on the cross-linking of polyethylene imines. Comparative investigation of the chemical composition, the swelling, the mobility, the chemical accessibility, and the performance in solid phase synthesis of very high-loaded resins”
J. Comb. Chem. 2004, 6, 340-349.
PubMed

S. Weik, J. Rademann
“A Phosphorane as Supported Acylanion Equivalent. Linker Reagents for Smooth and Versatile C-C-Coupling Reactions”
Angew. Chem. 2003, 115, 2595-2598; Angew. Chem. Int. Ed. 2003, 42, 2491-2494 (including 31 pages of supplemental material).
PubMed

J. Bauer, J. Rademann
"Trimellitic anhydride linker (TAL) – highly orthogonal conversions of primary amines employed in the parallel synthesis of labeled carbohydrate derivatives" (including 5 pages supplemental material)
Tetrahedron Lett. 2003, 44, 5019 - 5023.          

J. Rademann
“Inhibition of Proteases” 
Bioorganic Chemistry, H. Wennemers, C. Schmuck (Eds.), Wiley-VCH, Weinheim, 2004, 293-295. 

J. Rademann
"Solid phase synthesis (SPS) and polymer-assisted solution phase (PASP) synthesis"
Bioorganic Chemistry, H. Wennemers, C. Schmuck (Eds.), Wiley-VCH, Weinheim, 2004, 290-293.

J. Rademann
"Novel polymer- and linker reagents employed for the preparation of protease inhibitor libraries"
Bioorganic Chemistry, H. Wennemers, C. Schmuck (Eds.), Wiley-VCH, Weinheim, 2004, 277-290.

J. Rademann
"Novel matrix-supported reaction systems for applications in synthesis and biochemistry"
Habilitationsschrift, University of Tübingen, 2002. 

J. Rademann
"Advanced polymer reagents based on activated reactants and reactive intermediates: Powerful novel tools in diversity-oriented synthesis" 
Methods in Enzymology, Vol. 369, B. A. Bunin, G. Morales (Eds.), pp 366-390, Academic Press, San Diego, 2003.

J. Rademann
"Combinatorial Chemistry – Concepts and Methods for Tasks of Molecular Optimization" 
Encyclopedic Reference of Molecular Pharmacology, S. Offermanns, W. Rosenthal (Eds.), 257-261, Springer, Heidelberg, 2003.

L. Miranda, W. Lubbell, K. Halkes, T. Groth, M. Grötli, J. Rademann, C. Gotfredsen, M. Meldal
"SPOCC-194, a new high functional group density PEG-based resin for solid-phase organic synthesis"
J. Comb. Chem. 2002, 4, 523-539.
PubMed

J. Rademann
"Polymerverbindung aufgebaut aus linearen Polymerketten"
Deutsche Patentanmeldung 102 16 513.0 vom 10.04.2002.

J. Rademann, M. Barth
"ULTRA-loaded resins based on the crosslinking of linear polyethylene imine. Improving the atom economy of polymer-supported chemistry"
Angew. Chem. 2002, 114, 3087-3090; Angew. Chem. Int. Ed. 2002, 41, 2975-2978. 

J. Rademann, G. Sorg, A. Giannis, M. Mülbauer,
"Iod(V)-Verbindungen"
Patentanmeldung 101 58 002.9 vom 22.11.2001.

J. Rademann 
"Kombinatorische Verfahren in der medizinischen Chemie"
Pharmazeutische Zeitung – Prisma 2002, 9,90-98.

K. Kröger, J. Bauer, B. Fleckenstein, J. Rademann, G. Jung, G. Gauglitz
"Epitope-mapping of transglutaminase with parallel label-free optical detection"
Biosens. Bioelectron. 2002, 7, 937-944.

P. Grosche, J. Rademann, G. Jung
"Addition to Carbon-Hetero Multiple Bonds"
In: Handbook of Combinatorial Chemistry, Ed. K. C. Nicolaou, Wiley-VCH, Weinheim, 2002, Vol. 1, 322-345.

G. Sorg, A. Mengel, G. Jung, J. Rademann
"Oxidizing Polymers: A Polymer-Supported, Recyclable Hypervalent Iodine(V) Reagent for the Efficient Conversion of Alcohols, Carbonyl Compounds, and Unsaturated Carbamates in Solution"
Angew. Chem. 2001, 113, 4532-4535; Angew. Chem. Int. Ed. 2001, 40, 4395-4397.
PubMed

J. Rademann, S. Weik
"Oxoammonium salts and their application" 
Patentanmeldung beim Deutschen Patentamt, 16.03.2001, 101 13 710.9.

J. Rademann
„Combinatorial Chemistry in the Commercial Jungle (Web Review)”
Angew. Chem. Int. Ed. 2001, 40, 2721. 

J. Rademann
"High-Throughput Synthesis. Principles and Practice. Edited by Irving Sucholeiki (Book Review)”
Angew. Chem. Int. Ed. 2001, 40, 4298. 

A. Papanikos, J. Rademann, and M. Meldal
"α-Ketocarbonyl Peptides: A General Approach to Reactive Intermediates in the Synthesis of Peptide Isosteres for Protease Inhibitor Screening on Solid Support"
J. Am. Chem. Soc. 2001, 123, 2176-2181.

