58 research outputs found
Combination of inverse electron-demand Diels-Alder reaction with highly efficient oxime ligation expands the toolbox of site-selective peptide conjugations
No full textA modular approach combining inverse electron-demand Diels-Alder coupling (DAR(inv)) and oxime ligation expands the toolbox of bioorthogonal peptide chemistry. Applicability of versatile site-specific bifunctional building blocks is demonstrated by generation of defined conjugates comprising linear, cystine-bridged and multi-disulfide functional peptides as well as their conjugation with hybrid silsesquioxane nanoparticles.DFG priority program [SPP 1623
Synthesen von N‐Lost‐Derivaten, 2. Mitt. Reaktion von N‐Bis(2‐Chlorethyl)phosphorsäureamid‐dichlorid mit 1‐Aminopropan‐2,3‐diol
No full textSynthesis of unsymmetrical disulfides with thiolsulfonates immobilised on a polystyrene support
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Treatment of glioblastoma multiforme cells with temozolomide-BioShuttle ligated by the inverse Diels-Alder ligation chemistry
No full textKlaus Braun1, Manfred Wiessler1, Volker Ehemann2, Ruediger Pipkorn3, Herbert Spring4, Juergen Debus5, Bernd Didinger5, Mario Koch3, Gabriele Muller6, Waldemar Waldeck61German Cancer Research Center, Dept of Imaging and Radiooncology, Heidelberg, Germany; 2University of Heidelberg, Institute of Pathology, Heidelberg, Germany; 3German Cancer Research Center, Central Peptide Synthesis Unit, Heidelberg, Germany; 4German Cancer Research Center, Dept of Structural Analysis of Gene Structure and Function, Heidelberg, Germany; 5University of Heidelberg, Dept of Radiation Oncology, Heidelberg, Germany; 6German Cancer Research Center,Division of Biophysics of Macromolecules, Heidelberg, GermanyAbstract: Recurrent glioblastoma multiforme (GBM), insensitive against most therapeutic interventions, has low response and survival rates. Temozolomide (TMZ) was approved for second-line therapy of recurrent anaplastic astrocytoma. However, TMZ therapy in GBM patients reveals properties such as reduced tolerability and inauspicious hemogram. The solution addressed here concerning GBM therapy consolidates and uses the potential of organic and peptide chemistry with molecular medicine. We enhanced the pharmacologic potency with simultaneous reduction of unwanted adverse reactions of the highly efficient chemotherapeutic TMZ. The TMZ connection to transporter molecules (TMZ-BioShuttle) was investigated, resulting in a much higher pharmacological effect in glioma cell lines and also with reduced dose rate. From this result we can conclude that a suitable chemistry could realize the ligation of pharmacologically active, but sensitive and highly unstable pharmaceutical ingredients without functional deprivation. The TMZ-BioShuttle dramatically enhanced the potential of TMZ for the treatment of brain tumors and is an attractive drug for combination chemotherapy.Keywords: drug delivery, carrier molecules, facilitated transport, glioblastoma multiforme, temozolomid
The profile of urinary metabolites of 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone in rats is determined by its pulmonary metabolism
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