Search results for: Joerg Steinbach

Items from 1 to 9 out of 9 results

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Synthesis, in silico, in vitro, and in vivo investigation of 5-[11C]methoxy-substituted sunitinib, a tyrosine kinase inhibitor of VEGFR-2

Julio Caballero, Camila Muñoz, Jans H. Alzate-Morales, Susana Cunha, more

European Journal of Medicinal Chemistry > 2012 > 58 > Complete > 272-280

Sunitinib ^® (SU11248) is a highly potent tyrosine kinase inhibitor targeting vascular endothelial growth factor receptor (VEGFR). Radiolabeled inhibitors of receptor tyrosine kinases (RTKs) might be useful tools for monitoring RTKs levels in tumor tissue giving valuable information for anti-angiogenic therapy. Herein we report the synthesis of 5-methoxy-sunitinib 5 and its ¹¹ C-radiolabeled...

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18F-Labeled phosphopeptide-cell-penetrating peptide dimers with enhanced cell uptake properties in human cancer cells

Susan Richter, Vincent Bouvet, Melinda Wuest, Ralf Bergmann, more

Nuclear Medicine and Biology > 2012 > 39 > 8 > 1202-1212

Phosphopeptides represent interesting compounds to study and elucidate cellular protein phosphorylation/dephosphorylation processes underlying various signal transduction pathways. However, studies of phosphopeptide action in cells are severely constrained by the negatively charged phosphate moiety of the phosphopeptide resulting in poor transport through the cell membrane. The following study describes...

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Radiosynthesis of a 18F-labeled 2,3-diarylsubstituted indole via McMurry coupling for functional characterization of cyclooxygenase-2 (COX-2) in vitro and in vivo

Torsten Kniess, Markus Laube, Ralf Bergmann, Fabian Sehn, more

Bioorganic & Medicinal Chemistry > 2012 > 20 > 11 > 3410-3421

The radiosynthesis of 3-(4-[ ¹⁸ F]fluorophenyl)-2-(4-methylsulfonylphenyl)-1H-indole [ ¹⁸ F]-3 as potential PET radiotracer for functional characterization of cyclooxygenase-2 (COX-2) in vitro and in vivo is described. [ ¹⁸ F]-3 was prepared by McMurry cyclization of a ¹⁸ F-labeled intermediate with low valent titanium and zinc via a two-step procedure in a remote controlled...

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Phosphopeptides with improved cellular uptake properties as ligands for the polo-box domain of polo-like kinase 1

Susan Richter, Ines Neundorf, Kristin Loebner, Martin Gräber, more

Bioorganic & Medicinal Chemistry Letters > 2011 > 21 > 16 > 4686-4689

Human polo-like kinase 1 (Plk1) is involved in cell proliferation and overexpressed in a broad variety of different cancer types. Due to its crucial role in cancerogenesis Plk1 is a potential target for diagnostic and therapeutic applications. Peptidic ligands can specifically interact with the polo-box domain (PBD) of Plk1, a C-terminal located phosphoepitope binding motif. Recently, phosphopeptide...

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Expression, purification and fluorine-18 radiolabeling of recombinant S100A4: a potential probe for molecular imaging of receptor for advanced glycation endproducts in vivo?

Susann Wolf, Cathleen Haase-Kohn, Jens Lenk, Susan Hoppmann, more

Amino Acids > 2011 > 41 > 4 > 809-820

Data concerning the pathophysiological role of extracellular S100A4, a member of the multigenic family of Ca²⁺-modulated S100 proteins, and its interaction with the receptor for advanced glycation endproducts (RAGE) or other putative receptors in tumorigenesis, metastasis, and inflammatory processes in vivo are scarce. One reason is the shortage of suitable radiotracer methods. We report a novel methodology...

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Synthesis of neurotensin(8–13)–phosphopeptide heterodimers via click chemistry

Susan Richter, Theres Ramenda, Ralf Bergmann, T. Kniess, more

Bioorganic & Medicinal Chemistry Letters > 2010 > 20 > 11 > 3306-3309

Two neurotensin(8–13)-containing peptide heterodimers were prepared via copper(I)-mediated click chemistry. The resulting peptide dimers could be obtained in 28–31% yield after HPLC purification. Neurotensin(8–13)-containing peptide dimers were used in an in vitro binding assay to determine binding affinity towards the neurotensin receptor-1 (NTR1). The determined IC ₅₀ values of 8.3μM and...

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Scavenger receptors are associated with cellular interactions of S100A12 in vitro and in vivo

Susan Hoppmann, Joerg Steinbach, Jens Pietzsch

International Journal of Biochemistry and Cell Biology > 2010 > 42 > 5 > 651-661

Increased plasma levels of S100 proteins and interaction of S100 proteins with receptor for advanced glycation end products (RAGE) have been associated with a number of disease states, including chronic inflammatory processes and atherosclerosis. However, data concerning the role of circulating S100 proteins in these pathologies in vivo are scarce and, furthermore, it is currently not known whether...