J. Rademann, J. Smerdka
"Alkylations with triazenes"
Patentanmeldung beim Deutschen Patentamt, 14.01.2001, 101 02 404.5.

J. Rademann, M. Barth, R. Brock, H.-J. Egelhaaf, G. Jung
"Spatially and Temporally Resolved Single Bead Analysis. Homogeneity, Diffusion, and Adsorption in Cross-Linked Polystyrene"
Chem. Eur. J. 2001, 7, 3884-3889.

S. Weik, G. Nicholson, G. Jung, and J. Rademann
"Oxoammonium-resins as metal-free, highly reactive, versatile polymeric oxidation reagents"
Angew. Chem. 2001, 113, 1489-1492;  Angew. Chem. Int. Ed. 2001, 40, 1436-1439.
PubMed

J. Rademann, J. Smerdka, G. Jung, P. Grosche, and D. Schmid
"Alkylating polymers: Resin-Released Carbenium Ions as Versatile Reactive Intermediates in Polymer-Assisted Solution Phase Synthesis"
Angew. Chem. 2001, 113, 390-393; Angew. Chem." Int. Ed. 2001, 40, 381-385.
PubMed

J. Rademann, G. Jung
"Combinatorial bioassays" 
Transkript 2000, 6,36-38.

J. Rademann, G. Jung
"Integrating combinatorial synthesis and bioassays"
Science 2000, 287, 1947-1948.
PubMed

J. Rademann, B. Dörner, W. Kraas
"Polymer-assisted solution phase synthesis (PASP), Current methods in polymer-supported solution phase synthesis of compound libraries (trend report combinatorial chemistry)"
Nachrichten Chem. 2000, 48, 280-283.

M. Groetli, J. Rademann, T. Groth, W. Lubell, L. Miranda and M. Meldal
"Surfactant Mediated Cationic and Anionic Suspension Polymerization of PEG-based Resins in Silicon Oil; Beaded SPOCC 1500 and POEPOP 1500"
J. Comb. Chem. 2001, 3, 28-33. 

M. Groetli, C. Gotfredsen, J. Rademann, A. J. Clark, J. O. Duus, M. Meldal
"Physical Properties of Polyethylene Glycol (PEG)-based Resins for Combinatorial Solid Phase Organic Chemistry, A Comparison of PEG Cross-Linked and PEG Grafted Resins"
J. Comb. Chem. 2000, 3, 108-119.
PubMed

M. Meldal, J. Rademann, M. Groetli, K. Bock
"Identification of protease inhibitors using biocompatible resins and library synthesis"
In, Current Trends in Organic  Chemistry, Scolastico and Nicotra, Ed., Kluwer Academic/ Plenum, Dordrecht, 1999.

J. Rademann, M. Groetli, M. Meldal, K. Bock
"SPOCC- a resin for solid phase organic chemistry and enzymatic reactions on solid phase"
J. Am. Chem. Soc. 1999, 121, 5459-5465. 

J. Rademann, M. Meldal, K. Bock
"Solid Phase synthesis of peptide isosters via nucleophilic reactions with N-terminal peptide aldehydes on a polar support tailored for solid phase organic chemistry"
Chem. Eur. J. 1999, 5, 1218-1225. 

M. Meldal, J. Rademann, J. Buchardt
"PEG-based macromonomers, Chemically inert polymers prepared therefrom and the use of these polymers for organic synthesis and enzyme reactions"
patent PCT/DK99/00508, filed 29.9.1998.

A. Heckel, E. Mross, J. Rademann, R. R. Schmidt
"Oligosaccharide synthesis on controlled-pore glass as solid phase material" Synlett 1998, 171-173.

J. Rademann, A. Geyer, R. R. Schmidt
"Solid-Phase Supported Synthesis of the Branched Pentasaccharide Moiety That Occurs in Most Complex Type N-Glycan Chains"
Angew. Chem. 1998, 110, 1309-1313; Angew. Chem. Int. Ed. Engl. 1998, 37, 1241-1245.

J. Rademann
"Solid phase syntheses with carbohydrates – Synthesis of oligosaccharides, O-linked and C-linked glycopeptides"
Dissertation, University of Constance 1997.

U. K. Saha, L. S. Griffith, J. Rademann, A. Geyer, R. R. Schmidt
"An N-Acetylglucosamine-containing Glycopeptide - Synthesis and Structure Assignment"
Carbohydr. Res. 1997, 304, 21-28.

J. Rademann, R. R. Schmidt
"Repetitive Solid Phase Glycosylation on an Alkyl-thiol Polymer Leading to Sugar Oligomers Containing 1,2-trans- and 1,2-cis-Glycosidic Linkages"
J. Org. Chem. 1997, 62, 3650-3653.

R. R. Schmidt, J. Rademann
"Carbohydrate derivatives and their synthesis on solid support"
patent DE 0050/46931, filed 24.05.1996. 

J. Rademann, R. R. Schmidt
"A new method for the Solid phase synthesis of oligosaccharides"
Tetrahedron Letters 1996, 37, 2718-2719.

J. Rademann, R. R. Schmidt
"Solid-phase synthesis of a glycosylated hexapeptide of human sialophorin, using the trichloroacetimidate method"
Carbohydrate Research  1995, 269, 217-225.
PubMed